RM65RalphMazitschekRalph Mazitschek, Ph.D.42.36272860000000-71.0843313000000064094Mazitschek, Ralph617/643-6286Assistant Professor of Radiologycatalyst:eCommonsLogineCommons Loginprns:coAuthorOfcoauthor ofprns:endDateend dateFaculty Rankprns:fullNamefull nameprns:hasAuthorListauthor listprns:hasFacultyRankhas faculty rankprns:hasNetworkhas networkprns:hasPublicationVenuepublished inprns:informationResourceReferenceinformation resource referenceprns:isPrimaryPositionis primary positionprns:latitudelatitudeprns:longitudelongitudeprns:mainImagephotoprns:maxWeightmaximum weightprns:medlineTAjournal title abbreviationprns:meshDescriptorUIMeSH DescriptorUIprns:meshSemanticGroupNameMeSH semantic group nameprns:minWeightminimum weightprns:numberOfAuthorsnumber of authorsprns:numberOfConnectionsnumber of connectionsprns:numberOfPublicationsnumber of publicationsprns:personIdPerson IDprns:personInPrimaryPositionperson in primary positionprns:physicalNeighborOfphysical neighborprns:positionInDepartmentposition in departmentprns:positionInDivisionposition in divisionprns:predicateNodepredicate nodeprns:principalInvestigatorNameprincipal investigator nameprns:publicationDatepublication dateprns:similarTosimilar toprns:sortOrdersort orderprns:startDatestart dateprns:uniquenessWeightuniqueness weightprns:yearyearAcademic ArticleArticleDocumentbibo:pmidPubMed IdentifierAddressvivo:address1address line 1vivo:address2address line 2vivo:address3address line 3vivo:addressCitycityvivo:addressPostalCodepostal codevivo:addressStatestate or provincevivo:authorInAuthorshipselected publicationsvivo:authorRankauthor rank in publicationAuthorshipDepartmentDivisionGrantvivo:hasResearchArearesearch areasvivo:hasResearcherRoleresearch activitiesvivo:hrJobTitleHR job titleInformation Resourcevivo:linkedAuthorlinked authorvivo:linkedInformationResourcelinked information resourcevivo:mailingAddressmailing addressvivo:personInPositionpositionsvivo:phoneNumberphonePositionvivo:positionInOrganizationposition in organizationvivo:preferredTitlepreferred titleResearcher Rolevivo:researcherRoleOfresearcher role ofvivo:roleContributesTocontributes tovivo:sponsorAwardIdsponsor award idrdf:predicatepredicaterdf:typetyperdfs:labellabelConceptAgentfoaf:firstNamefirst namefoaf:lastNamelast nameOrganizationPersonAuthorship 1048992429410158Vinegoni C, Feruglio PF, Gryczynski I, Mazitschek R, Weissleder RAdvanced drug delivery reviewsFluorescence anisotropy imaging in drug discovery. Adv Drug Deliv Rev. 2019 Nov - Dec; 151-152:262-288.Adv Drug Deliv Rev2018-02-02T00:00:002018Fluorescence anisotropy imaging in drug discovery.19386607Kawada J, Zou P, Mazitschek R, Bradner JE, Cohen JIThe Journal of biological chemistryTubacin kills Epstein-Barr virus (EBV)-Burkitt lymphoma cells by inducing reactive oxygen species and EBV lymphoblastoid cells by inducing apoptosis. J Biol Chem. 2009 Jun 19; 284(25):17102-17109.J Biol Chem2009-04-22T00:00:002009Tubacin kills Epstein-Barr virus (EBV)-Burkitt lymphoma cells by inducing reactive oxygen species and EBV lymphoblastoid cells by inducing apoptosis.18559893Groen AC, Needleman D, Brangwynne C, Gradinaru C, Fowler B, Mazitschek R, Mitchison TJJournal of cell scienceA novel small-molecule inhibitor reveals a possible role of kinesin-5 in anastral spindle-pole assembly. J Cell Sci. 2008 Jul 15; 121(Pt 14):2293-300.J Cell Sci2008-06-17T00:00:002008A novel small-molecule inhibitor reveals a possible role of kinesin-5 in anastral spindle-pole assembly.22473535Hendricks JA, Keliher EJ, Wan D, Hilderbrand SA, Weissleder R, Mazitschek RAngewandte Chemie (International ed. in English)Synthesis of [18F]BODIPY: bifunctional reporter for hybrid optical/positron emission tomography imaging. Angew Chem Int Ed Engl. 2012 May 07; 51(19):4603-6.Angew Chem Int Ed Engl2012-04-04T00:00:002012Synthesis of [18F]BODIPY: bifunctional reporter for hybrid optical/positron emission tomography imaging.14695616Rosenbaum C, Baumhof P, Mazitschek R, Müller O, Giannis A, Waldmann HAngewandte Chemie (International ed. in English)Synthesis and biological evaluation of an indomethacin library reveals a new class of angiogenesis-related kinase inhibitors. Angew Chem Int Ed Engl. 2004 Jan; 43(2):224-8.Angew Chem Int Ed Engl2004-01-01T00:00:002004Synthesis and biological evaluation of an indomethacin library reveals a new class of angiogenesis-related kinase inhibitors.22771460Fass DM, Reis SA, Ghosh B, Hennig KM, Joseph NF, Zhao WN, Nieland TJ, Guan JS, Kuhnle CE, Tang W, Barker DD, Mazitschek R, Schreiber SL, Tsai LH, Haggarty SJNeuropharmacologyCrebinostat: a novel cognitive enhancer that inhibits histone deacetylase activity and modulates chromatin-mediated neuroplasticity. Neuropharmacology. 2013 Jan; 64:81-96.Neuropharmacology2012-07-04T00:00:002012Crebinostat: a novel cognitive enhancer that inhibits histone deacetylase activity and modulates chromatin-mediated neuroplasticity.Authorship 1073811929932631Zhao WN, Ghosh B, Tyler M, Lalonde J, Joseph NF, Kosaric N, Fass DM, Tsai LH, Mazitschek R, Haggarty SJACS chemical neuroscienceClass I Histone Deacetylase Inhibition by Tianeptinaline Modulates Neuroplasticity and Enhances Memory. ACS Chem Neurosci. 2018 09 19; 9(9):2262-2273.ACS Chem Neurosci2018-06-22T00:00:002018Class I Histone Deacetylase Inhibition by Tianeptinaline Modulates Neuroplasticity and Enhances Memory.18285338Schuetz A, Min J, Allali-Hassani A, Schapira M, Shuen M, Loppnau P, Mazitschek R, Kwiatkowski NP, Lewis TA, Maglathin RL, McLean TH, Bochkarev A, Plotnikov AN, Vedadi M, Arrowsmith CHThe Journal of biological chemistryHuman HDAC7 harbors a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity. J Biol Chem. 2008 Apr 25; 283(17):11355-63.J Biol Chem2008-02-19T00:00:002008Human HDAC7 harbors a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity.19932094Ueno T, Kaneko K, Katano H, Sato Y, Mazitschek R, Tanaka K, Hattori S, Irie S, Sata T, Ogawa-Goto KExperimental cell researchExpansion of the trans-Golgi network following activated collagen secretion is supported by a coiled-coil microtubule-bundling protein, p180, on the ER. Exp Cell Res. 2010 Feb 01; 316(3):329-40.Exp Cell Res2009-11-27T00:00:002009Expansion of the trans-Golgi network following activated collagen secretion is supported by a coiled-coil microtubule-bundling protein, p180, on the ER.21699378Aldana-Masangkay GI, Rodriguez-Gonzalez A, Lin T, Ikeda AK, Hsieh YT, Kim YM, Lomenick B, Okemoto K, Landaw EM, Wang D, Mazitschek R, Bradner JE, Sakamoto KMLeukemia & lymphomaTubacin suppresses proliferation and induces apoptosis of acute lymphoblastic leukemia cells. Leuk Lymphoma. 2011 Aug; 52(8):1544-55.Leuk Lymphoma2011-06-23T00:00:002011Tubacin suppresses proliferation and induces apoptosis of acute lymphoblastic leukemia cells.19010849Bazzaro M, Lin Z, Santillan A, Lee MK, Wang MC, Chan KC, Bristow RE, Mazitschek R, Bradner J, Roden RBClinical cancer research : an official journal of the American Association for Cancer ResearchUbiquitin proteasome system stress underlies synergistic killing of ovarian cancer cells by bortezomib and a novel HDAC6 inhibitor. Clin Cancer Res. 2008 Nov 15; 14(22):7340-7.Clin Cancer Res2008-11-15T00:00:002008Ubiquitin proteasome system stress underlies synergistic killing of ovarian cancer cells by bortezomib and a novel HDAC6 inhibitor.22438279Derbyshire ER, Mazitschek R, Clardy JChemMedChemCharacterization of Plasmodium liver stage inhibition by halofuginone. ChemMedChem. 