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Last Name

profileRalph Mazitschek, Ph.D.

TitleAssistant Professor of Radiology
InstitutionMassachusetts General Hospital
AddressMassachusetts General Hospital
Simches Research Building - 5.212
185 Cambridge St
Boston MA 02114
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Other Positions
TitleAssistant Professor in the Department of Immunology and Infectious Diseases
InstitutionHarvard T.H. Chan School of Public Health
DepartmentImmunology and Infectious Diseases

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Collapse research activities and funding
The research activities and funding listed below are automatically derived from NIH ExPORTER and other sources, which might result in incorrect or missing items. Faculty can login to make corrections and additions.
R01NS088209     (MAZITSCHEK, RALPH)Jun 1, 2014 - Apr 30, 2019
Chemical Optoepigenetic Regulation of Chromatin-Mediated Neuroplasticity
Role: Co-Principal Investigator

P50CA086355     (WEISSLEDER, RALPH)Aug 9, 2000 - Jun 30, 2016
Center for Molecular Imaging Research at MGH/HMS
Role: Co-Principal Investigator

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Collapse selected publications
Publications listed below are automatically derived from MEDLINE/PubMed and other sources, which might result in incorrect or missing publications. Faculty can login to make corrections and additions.
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  1. Srinivasulu V, Mazitschek R, Kariem NM, Reddy A, Rabeh WM, Li L, O'Connor MJ, Al-Tel TH. Modular Bi-Directional One-Pot Strategies for the Diastereoselective Synthesis of Structurally Diverse Collections of Constrained ß-Carboline-Benzoxazepines. Chemistry. 2017 Aug 02. PMID: 28770556.
    View in: PubMed
  2. She A, Kurtser I, Reis SA, Hennig K, Lai J, Lang A, Zhao WN, Mazitschek R, Dickerson BC, Herz J, Haggarty SJ. Selectivity and Kinetic Requirements of HDAC Inhibitors as Progranulin Enhancers for Treating Frontotemporal Dementia. Cell Chem Biol. 2017 Jul 20; 24(7):892-906.e5. PMID: 28712747.
    View in: PubMed
  3. Iaconelli J, Lalonde J, Watmuff B, Liu B, Mazitschek R, Haggarty SJ, Karmacharya R. Lysine Deacetylation by HDAC6 Regulates the Kinase Activity of AKT in Human Neural Progenitor Cells. ACS Chem Biol. 2017 Aug 18; 12(8):2139-2148. PMID: 28628306.
    View in: PubMed
  4. Hideshima T, Mazitschek R, Qi J, Mimura N, Tseng JC, Kung AL, Bradner JE, Anderson KC. HDAC6 inhibitor WT161 downregulates growth factor receptors in breast cancer. Oncotarget. 2017 Jul 05. PMID: 28708596.
    View in: PubMed
  5. Vinegoni C, Fumene Feruglio P, Brand C, Lee S, Nibbs AE, Stapleton S, Shah S, Gryczynski I, Reiner T, Mazitschek R, Weissleder R. Measurement of drug-target engagement in live cells by two-photon fluorescence anisotropy imaging. Nat Protoc. 2017 Jul; 12(7):1472-1497. PMID: 28686582.
    View in: PubMed
  6. Krukowski K, Ma J, Golonzhka O, Laumet GO, Gutti T, van Duzer JH, Mazitschek R, Jarpe MB, Heijnen CJ, Kavelaars A. HDAC6 inhibition effectively reverses chemotherapy-induced peripheral neuropathy. Pain. 2017 Jun; 158(6):1126-1137. PMID: 28267067.
    View in: PubMed
  7. Harada T, Ohguchi H, Grondin Y, Kikuchi S, Sagawa M, Tai YT, Mazitschek R, Hideshima T, Anderson KC. HDAC3 regulates DNMT1 expression in multiple myeloma: therapeutic implications. Leukemia. 2017 May 11. PMID: 28490812.
    View in: PubMed
  8. Vieson MD, Gojmerac AM, Khan D, Dai R, van Duzer JH, Mazitschek R, Caudell DL, Liao X, Luo XM, Reilly CM. Treatment with a selective histone deacetylase 6 inhibitor decreases lupus nephritis in NZB/W mice. Histol Histopathol. 2017 Feb 28; 11885. PMID: 28245046.