2012 May; 7(5):844-9.ChemMedChem2012-03-21T00:00:002012Characterization of Plasmodium liver stage inhibition by halofuginone.Authorship 126149620616024Bradner JE, Mak R, Tanguturi SK, Mazitschek R, Haggarty SJ, Ross K, Chang CY, Bosco J, West N, Morse E, Lin K, Shen JP, Kwiatkowski NP, Gheldof N, Dekker J, DeAngelo DJ, Carr SA, Schreiber SL, Golub TR, Ebert BLProceedings of the National Academy of Sciences of the United States of AmericaChemical genetic strategy identifies histone deacetylase 1 (HDAC1) and HDAC2 as therapeutic targets in sickle cell disease. Proc Natl Acad Sci U S A. 2010 Jul 13; 107(28):12617-22.Proc Natl Acad Sci U S A2010-06-28T00:00:002010Chemical genetic strategy identifies histone deacetylase 1 (HDAC1) and HDAC2 as therapeutic targets in sickle cell disease.22724584McLellan CA, Whitesell L, King OD, Lancaster AK, Mazitschek R, Lindquist SACS chemical biologyInhibiting GPI anchor biosynthesis in fungi stresses the endoplasmic reticulum and enhances immunogenicity. ACS Chem Biol. 2012 Sep 21; 7(9):1520-8.ACS Chem Biol2012-06-22T00:00:002012Inhibiting GPI anchor biosynthesis in fungi stresses the endoplasmic reticulum and enhances immunogenicity.Authorship 1100541Authorship 1216531Authorship 130744616720270Bradner JE, McPherson OM, Mazitschek R, Barnes-Seeman D, Shen JP, Dhaliwal J, Stevenson KE, Duffner JL, Park SB, Neuberg DS, Nghiem P, Schreiber SL, Koehler ANChemistry & biologyA robust small-molecule microarray platform for screening cell lysates. Chem Biol. 2006 May; 13(5):493-504.Chem Biol2006-05-01T00:00:002006A robust small-molecule microarray platform for screening cell lysates.19572548Moy TI, Conery AL, Larkins-Ford J, Wu G, Mazitschek R, Casadei G, Lewis K, Carpenter AE, Ausubel FMACS chemical biologyHigh-throughput screen for novel antimicrobials using a whole animal infection model. ACS Chem Biol. 2009 Jul 17; 4(7):527-33.ACS Chem Biol2009-07-17T00:00:002009High-throughput screen for novel antimicrobials using a whole animal infection model.21721525Hendricks JA, Keliher EJ, Marinelli B, Reiner T, Weissleder R, Mazitschek RJournal of medicinal chemistryIn vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA). J Med Chem. 2011 Aug 11; 54(15):5576-82.J Med Chem2011-07-18T00:00:002011In vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA).21874153Fass DM, Shah R, Ghosh B, Hennig K, Norton S, Zhao WN, Reis SA, Klein PS, Mazitschek R, Maglathlin RL, Lewis TA, Haggarty SJACS medicinal chemistry lettersEffect of Inhibiting Histone Deacetylase with Short-Chain Carboxylic Acids and Their Hydroxamic Acid Analogs on Vertebrate Development and Neuronal Chromatin. ACS Med Chem Lett. 2010 Oct 08; 2(1):39-42.ACS Med Chem Lett2010-10-08T00:00:002010Effect of Inhibiting Histone Deacetylase with Short-Chain Carboxylic Acids and Their Hydroxamic Acid Analogs on Vertebrate Development and Neuronal Chromatin.2019-10-31MAZITSCHEK, RALPH2017-05-23Inhibitor class dependent consequences of prolyl-tRNA synthetase inhibition in Plasmodium falciparumR21AI132981Principal InvestigatorAuthorship 113623410Authorship 1139024730773881Fagbami L, Deik AA, Singh K, Santos SA, Herman JD, Bopp SE, Lukens AK, Clish CB, Wirth DF, Mazitschek RACS infectious diseasesThe Adaptive Proline Response in P. falciparum Is Independent of PfeIK1 and eIF2a Signaling. ACS Infect Dis. 2019 04 12; 5(4):515-520.ACS Infect Dis2019-02-21T00:00:002019The Adaptive Proline Response in P. falciparum Is Independent of PfeIK1 and eIF2a Signaling.30834641Manna D, Maji B, Gangopadhyay SA, Cox KJ, Zhou Q, Law BK, Mazitschek R, Choudhary AAngewandte Chemie (International ed. in English)A Singular System with Precise Dosing and Spatiotemporal Control of CRISPR-Cas9. Angew Chem Int Ed Engl. 2019 05 06; 58(19):6285-6289.Angew Chem Int Ed Engl2019-04-02T00:00:002019A Singular System with Precise Dosing and Spatiotemporal Control of CRISPR-Cas9.D056572Chemicals & Drugs3957880.658497Histone Deacetylase InhibitorsD000962Chemicals & Drugs2529130.586424AntimalarialsD006877Chemicals & Drugs2684950.771789Hydroxamic AcidsD006655Chemicals & Drugs3977290.680553Histone DeacetylasesD000604Chemicals & Drugs68920.900071Amino Acyl-tRNA SynthetasesGeneticsImmunology and Infectious DiseasesMalaria/WirthMedicineNeurologyPMERadiologyAdult OncologyOncologyDana-Farber Cancer InstituteHarvard Medical SchoolHarvard T.H. Chan School of Public HealthMassachusetts General HospitalMassachusetts Institute of TechnologyDFW3DyannWirthDyann Fergus Wirth, Ph.D.42.33547570000000-71.1014834000000053759Wirth, DyannRichard Pearson Strong Professor of Infectious DiseasesSJH20StephenHaggartyStephen John Haggarty, Ph.D.42.36125700000000-71.0655270000000079122Haggarty, StephenAssociate Professor of NeurologyMD47ManojDuraisinghManoj T. Duraisingh, Ph.D.60621Duraisingh, ManojJohn LaPorte Given Professor of Immunology and Infectious Diseases11128selected publications3.678840.00279455511research areas1.341540.018069771coauthor of76.17069.0699160similar toPGR1PaulRichardsonPaul Gerard Guy Richardson, M.B.,B.S.42.33789600000000-71.1072493000000065832Richardson, PaulR.J. Corman Professor of MedicineAuthorship 11581231431142847Ho M, Chen T, Liu J, Dowling P, Hideshima T, Zhang L, Morelli E, Camci-Unal G, Wu X, Tai YT, Wen K, Samur M, Schlossman RL, Mazitschek R, Kavanagh EL, Lindsay S, Harada T, McCann A, Anderson KC, O'Gorman P, Bianchi GLeukemiaTargeting histone deacetylase 3 (HDAC3) in the bone marrow microenvironment inhibits multiple myeloma proliferation by modulating exosomes and IL-6 trans-signaling. Leukemia. 2020 01; 34(1):196-209.Leukemia2019-05-29T00:00:002019Targeting histone deacetylase 3 (HDAC3) in the bone marrow microenvironment inhibits multiple myeloma proliferation by modulating exosomes and IL-6 trans-signaling.KCA1KennethAndersonKenneth Carl Anderson, M.D.42.33789600000000-71.107249300000008381Anderson, KennethKraft Family Professor of MedicineHEG7HeidiGreulichHeidi E. Greulich, Ph.D.42.36272860000000-71.0843313000000039588Greulich, HeidiResearch Associate in MedicineAKL2AmandaLukensAmanda Kathleen Lukens, Ph.D.56648Lukens, AmandaVisiting ScientistJCC14JonClardyJon Clardy, Ph.D.42.33588600000000-71.1051460000000021956Clardy, JonChristopher T. Walsh, PhD Professor of Biological Chemistry and Molecular PharmacologyJEG24JamesGomezJames E. Gomez, Ph.D.42.36272860000000-71.0843313000000020104Gomez, JamesResearch Associate in GeneticsAuthorship 1162400831202891Zhao WN, Hylton NK, Wang J, Chindavong PS, Alural B, Kurtser I, Subramanian A, Mazitschek R, Perlis RH, Haggarty SJMolecular and cellular neurosciencesActivation of WNT and CREB signaling pathways in human neuronal cells in response to the Omega-3 fatty acid docosahexaenoic acid (DHA). Mol Cell Neurosci. 2019 09; 99:103386.Mol Cell Neurosci2019-06-14T00:00:002019Activation of WNT and CREB signaling pathways in human neuronal cells in response to the Omega-3 fatty acid docosahexaenoic acid (DHA).AFC3AlanCowmanAlan F. Cowman, Ph.D.42.33547570000000-71.1014834000000052396Cowman, AlanVisiting ScientistDCP1DavidPageDavid C. Page, M.D.42.36272860000000-71.0843313000000065134Page, DavidMember of the Harvard-MIT Health Sciences and Technology FacultyRW4RalphWeisslederRalph Weissleder, M.D., Ph.D.42.36125700000000-71.0655270000000048432Weissleder, RalphThrall Family Professor of RadiologyAuthorship 1529052Authorship 1440606true1Kraft Family Professor of MedicineKraft Family Professor of Medicinetrue1Research Associate in MedicineResearch Associate in Medicinetrue1Associate Professor of NeurologyAssociate Professor of Neurologytrue1R.J. Corman Professor of MedicineR.J. Corman Professor of MedicineAuthorship 1205814Authorship 16745142025-03-31MAZITSCHEK, RALPH ;WIRTH, DYANN F2020-04-01Proline homeostasis: a novel mediator of drug tolerance in Plasmodium falciparumR01AI143723Principal InvestigatorAuthorship 1239477832253314Kim Y, Sundrud MS, Zhou C, Edenius M, Zocco D, Powers K, Zhang M, Mazitschek R, Rao A, Yeo CY, Noss EH, Brenner MB, Whitman M, Keller TLProceedings of the National Academy of Sciences of the United States of AmericaAminoacyl-tRNA synthetase inhibition activates a pathway that branches from the canonical amino acid response in mammalian cells. Proc Natl Acad Sci U S A. 2020 04 21; 117(16):8900-8911.Proc Natl Acad Sci U S A2020-04-06T00:00:002020Aminoacyl-tRNA synthetase inhibition activates a pathway that branches from the canonical amino acid response in mammalian cells.Authorship 12433471432338864Badr CE, da Hora CC, Kirov AB, Tabet E, Amante R, Maksoud S, Nibbs AE, Fitzsimons E, Boukhali M, Chen JW, Chiu NHL, Nakano I, Haas W, Mazitschek R, Tannous BAACS chemical biologyObtusaquinone: A Cysteine-Modifying Compound That Targets Keap1 for Degradation. ACS Chem Biol. 2020 06 19; 15(6):1445-1454.ACS Chem Biol2020-05-08T00:00:002020Obtusaquinone: A Cysteine-Modifying Compound That Targets Keap1 for Degradation.Authorship 1269901432661007Liston SD, Whitesell L, McLellan CA, Mazitschek R, Petraitis V, Petraitiene R, Kavaliauskas P, Walsh TJ, Cowen LEAntimicrobial agents and chemotherapyAntifungal Activity of Gepinacin Scaffold Glycosylphosphatidylinositol Anchor Biosynthesis Inhibitors with Improved Metabolic Stability. Antimicrob Agents Chemother. 2020 09 21; 64(10).Antimicrob Agents Chemother2020-09-21T00:00:002020Antifungal Activity of Gepinacin Scaffold Glycosylphosphatidylinositol Anchor Biosynthesis Inhibitors with Improved Metabolic Stability.BCMPAuthorship 12873281332909004Yue H, Nowak RP, Overwijn D, Payne NC, Fischinger S, Atyeo C, Baden LR, Nilles EJ, Karlson EW, Yu XG, Li JZ, Alter G, Mazitschek R, Fischer ESmedRxiv : the preprint server for health sciencesRapid 'mix and read' assay for scalable detection of SARS-CoV-2 antibodies in patient plasma. medRxiv. 2020 Sep 03.medRxiv2020-09-03T00:00:002020Rapid 'mix and read' assay for scalable detection of SARS-CoV-2 antibodies in patient plasma.Authorship 13450024233791697Sandoval DR, Clausen TM, Nora C, Cribbs AP, Denardo A, Clark AE, Garretson AF, Coker JKC, Narayanan A, Majowicz SA, Philpott M, Johansson C, Dunford JE, Spliid CB, Golden GJ, Payne NC, Tye MA, Nowell CJ, Griffis ER, Piermatteo A, Grunddal KV, Alle T, Magida JA, Hauser BM, Feldman J, Caradonna TM, Pu Y, Yin X, McVicar RN, Kwong EM, Weiss RJ, Downes M, Tsimikas S, Smidt AG, Ballatore C, Zengler K, Evans RM, Chanda SK, Croker BA, Leibel SL, Jose J, Mazitschek R, Oppermann U, Esko JD, Carlin AF, Gordts PLSMbioRxiv : the preprint server for biologyThe Prolyl-tRNA Synthetase Inhibitor Halofuginone Inhibits SARS-CoV-2 Infection. bioRxiv. 2021 Mar 26.bioRxiv2021-03-26T00:00:002021The Prolyl-tRNA Synthetase Inhibitor Halofuginone Inhibits SARS-CoV-2 Infection.Authorship 1362083534116381El-Awady R, Saleh E, Hamoudi R, Ramadan WS, Mazitschek R, Nael MA, Elokely KM, Abou-Gharbia M, Childers WE, Srinivasulu V, Aloum L, Menon V, Al-Tel THBioorganic & medicinal chemistryDiscovery of novel class of histone deacetylase inhibitors as potential anticancer agents. Bioorg Med Chem. 2021 07 15; 42:116251.Bioorg Med Chem2021-06-08T00:00:002021Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.Authorship 1605812Authorship 1388563234434504Hideshima T, Mazitschek R, Qi J, Mimura N, Tseng JC, Kung AL, Bradner JE, Anderson KCOncotargetCorrection: HDAC6 inhibitor WT161 downregulates growth factor receptors in breast cancer. Oncotarget. 2021 Aug 17; 12(17):1736.Oncotarget2021-08-17T00:00:002021Correction: HDAC6 inhibitor WT161 downregulates growth factor receptors in breast cancer.Authorship 1404088534675420Payne NC, Kalyakina AS, Singh K, Tye MA, Mazitschek RNature chemical biologyBright and stable luminescent probes for target engagement profiling in live cells. Nat Chem Biol. 2021 11; 17(11):1168-1177.Nat Chem Biol2021-10-21T00:00:002021Bright and stable luminescent probes for target engagement profiling in live cells.Authorship 1412613734761180Poli V, Pui-Yan Ma V, Di Gioia M, Broggi A, Benamar M, Chen Q, Mazitschek R, Haggarty SJ, Chatila TA, Karp JM, Zanoni IiScienceZinc-dependent histone deacetylases drive neutrophil extracellular trap formation and potentiate local and systemic inflammation. iScience. 2021 Nov 19; 24(11):103256.iScience2021-10-11T00:00:002021Zinc-dependent histone deacetylases drive neutrophil extracellular trap formation and potentiate local and systemic inflammation.35014258Srinivasulu V, Srikanth G, Khanfar MA, Abu-Yousef IA, Majdalawieh AF, Mazitschek R, Setty SC, Sebastian A, Al-Tel THThe Journal of organic chemistryStereodivergent Complexity-to-Diversity Strategy en Route to the Synthesis of Nature-Inspired Skeleta. J Org Chem. 2022 01 21; 87(2):1377-1397.J Org Chem2022-01-11T00:00:002022Stereodivergent Complexity-to-Diversity Strategy en Route to the Synthesis of Nature-Inspired Skeleta.Authorship 14252286Authorship 228069Authorship 1439990235298895Payne NC, Mazitschek RCell chemical biologyResolving the deceptive isoform and complex selectivity of HDAC1/2 inhibitors. Cell Chem Biol. 2022 07 21; 29(7):1140-1152.e5.Cell Chem Biol2022-03-16T00:00:002022Resolving the deceptive isoform and complex selectivity of HDAC1/2 inhibitors.Authorship 3339051Authorship 3734458Authorship 1458247435649410Payne NC, Maksoud S, Tannous BA, Mazitschek RCell chemical biologyA direct high-throughput protein quantification strategy facilitates discovery and characterization of a celastrol-derived BRD4 degrader. Cell Chem Biol. 2022 08 18; 29(8):1333-1340.e5.Cell Chem Biol2022-05-31T00:00:002022A direct high-throughput protein quantification strategy facilitates discovery and characterization of a celastrol-derived BRD4 degrader.Authorship 14839131836008486Tye MA, Payne NC, Johansson C, Singh K, Santos SA, Fagbami L, Pant A, Sylvester K, Luth MR, Marques S, Whitman M, Mota MM, Winzeler EA, Lukens AK, Derbyshire ER, Oppermann U, Wirth DF, Mazitschek RNature communicationsElucidating the path to Plasmodium prolyl-tRNA synthetase inhibitors that overcome halofuginone resistance. Nat Commun. 2022 08 25; 13(1):4976.Nat Commun2022-08-25T00:00:002022Elucidating the path to Plasmodium prolyl-tRNA synthetase inhibitors that overcome halofuginone resistance.Authorship 15167772636631435Kurata K, James-Bott A, Tye MA, Yamamoto L, Samur MK, Tai YT, Dunford J, Johansson C, Senbabaoglu F, Philpott M, Palmer C, Ramasamy K, Gooding S, Smilova M, Gaeta G, Guo M, Christianson JC, Payne NC, Singh K, Karagoz K, Stokes ME, Ortiz M, Hagner P, Thakurta A, Cribbs A, Mazitschek R, Hideshima T, Anderson KC, Oppermann UBlood cancer journalProlyl-tRNA synthetase as a novel therapeutic target in multiple myeloma. Blood Cancer J. 2023 01 12; 13(1):12.Blood Cancer J2023-01-12T00:00:002023Prolyl-tRNA synthetase as a novel therapeutic target in multiple myeloma.true1Member of the Harvard-MIT Health Sciences and Technology FacultyMember of the Harvard-MIT Health Sciences and Technology FacultyAuthorship 15231692636746923Kurata K, James-Bott A, Tye MA, Yamamoto L, Samur MK, Tai YT, Dunford J, Johansson C, Senbabaoglu F, Philpott M, Palmer C, Ramasamy K, Gooding S, Smilova M, Gaeta G, Guo M, Christianson JC, Payne NC, Singh K, Karagoz K, Stokes ME, Ortiz M, Hagner P, Thakurta A, Cribbs A, Mazitschek R, Hideshima T, Anderson KC, Oppermann UBlood cancer journalCorrection: Prolyl-tRNA synthetase as a novel therapeutic target in multiple myeloma. Blood Cancer J. 2023 Feb 07; 13(1):24.Blood Cancer J2023-02-07T00:00:002023Correction: Prolyl-tRNA synthetase as a novel therapeutic target in multiple myeloma.Authorship 15599814Authorship 156414314Authorship 157030216Authorship 156233322Authorship 1563735537186406Kitson SL, Watters W, Moody TS, Chappell T, Mazitschek RJournal of labelled compounds & radiopharmaceuticalsNitrilase mediated mild hydrolysis of a carbon-14 nitrile for the radiosynthesis of 4-(7-hydroxycarbamoyl-[1-14 C-heptanoyl]-oxy)-benzoic acid methyl ester, [14 C]-SHP-141: A novel class I/II histone deacetylase (HDAC) inhibitor. J Labelled Comp Radiopharm. 2023 06; 66(7-8):172-179.J Labelled Comp Radiopharm2023-05-14T00:00:002023Nitrilase mediated mild hydrolysis of a carbon-14 nitrile for the radiosynthesis of 4-(7-hydroxycarbamoyl-[1-14 C-heptanoyl]-oxy)-benzoic acid methyl ester, [14 C]-SHP-141: A novel class I/II histone deacetylase (HDAC) inhibitor.37291337Pryce KD, Serafini RA, Ramakrishnan A, Nicolais A, Giosan IM, Polizu C, Torres-Berrío A, Vuppala S, Kronman H, Ruiz A, Gaspari S, Peña CJ, Sakloth F, Mitsi V, van Duzer J, Mazitschek R, Jarpe M, Shen L, Nestler EJ, Zachariou VNature neuroscienceOxycodone withdrawal induces HDAC1/HDAC2-dependent transcriptional maladaptations in the reward pathway in a mouse model of peripheral nerve injury. Nat Neurosci. 2023 07; 26(7):1229-1244.Nat Neurosci2023-06-08T00:00:002023Oxycodone withdrawal induces HDAC1/HDAC2-dependent transcriptional maladaptations in the reward pathway in a mouse model of peripheral nerve injury.37056371Yue H, Nowak RP, Overwijn D, Payne NC, Fischinger S, Atyeo C, Lam EC, St Denis K, Brais LK, Konishi Y, Sklavenitis-Pistofidis R, Baden LR, Nilles EJ, Karlson EW, Yu XG, Li JZ, Woolley AE, Ghobrial IM, Meyerhardt JA, Balazs AB, Alter G, Mazitschek R, Fischer ESCell reports methodsDiagnostic TR-FRET assays for detection of antibodies in patient samples. Cell Rep Methods. 2023 03 27; 3(3):100421.Cell Rep Methods2023-02-20T00:00:002023Diagnostic TR-FRET assays for detection of antibodies in patient samples.37156295Adamson RJ, Payne NC, Bartual SG, Mazitschek R, Bullock ANFree radical biology & medicineStructural and biochemical characterization establishes a detailed understanding of KEAP1-CUL3 complex assembly. Free Radic Biol Med. 2023 08 01; 204:215-225.Free Radic Biol Med2023-05-06T00:00:002023Structural and biochemical characterization establishes a detailed understanding of KEAP1-CUL3 complex assembly.37197802Armstrong JF, Campo B, Alexander SPH, Arendse LB, Cheng X, Davenport AP, Faccenda E, Fidock DA, Godinez-Macias KP, Harding SD, Kato N, Lee MCS, Luth MR, Mazitschek R, Mittal N, Niles JC, Okombo J, Ottilie S, Pasaje CFA, Probst AS, Rawat M, Rocamora F, Sakata-Kato T, Southan C, Spedding M, Tye MA, Yang T, Zhao N, Davies JABritish journal of pharmacologyAdvances in malaria pharmacology and the online guide to MALARIA PHARMACOLOGY: IUPHAR review 38. Br J Pharmacol. 2023 08; 180(15):1899-1929.Br J Pharmacol2023-06-10T00:00:002023Advances in malaria pharmacology and the online guide to MALARIA PHARMACOLOGY: IUPHAR review 38.true1Christopher T. Walsh, PhD Professor of Biological Chemistry and Molecular PharmacologyChristopher T. Walsh, PhD Professor of Biological Chemistry and Molecular PharmacologyAuthorship 1589547437737220Mandt REK, Luth MR, Tye MA, Mazitschek R, Ottilie S, Winzeler EA, Lafuente-Monasterio MJ, Gamo FJ, Wirth DF, Lukens AKeLifeDiverse evolutionary pathways challenge the use of collateral sensitivity as a strategy to suppress resistance. Elife. 2023 Sep 22; 12.Elife2023-09-22T00:00:002023Diverse evolutionary pathways challenge the use of collateral sensitivity as a strategy to suppress resistance.true1Research Associate in GeneticsResearch Associate in Geneticstrue1Thrall Family Professor of RadiologyThrall Family Professor of RadiologyAuthorship 1601840637899940Michelson D, Chin WW, Dworkin RH, Freeman R, Herrmann DN, Mazitschek R, Pop-Busui R, Shaibani A, Vornov J, Jones M, Jarpe M, Hader B, Viera T, Hylan M, Kachmar T, Jones SPain reportsA randomized, double-blind, placebo-controlled study of histone deacetylase type 6 inhibition for the treatment of painful diabetic peripheral neuropathy. Pain Rep. 2023 Dec; 8(6):e1114.Pain Rep2023-10-26T00:00:002023A randomized, double-blind, placebo-controlled study of histone deacetylase type 6 inhibition for the treatment of painful diabetic peripheral neuropathy.Authorship 16219461538241649Carrow KP, Hamilton HL, Hopps MP, Li Y, Qiao B, Payne NC, Thompson MP, Zhang X, Magassa A, Fattah M, Agarwal S, Vincent MP, Buyanova M, Bertin PA, Mazitschek R, Olvera de la Cruz M, Johnson DA, Johnson JA, Gianneschi NCAdvanced materials (Deerfield Beach, Fla.)Inhibiting the Keap1/Nrf2 Protein-Protein Interaction with Protein-Like Polymers. Adv Mater. 2024 Jan 19; e2311467.Adv Mater2024-01-19T00:00:002024Inhibiting the Keap1/Nrf2 Protein-Protein Interaction with Protein-Like Polymers.Authorship 16230051638253639Pryce KD, Serafini RA, Ramakrishnan A, Nicolais A, Giosan IM, Polizu C, Torres-Berrío A, Vuppala S, Kronman H, Ruiz A, Gaspari S, Peña CJ, Sakloth F, Mitsi V, van Duzer J, Mazitschek R, Jarpe M, Shen L, Nestler EJ, Zachariou VNature neuroscienceAuthor Correction: Oxycodone withdrawal induces HDAC1/HDAC2-dependent transcriptional maladaptations in the reward pathway in a mouse model of peripheral nerve injury. Nat Neurosci. 2024 Feb; 27(2):384.Nat Neurosci2024-02-01T00:00:002024Author Correction: Oxycodone withdrawal induces HDAC1/HDAC2-dependent transcriptional maladaptations in the reward pathway in a mouse model of peripheral nerve injury.Authorship 1627542838320555Ichikawa S, Payne NC, Xu W, Chang CF, Vallavoju N, Frome S, Flaxman HA, Mazitschek R, Woo CMCell chemical biologyThe cyclimids: Degron-inspired cereblon binders for targeted protein degradation. Cell Chem Biol. 2024 Jan 31.Cell Chem Biol2024-01-31T00:00:002024The cyclimids: Degron-inspired cereblon binders for targeted protein degradation.true1Richard Pearson Strong Professor of Infectious DiseasesRichard Pearson Strong Professor of Infectious Diseasestrue1Visiting ScientistVisiting Scientisttrue1John LaPorte Given Professor of Immunology and Infectious DiseasesJohn LaPorte Given Professor of Immunology and Infectious Diseasestrue1Assistant Professor of RadiologyAssistant Professor of Radiology2Assistant Professor in the Department of Immunology and Infectious DiseasesAssistant Professor in the Department of Immunology and Infectious Diseasestrue1Visiting ScientistVisiting ScientistAuthorship 32942311Authorship 34264312Authorship 2488603Authorship 5561901Authorship 258863Authorship 679951824113571Ageta-Ishihara N, Miyata T, Ohshima C, Watanabe M, Sato Y, Hamamura Y, Higashiyama T, Mazitschek R, Bito H, Kinoshita MNature communicationsSeptins promote dendrite and axon development by negatively regulating microtubule stability via HDAC6-mediated deacetylation. Nat Commun. 2013; 4:2532.Nat Commun2013-01-01T00:00:002013Septins promote dendrite and axon development by negatively regulating microtubule stability via HDAC6-mediated deacetylation.23913134Minami J, Suzuki R, Mazitschek R, Gorgun G, Ghosh B, Cirstea D, Hu Y, Mimura N, Ohguchi H, Cottini F, Jakubikova J, Munshi NC, Haggarty SJ, Richardson PG, Hideshima T, Anderson KCLeukemiaHistone deacetylase 3 as a novel therapeutic target in multiple myeloma. Leukemia. 2014 Mar; 28(3):680-9.Leukemia2013-08-05T00:00:002013Histone deacetylase 3 as a novel therapeutic target in multiple myeloma.Authorship 3315926Authorship 3351097Authorship 1836378Authorship 698126623954848Jochems J, Boulden J, Lee BG, Blendy JA, Jarpe M, Mazitschek R, Van Duzer JH, Jones S, Berton ONeuropsychopharmacology : official publication of the American College of NeuropsychopharmacologyAntidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology. 2014 Jan; 39(2):389-400.Neuropsychopharmacology2013-08-19T00:00:002013Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability.Authorship 3031563Authorship 7157303Authorship 7238575Authorship 715886224150220Hideshima T, Mazitschek R, Santo L, Mimura N, Gorgun G, Richardson PG, Raje N, Anderson KCLeukemiaInduction of differential apoptotic pathways in multiple myeloma cells by class-selective histone deacetylase inhibitors. Leukemia. 2014 Feb; 28(2):457-60.Leukemia2013-10-22T00:00:002013Induction of differential apoptotic pathways in multiple myeloma cells by class-selective histone deacetylase inhibitors.24624974McLellan CA, Whitesell L, King OD, Lancaster AK, Mazitschek R, Lindquist SACS chemical biologyCorrection to inhibiting GPI anchor biosynthesis in fungi stresses the endoplasmic reticulum and enhances immunogenicity. ACS Chem Biol. 2014 Apr 18; 9(4):1061.ACS Chem Biol2014-03-13T00:00:002014Correction to inhibiting GPI anchor biosynthesis in fungi stresses the endoplasmic reticulum and enhances immunogenicity.Authorship 1889092Authorship 731902324867710Dubach JM, Vinegoni C, Mazitschek R, Fumene Feruglio P, Cameron LA, Weissleder RNature communicationsIn vivo imaging of specific drug-target binding at subcellular resolution. Nat Commun. 2014 May 28; 5:3946.Nat Commun2014-05-28T00:00:002014In vivo imaging of specific drug-target binding at subcellular resolution.Authorship 25871519Authorship 735838924797834Courtis AM, Santos SA, Guan Y, Hendricks JA, Ghosh B, Szantai-Kis DM, Reis SA, Shah JV, Mazitschek RBioconjugate chemistryMonoalkoxy BODIPYs--a fluorophore class for bioimaging. Bioconjug Chem. 2014 Jun 18; 25(6):1043-51.Bioconjug Chem2014-05-14T00:00:002014Monoalkoxy BODIPYs--a fluorophore class for bioimaging.Authorship 294163Authorship 738964424596307Keliher EJ, Klubnick JA, Reiner T, Mazitschek R, Weissleder RChemMedChemEfficient acid-catalyzed (18) F/(19) F fluoride exchange of BODIPY dyes. ChemMedChem. 2014 Jul; 9(7):1368-73.ChemMedChem2014-03-05T00:00:002014Efficient acid-catalyzed (18) F/(19) F fluoride exchange of BODIPY dyes.Authorship 3409512Authorship 743972524613069Zhao T, Li Y, Liu B, Halaweish I, Mazitschek R, Alam HBThe Journal of surgical researchSelective inhibition of histone deacetylase 6 alters the composition of circulating blood cells in a lethal septic model. J Surg Res. 2014 Aug; 190(2):647-54.J Surg Res2014-02-04T00:00:002014Selective inhibition of histone deacetylase 6 alters the composition of circulating blood cells in a lethal septic model.Authorship 747947925111632Derbyshire ER, Zuzarte-Luís V, Magalhães AD, Kato N, Sanschagrin PC, Wang J, Zhou W, Miduturu CV, Mazitschek R, Sliz P, Mota MM, Gray NS, Clardy JChembiochem : a European journal of chemical biologyChemical interrogation of the malaria kinome. Chembiochem. 2014 Sep 05; 15(13):1920-30.Chembiochem2014-08-08T00:00:002014Chemical interrogation of the malaria kinome.Authorship 4683484Authorship 775857525320008Chan CT, Qi J, Smith W, Paranol R, Mazitschek R, West N, Reeves R, Chiosis G, Schreiber SL, Bradner JE, Paulmurugan R, Gambhir SSCancer researchSyntheses and discovery of a novel class of cinnamic hydroxamates as histone deacetylase inhibitors by multimodality molecular imaging in living subjects. Cancer Res. 2014 Dec 15; 74(24):7475-86.Cancer Res2014-10-15T00:00:002014Syntheses and discovery of a novel class of cinnamic hydroxamates as histone deacetylase inhibitors by multimodality molecular imaging in living subjects.Authorship 7776851125395010Herman JD, Rice DP, Ribacke U, Silterra J, Deik AA, Moss EL, Broadbent KM, Neafsey DE, Desai MM, Clish CB, Mazitschek R, Wirth DFGenome biologyA genomic and evolutionary approach reveals non-genetic drug resistance in malaria. Genome Biol. 2014; 15(11):511.Genome Biol2014-01-01T00:00:002014A genomic and evolutionary approach reveals non-genetic drug resistance in malaria.Authorship 5544148Authorship 5772625Authorship 3102083Authorship 51814012Authorship 4667268Authorship 4682465Authorship 1784543Authorship 5203127Authorship 654519Authorship 3149513Authorship 2510638Authorship 2714406Authorship 2816901Authorship 549750325546293Iaconelli J, Huang JH, Berkovitch SS, Chattopadhyay S, Mazitschek R, Schreiber SL, Haggarty SJ, Karmacharya RACS chemical biologyHDAC6 inhibitors modulate Lys49 acetylation and membrane localization of ß-catenin in human iPSC-derived neuronal cells. ACS Chem Biol. 2015 Mar 20; 10(3):883-90.ACS Chem Biol2015-01-08T00:00:002015HDAC6 inhibitors modulate Lys49 acetylation and membrane localization of ß-catenin in human iPSC-derived neuronal cells.Authorship 2352956Authorship 3640072Authorship 4507164Authorship 7918465Authorship 8047265Authorship 8038859Authorship 7923323Authorship 7963864Authorship 8063345Authorship 7957202425995223Herman JD, Pepper LR, Cortese JF, Estiu G, Galinsky K, Zuzarte-Luis V, Derbyshire ER, Ribacke U, Lukens AK, Santos SA, Patel V, Clish CB, Sullivan WJ, Zhou H, Bopp SE, Schimmel P, Lindquist S, Clardy J, Mota MM, Keller TL, Whitman M, Wiest O, Wirth DF, Mazitschek RScience translational medicineThe cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs. Sci Transl Med. 2015 May 20; 7(288):288ra77.Sci Transl Med2015-05-20T00:00:002015The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs.25479907Zhao Y, Zhou P, Liu B, Bambakidis T, Mazitschek R, Alam HB, Li YThe Journal of surgical researchProtective effect of suberoylanilide hydroxamic acid against lipopolysaccharide-induced liver damage in rodents. J Surg Res. 2015 Apr; 194(2):544-550.J Surg Res2014-11-06T00:00:002014Protective effect of suberoylanilide hydroxamic acid against lipopolysaccharide-induced liver damage in rodents.26000480Liu J, Lee J, Salazar Hernandez MA, Mazitschek R, Ozcan UCellTreatment of obesity with celastrol. Cell. 2015 May 21; 161(5):999-1011.Cell2015-05-21T00:00:002015Treatment of obesity with celastrol.25757125Li Y, Zhao T, Liu B, Halaweish I, Mazitschek R, Duan X, Alam HBThe journal of trauma and acute care surgeryInhibition of histone deacetylase 6 improves long-term survival in a lethal septic model. J Trauma Acute Care Surg. 2015 Feb; 78(2):378-85.J Trauma Acute Care Surg2015-02-01T00:00:002015Inhibition of histone deacetylase 6 improves long-term survival in a lethal septic model.25853389Ecker J, Oehme I, Mazitschek R, Korshunov A, Kool M, Hielscher T, Kiss J, Selt F, Konrad C, Lodrini M, Deubzer HE, von Deimling A, Kulozik AE, Pfister SM, Witt O, Milde TActa neuropathologica communicationsTargeting class I histone deacetylase 2 in MYC amplified group 3 medulloblastoma. Acta Neuropathol Commun. 2015 Apr 03; 3:22.Acta Neuropathol Commun2015-04-03T00:00:002015Targeting class I histone deacetylase 2 in MYC amplified group 3 medulloblastoma.25877871Guan Y, Meurer M, Raghavan S, Rebane A, Lindquist JR, Santos S, Kats I, Davidson MW, Mazitschek R, Hughes TE, Drobizhev M, Knop M, Shah JVMolecular biology of the cellLive-cell multiphoton fluorescence correlation spectroscopy with an improved large Stokes shift fluorescent protein. Mol Biol Cell. 2015 Jun 01; 26(11):2054-66.Mol Biol Cell2015-04-15T00:00:002015Live-cell multiphoton fluorescence correlation spectroscopy with an improved large Stokes shift fluorescent protein.Authorship 44467210Authorship 46246614Authorship 2978164Authorship 4393995Authorship 5355193Authorship 8340495Authorship 834150626295174Santos SA, Lukens AK, Coelho L, Nogueira F, Wirth DF, Mazitschek R, Moreira R, Paulo AEuropean journal of medicinal chemistryExploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype. Eur J Med Chem. 2015 Sep 18; 102:320-33.Eur J Med Chem2015-07-31T00:00:002015Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype.26024776Vinegoni C, Dubach JM, Thurber GM, Miller MA, Mazitschek R, Weissleder RDrug discovery todayAdvances in measuring single-cell pharmacology in vivo. Drug Discov Today. 2015 Sep; 20(9):1087-92.Drug Discov Today2015-05-27T00:00:002015Advances in measuring single-cell pharmacology in vivo.Authorship 869873726804233Ghosh B, Zhao WN, Reis SA, Patnaik D, Fass DM, Tsai LH, Mazitschek R, Haggarty SJBioorganic & medicinal chemistry lettersDissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation. Bioorg Med Chem Lett. 2016 Feb 15; 26(4):1265-1271.Bioorg Med Chem Lett2016-01-11T00:00:002016Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation.Authorship 604118Authorship 3132162Authorship 8778871326974814Reis SA, Ghosh B, Hendricks JA, Szantai-Kis DM, Törk L, Ross KN, Lamb J, Read-Button W, Zheng B, Wang H, Salthouse C, Haggarty SJ, Mazitschek RNature chemical biologyLight-controlled modulation of gene expression by chemical optoepigenetic probes. Nat Chem Biol. 2016 May; 12(5):317-23.Nat Chem Biol2016-03-14T00:00:002016Light-controlled modulation of gene expression by chemical optoepigenetic probes.2Assistant Professor1Associate Professor0Full Professor5Other FacultyAuthorship 913355Authorship 763453Authorship 49481952019-04-30MAZITSCHEK, RALPH2014-06-01Chemical Optoepigenetic Regulation of Chromatin-Mediated NeuroplasticityR01NS0882092016-06-30WEISSLEDER, RALPH2000-08-09Center for Molecular Imaging Research at MGH/HMSP50CA086355Co-Principal InvestigatorCo-Principal InvestigatorAuthorship 897662Authorship 3453753Authorship 9232141327538856Carrasco MP, Machado M, Gonçalves L, Sharma M, Gut J, Lukens AK, Wirth DF, André V, Duarte MT, Guedes RC, Dos Santos DJ, Rosenthal PJ, Mazitschek R, Prudêncio M, Moreira RChemMedChemProbing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites. ChemMedChem. 2016 10 06; 11(19):2194-2204.ChemMedChem2016-08-19T00:00:002016Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites.Authorship 932783927799547Hideshima T, Qi J, Paranal RM, Tang W, Greenberg E, West N, Colling ME, Estiu G, Mazitschek R, Perry JA, Ohguchi H, Cottini F, Mimura N, Görgün G, Tai YT, Richardson PG, Carrasco RD, Wiest O, Schreiber SL, Anderson KC, Bradner JEProceedings of the National Academy of Sciences of the United States of AmericaDiscovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma. Proc Natl Acad Sci U S A. 2016 11 15; 113(46):13162-13167.Proc Natl Acad Sci U S A2016-10-31T00:00:002016Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma.Authorship 2204764Authorship 940054527926524Huang P, Almeciga-Pinto I, Jarpe M, van Duzer JH, Mazitschek R, Yang M, Jones SS, Quayle SNOncotargetSelective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models. Oncotarget. 2017 Jan 10; 8(2):2694-2707.Oncotarget2017-01-10T00:00:002017Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models.Authorship 943939327997727Srinivasulu V, Reddy A, Mazitschek R, Lukens AK, Wirth DF, Li L, Naumov P, O'Connor MJ, Al-Tel THChemistry (Weinheim an der Bergstrasse, Germany)Intramolecular Diaza-Diels-Alder Protocol: A New Diastereoselective and Modular One-Step Synthesis of Constrained Polycyclic Frameworks. Chemistry. 2017 Mar 23; 23(17):4137-4148.Chemistry2017-02-17T00:00:002017Intramolecular Diaza-Diels-Alder Protocol: A New Diastereoselective and Modular One-Step Synthesis of Constrained Polycyclic Frameworks.Authorship 945797828023028Santo L, Hideshima T, Kung AL, Yang M, Tamang D, Jarpe M, van Duzer JH, Mazitschek R, Cirstea D, Patel K, Tseng J, Rodig S, Pozzi S, Bradner J, Anderson KC, Jones SS, Raje NSJournal of clinical oncology : official journal of the American Society of Clinical OncologyThe effect of selective inhibition of HDAC6 with ACY1215 on bortezomib activity in multiple myeloma (MM). J Clin Oncol. 2011 May 20; 29(15_suppl):e18569.J Clin Oncol2011-05-20T00:00:002011The effect of selective inhibition of HDAC6 with ACY1215 on bortezomib activity in multiple myeloma (MM).Authorship 5054433Authorship 5166059185 Cambridge StMassachusetts General HospitalSimches Research Building - 5.212185 Cambridge StBoston02114MA12481350Stieber F, Mazitschek R, Soric N, Giannis A, Waldmann HAngewandte Chemie (International ed. in English)Traceless solid-phase synthesis of 2-aminothiazoles: receptor tyrosine kinase inhibitors with dual selectivity for Tie-2 and VEGFR-2. Angew Chem Int Ed Engl. 2002 Dec 16; 41(24):4757-61.Angew Chem Int Ed Engl2002-12-16T00:00:002002Traceless solid-phase synthesis of 2-aminothiazoles: receptor tyrosine kinase inhibitors with dual selectivity for Tie-2 and VEGFR-2.15386354Kirkin V, Thiele W, Baumann P, Mazitschek R, Rohde K, Fellbrich G, Weich H, Waltenberger J, Giannis A, Sleeman JPInternational journal of cancerMAZ51, an indolinone that inhibits endothelial cell and tumor cell growth in vitro, suppresses tumor growth in vivo. Int J Cancer. 2004 Dec 20; 112(6):986-93.Int J Cancer2004-12-20T00:00:002004MAZ51, an indolinone that inhibits endothelial cell and tumor cell growth in vitro, suppresses tumor growth in vivo.Authorship 9678167Authorship 969126628267067Krukowski K, Ma J, Golonzhka O, Laumet GO, Gutti T, van Duzer JH, Mazitschek R, Jarpe MB, Heijnen CJ, Kavelaars APainHDAC6 inhibition effectively reverses chemotherapy-induced peripheral neuropathy. Pain. 2017 06; 158(6):1126-1137.Pain2017-06-01T00:00:002017HDAC6 inhibition effectively reverses chemotherapy-induced peripheral neuropathy.28245046Vieson MD, Gojmerac AM, Khan D, Dai R, van Duzer JH, Mazitschek R, Caudell DL, Liao X, Luo XM, Reilly CMHistology and histopathologyTreatment with a selective histone deacetylase 6 inhibitor decreases lupus nephritis in NZB/W mice. Histol Histopathol. 2017 Dec; 32(12):1317-1332.Histol Histopathol2017-02-28T00:00:002017Treatment with a selective histone deacetylase 6 inhibitor decreases lupus nephritis in NZB/W mice.18430569Mazitschek R, Patel V, Wirth DF, Clardy JBioorganic & medicinal chemistry lettersDevelopment of a fluorescence polarization based assay for histone deacetylase ligand discovery. Bioorg Med Chem Lett. 2008 May 01; 18(9):2809-12.Bioorg Med Chem Lett2008-04-07T00:00:002008Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.19498172Sundrud MS, Koralov SB, Feuerer M, Calado DP, Kozhaya AE, Rhule-Smith A, Lefebvre RE, Unutmaz D, Mazitschek R, Waldner H, Whitman M, Keller T, Rao AScience (New York, N.Y.)Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response. Science. 2009 Jun 05; 324(5932):1334-8.Science2009-06-05T00:00:002009Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response.15288254Mazitschek R, Giannis ACurrent opinion in chemical biologyInhibitors of angiogenesis and cancer-related receptor tyrosine kinases. Curr Opin Chem Biol. 2004 Aug; 8(4):432-41.Curr Opin Chem Biol2004-08-01T00:00:002004Inhibitors of angiogenesis and cancer-related receptor tyrosine kinases.15917904Mazitschek R, Huwe A, Giannis AOrganic & biomolecular chemistrySynthesis and biological evaluation of novel fumagillin and ovalicin analogues. Org Biomol Chem. 2005 Jun 07; 3(11):2150-4.Org Biomol Chem2005-04-22T00:00:002005Synthesis and biological evaluation of novel fumagillin and ovalicin analogues.12761741Huwe A, Mazitschek R, Giannis AAngewandte Chemie (International ed. in English)Small molecules as inhibitors of cyclin-dependent kinases. Angew Chem Int Ed Engl. 2003 May 16; 42(19):2122-38.Angew Chem Int Ed Engl2003-05-16T00:00:002003Small molecules as inhibitors of cyclin-dependent kinases.12412081Mazitschek R, Mülbaier M, Giannis AAngewandte Chemie (International ed. in English)IBX-mediated oxidation of primary alcohols and aldehydes to form carboxylic acids. Angew Chem Int Ed Engl. 2002 Nov 04; 41(21):4059-61.Angew Chem Int Ed Engl2002-11-04T00:00:002002IBX-mediated oxidation of primary alcohols and aldehydes to form carboxylic acids.10556911Wernert N, Stanjek A, Kiriakidis S, Hügel A, Jha HC, Mazitschek R, Giannis AAngewandte Chemie (International ed. in English)Inhibition of Angiogenesis In Vivo by ets-1 Antisense Oligonucleotides-Inhibition of Ets-1 Transcription Factor Expression by the Antibiotic Fumagillin. Angew Chem Int Ed Engl. 1999 Nov 02; 38(21):3228-3231.Angew Chem Int Ed Engl1999-11-02T00:00:001999Inhibition of Angiogenesis In Vivo by ets-1 Antisense Oligonucleotides-Inhibition of Ets-1 Transcription Factor Expression by the Antibiotic Fumagillin.11683876Kirkin V, Mazitschek R, Krishnan J, Steffen A, Waltenberger J, Pepper MS, Giannis A, Sleeman JPEuropean journal of biochemistryCharacterization of indolinones which preferentially inhibit VEGF-C- and VEGF-D-induced activation of VEGFR-3 rather than VEGFR-2. Eur J Biochem. 2001 Nov; 268(21):5530-40.Eur J Biochem2001-11-01T00:00:002001Characterization of indolinones which preferentially inhibit VEGF-C- and VEGF-D-induced activation of VEGFR-3 rather than VEGFR-2.12491250Stahl P, Kissau L, Mazitschek R, Giannis A, Waldmann HAngewandte Chemie (International ed. in English)Natural product derived receptor tyrosine kinase inhibitors: identification of IGF1R, Tie-2, and VEGFR-3 inhibitors. Angew Chem Int Ed Engl. 2002 Apr 02; 41(7):1174-8.Angew Chem Int Ed Engl2002-04-02T00:00:002002Natural product derived receptor tyrosine kinase inhibitors: identification of IGF1R, Tie-2, and VEGFR-3 inhibitors.16912225Mosley AJ, Meekings KN, McCarthy C, Shepherd D, Cerundolo V, Mazitschek R, Tanaka Y, Taylor GP, Bangham CRBloodHistone deacetylase inhibitors increase virus gene expression but decrease CD8+ cell antiviral function in HTLV-1 infection. Blood. 2006 Dec 01; 108(12):3801-7.Blood2006-08-15T00:00:002006Histone deacetylase inhibitors increase virus gene expression but decrease CD8+ cell antiviral function in HTLV-1 infection.11716712Stahl P, Kissau L, Mazitschek R, Huwe A, Furet P, Giannis A, Waldmann HJournal of the American Chemical SocietyTotal synthesis and biological evaluation of the nakijiquinones. J Am Chem Soc. 2001 Nov 28; 123(47):11586-93.J Am Chem Soc2001-11-28T00:00:002001Total synthesis and biological evaluation of the nakijiquinones.12370049Mazitschek R, Baumhof P, Giannis AMini reviews in medicinal chemistryPeptidomimetics and angiogenesis. Mini Rev Med Chem. 2002 Oct; 2(5):491-506.Mini Rev Med Chem2002-10-01T00:00:002002Peptidomimetics and angiogenesis.Authorship 981297728490812Harada T, Ohguchi H, Grondin Y, Kikuchi S, Sagawa M, Tai YT, Mazitschek R, Hideshima T, Anderson KCLeukemiaHDAC3 regulates DNMT1 expression in multiple myeloma: therapeutic implications. Leukemia. 2017 12; 31(12):2670-2677.Leukemia2017-05-11T00:00:002017HDAC3 regulates DNMT1 expression in multiple myeloma: therapeutic implications.19307367Rush MA, Baniecki ML, Mazitschek R, Cortese JF, Wiegand R, Clardy J, Wirth DFAntimicrobial agents and chemotherapyColorimetric high-throughput screen for detection of heme crystallization inhibitors. Antimicrob Agents Chemother. 2009 Jun; 53(6):2564-8.Antimicrob Agents Chemother2009-03-23T00:00:002009Colorimetric high-throughput screen for detection of heme crystallization inhibitors.12866072Stieber F, Grether U, Mazitschek R, Soric N, Giannis A, Waldmann HChemistry (Weinheim an der Bergstrasse, Germany)Multistep solid-phase synthesis of an antibiotic and receptor tyrosine kinase inhibitors using the traceless phenylhydrazide linker. Chemistry. 2003 Jul 21; 9(14):3282-91.Chemistry2003-07-21T00:00:002003Multistep solid-phase synthesis of an antibiotic and receptor tyrosine kinase inhibitors using the traceless phenylhydrazide linker.12404633Addicks E, Mazitschek R, Giannis AChembiochem : a European journal of chemical biologySynthesis and biological investigation of novel tricyclic benzodiazepinedione-based RGD analogues. Chembiochem. 2002 Nov 04; 3(11):1078-88.Chembiochem2002-11-04T00:00:002002Synthesis and biological investigation of novel tricyclic benzodiazepinedione-based RGD analogues.12825933Kissau L, Stahl P, Mazitschek R, Giannis A, Waldmann HJournal of medicinal chemistryDevelopment of natural product-derived receptor tyrosine kinase inhibitors based on conservation of protein domain fold. J Med Chem. 2003 Jul 03; 46(14):2917-31.J Med Chem2003-07-03T00:00:002003Development of natural product-derived receptor tyrosine kinase inhibitors based on conservation of protein domain fold.22262760Santo L, Hideshima T, Kung AL, Tseng JC, Tamang D, Yang M, Jarpe M, van Duzer JH, Mazitschek R, Ogier WC, Cirstea D, Rodig S, Eda H, Scullen T, Canavese M, Bradner J, Anderson KC, Jones SS, Raje NBloodPreclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. 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Bioorg Med Chem Lett. 2010 Jan 01; 20(1):228-31.Bioorg Med Chem Lett2009-10-31T00:00:002009Synthesis and antiplasmodial activity of novel 2,4-diaminopyrimidines.19914069Martyn DC, Cortese JF, Tyndall E, Dick J, Mazitschek R, Munoz B, Clardy JBioorganic & medicinal chemistry lettersAntiplasmodial activity of piperazine sulfonamides. Bioorg Med Chem Lett. 2010 Jan 01; 20(1):218-21.Bioorg Med Chem Lett2009-10-31T00:00:002009Antiplasmodial activity of piperazine sulfonamides.22195562Dong CK, Urgaonkar S, Cortese JF, Gamo FJ, Garcia-Bustos JF, Lafuente MJ, Patel V, Ross L, Coleman BI, Derbyshire ER, Clish CB, Serrano AE, Cromwell M, Barker RH, Dvorin JD, Duraisingh MT, Wirth DF, Clardy J, Mazitschek RChemistry & biologyIdentification and validation of tetracyclic benzothiazepines as Plasmodium falciparum cytochrome bc1 inhibitors. Chem Biol. 2011 Dec 23; 18(12):1602-10.Chem Biol2011-12-23T00:00:002011Identification and validation of tetracyclic benzothiazepines as Plasmodium falciparum cytochrome bc1 inhibitors.Authorship 1002703228770556Srinivasulu V, Mazitschek R, Kariem NM, Reddy A, Rabeh WM, Li L, O'Connor MJ, Al-Tel THChemistry (Weinheim an der Bergstrasse, Germany)Modular Bi-Directional One-Pot Strategies for the Diastereoselective Synthesis of Structurally Diverse Collections of Constrained ß-Carboline-Benzoxazepines. Chemistry. 2017 Oct 12; 23(57):14182-14192.Chemistry2017-09-07T00:00:002017Modular Bi-Directional One-Pot Strategies for the Diastereoselective Synthesis of Structurally Diverse Collections of Constrained ß-Carboline-Benzoxazepines.19424149Guan JS, Haggarty SJ, Giacometti E, Dannenberg JH, Joseph N, Gao J, Nieland TJ, Zhou Y, Wang X, Mazitschek R, Bradner JE, DePinho RA, Jaenisch R, Tsai LHNatureHDAC2 negatively regulates memory formation and synaptic plasticity. Nature. 2009 May 07; 459(7243):55-60.Nature2009-05-07T00:00:002009HDAC2 negatively regulates memory formation and synaptic plasticity.20306505Devaraj NK, Hilderbrand S, Upadhyay R, Mazitschek R, Weissleder RAngewandte Chemie (International ed. in English)Bioorthogonal turn-on probes for imaging small molecules inside living cells. Angew Chem Int Ed Engl. 2010 Apr 06; 49(16):2869-72.Angew Chem Int Ed Engl2010-03-19T00:00:002010Bioorthogonal turn-on probes for imaging small molecules inside living cells.21974968Kamberov YG, Kim J, Mazitschek R, Kuo WP, Whitman MBMC research notesMicroarray profiling reveals the integrated stress response is activated by halofuginone in mammary epithelial cells. BMC Res Notes. 2011 Oct 05; 4:381.BMC Res Notes2011-10-05T00:00:002011Microarray profiling reveals the integrated stress response is activated by halofuginone in mammary epithelial cells.15273654Unsoeld AS, Junker B, Mazitschek R, Martin G, Hansen LL, Giannis A, Agostini HTMolecular visionLocal injection of receptor tyrosine kinase inhibitor MAE 87 reduces retinal neovascularization in mice. Mol Vis. 2004 Jul 15; 10:468-75.Mol Vis2004-07-15T00:00:002004Local injection of receptor tyrosine kinase inhibitor MAE 87 reduces retinal neovascularization in mice.17389687Tran AD, Marmo TP, Salam AA, Che S, Finkelstein E, Kabarriti R, Xenias HS, Mazitschek R, Hubbert C, Kawaguchi Y, Sheetz MP, Yao TP, Bulinski JCJournal of cell scienceHDAC6 deacetylation of tubulin modulates dynamics of cellular adhesions. J Cell Sci. 2007 Apr 15; 120(Pt 8):1469-79.J Cell Sci2007-03-27T00:00:002007HDAC6 deacetylation of tubulin modulates dynamics of cellular adhesions.22327401Keller TL, Zocco D, Sundrud MS, Hendrick M, Edenius M, Yum J, Kim YJ, Lee HK, Cortese JF, Wirth DF, Dignam JD, Rao A, Yeo CY, Mazitschek R, Whitman MNature chemical biologyHalofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase. Nat Chem Biol. 2012 Feb 12; 8(3):311-7.Nat Chem Biol2012-02-12T00:00:002012Halofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase.Authorship 1014095828712747She A, Kurtser I, Reis SA, Hennig K, Lai J, Lang A, Zhao WN, Mazitschek R, Dickerson BC, Herz J, Haggarty SJCell chemical biologySelectivity and Kinetic Requirements of HDAC Inhibitors as Progranulin Enhancers for Treating Frontotemporal Dementia. Cell Chem Biol. 2017 Jul 20; 24(7):892-906.e5.Cell Chem Biol2017-07-14T00:00:002017Selectivity and Kinetic Requirements of HDAC Inhibitors as Progranulin Enhancers for Treating Frontotemporal Dementia.20472442Estiu G, West N, Mazitschek R, Greenberg E, Bradner JE, Wiest OBioorganic & medicinal chemistryOn the inhibition of histone deacetylase 8. 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J Med Chem. 2008 May 22; 51(10):2898-906.J Med Chem2008-04-16T00:00:002008Structural origin of selectivity in class II-selective histone deacetylase inhibitors.19081376Kim D, Frank CL, Dobbin MM, Tsunemoto RK, Tu W, Peng PL, Guan JS, Lee BH, Moy LY, Giusti P, Broodie N, Mazitschek R, Delalle I, Haggarty SJ, Neve RL, Lu Y, Tsai LHNeuronDeregulation of HDAC1 by p25/Cdk5 in neurotoxicity. Neuron. 2008 Dec 10; 60(5):803-17.Neuron2008-12-10T00:00:002008Deregulation of HDAC1 by p25/Cdk5 in neurotoxicity.21444725de Zoeten EF, Wang L, Butler K, Beier UH, Akimova T, Sai H, Bradner JE, Mazitschek R, Kozikowski AP, Matthias P, Hancock WWMolecular and cellular biologyHistone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells. Mol Cell Biol. 2011 May; 31(10):2066-78.Mol Cell Biol2011-03-28T00:00:002011Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells.22027590Shi P, Scott MA, Ghosh B, Wan D, Wissner-Gross Z, Mazitschek R, Haggarty SJ, Yanik MFNature communicationsSynapse microarray identification of small molecules that enhance synaptogenesis. Nat Commun. 2011 Oct 25; 2:510.Nat Commun2011-10-25T00:00:002011Synapse microarray identification of small molecules that enhance synaptogenesis.20718474Urgaonkar S, Cortese JF, Barker RH, Cromwell M, Serrano AE, Wirth DF, Clardy J, Mazitschek ROrganic lettersA concise silylamine approach to 2-amino-3-hydroxy-indoles with potent in vivo antimalaria activity. Org Lett. 2010 Sep 17; 12(18):3998-4001.Org Lett2010-09-17T00:00:002010A concise silylamine approach to 2-amino-3-hydroxy-indoles with potent in vivo antimalaria activity.23084749Mak AB, Nixon AM, Kittanakom S, Stewart JM, Chen GI, Curak J, Gingras AC, Mazitschek R, Neel BG, Stagljar I, Moffat JCell reportsRegulation of CD133 by HDAC6 promotes ß-catenin signaling to suppress cancer cell differentiation. Cell Rep. 2012 Oct 25; 2(4):951-63.Cell Rep2012-10-19T00:00:002012Regulation of CD133 by HDAC6 promotes ß-catenin signaling to suppress cancer cell differentiation.Authorship 105930411592218Baumhof P, Mazitschek R, Giannis AAngewandte Chemie (International ed. in English)A Mild and Effective Method for the Transesterification of Carboxylic Acid Esters P.B. and R.M. are grateful to the Land Baden-Württemberg for a scholarship from the Landesgraduiertenförderung. Angew Chem Int Ed Engl. 2001 Oct 01; 40(19):3672-3674.Angew Chem Int Ed Engl2001-10-01T00:00:002001A Mild and Effective Method for the Transesterification of Carboxylic Acid Esters P.B. and R.M. are grateful to the Land Baden-Württemberg for a scholarship from the Landesgraduiertenförderung.