    View in: PubMed
  9. Srinivasulu V, Reddy A, Mazitschek R, Lukens AK, Wirth DF, Li L, Naumov P, O'Connor MJ, Al-Tel TH. 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. PMID: 27997727.
    View in: PubMed
  10. Huang P, Almeciga-Pinto I, Jarpe M, van Duzer JH, Mazitschek R, Yang M, Jones SS, Quayle SN. Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models. Oncotarget. 2017 Jan 10; 8(2):2694-2707. PMID: 27926524.
    View in: PubMed
  11. Hideshima 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 JE. Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma. Proc Natl Acad Sci U S A. 2016 Nov 15; 113(46):13162-13167. PMID: 27799547.
    View in: PubMed
  12. Carrasco 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 R. Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites. ChemMedChem. 2016 Oct 06; 11(19):2194-2204. PMID: 27538856.
    View in: PubMed
  13. Reis 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 R. Light-controlled modulation of gene expression by chemical optoepigenetic probes. Nat Chem Biol. 2016 May; 12(5):317-23. PMID: 26974814; PMCID: PMC4836974.
  14. Ghosh B, Zhao WN, Reis SA, Patnaik D, Fass DM, Tsai LH, Mazitschek R, Haggarty SJ. Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation. Bioorg Med Chem Lett. 2016 Feb 15; 26(4):1265-1271. PMID: 26804233; PMCID: PMC4753070 [Available on 02/15/17].
  15. Santos SA, Lukens AK, Coelho L, Nogueira F, Wirth DF, Mazitschek R, Moreira R, Paulo A. Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype. Eur J Med Chem. 2015 Sep 18; 102:320-33. PMID: 26295174.
    View in: PubMed
  16. Vinegoni C, Dubach JM, Thurber GM, Miller MA, Mazitschek R, Weissleder R. Advances in measuring single-cell pharmacology in vivo. Drug Discov Today. 2015 Sep; 20(9):1087-92. PMID: 26024776; PMCID: PMC4567932 [Available on 09/01/16].
  17. Liu J, Lee J, Salazar Hernandez MA, Mazitschek R, Ozcan U. Treatment of obesity with celastrol. Cell. 2015 May 21; 161(5):999-1011. PMID: 26000480; PMCID: PMC4768733.
  18. Herman 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 R. The 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. PMID: 25995223; PMCID: PMC4675670.
  19. Guan Y, Meurer M, Raghavan S, Rebane A, Lindquist JR, Santos S, Kats I, Davidson MW, Mazitschek R, Hughes TE, Drobizhev M, Knop M, Shah JV. Live-cell multiphoton fluorescence correlation spectroscopy with an improved large Stokes shift fluorescent protein. Mol Biol Cell. 2015 Jun 01; 26(11):2054-66. PMID: 25877871; PMCID: PMC4472016.
  20. Ecker 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 T. Targeting class I histone deacetylase 2 in MYC amplified group 3 medulloblastoma. Acta Neuropathol Commun. 2015 Apr 03; 3:22. PMID: 25853389; PMCID: PMC4382927.
  21. Li Y, Zhao T, Liu B, Halaweish I, Mazitschek R, Duan X, Alam HB. Inhibition of histone deacetylase 6 improves long-term survival in a lethal septic model. J Trauma Acute Care Surg. 2015 Feb; 78(2):378-85. PMID: 25757125; PMCID: PMC4357277.
  22. Iaconelli J, Huang JH, Berkovitch SS, Chattopadhyay S, Mazitschek R, Schreiber SL, Haggarty SJ, Karmacharya R. HDAC6 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. PMID: 25546293; PMCID: PMC4372110.
  23. Zhao Y, Zhou P, Liu B, Bambakidis T, Mazitschek R, Alam HB, Li Y. Protective effect of suberoylanilide hydroxamic acid against lipopolysaccharide-induced liver damage in rodents. J Surg Res. 2015 Apr; 194(2):544-50. PMID: 25479907; PMCID: PMC4361238.
  24. Chan CT, Qi J, Smith W, Paranol R, Mazitschek R, West N, Reeves R, Chiosis G, Schreiber SL, Bradner JE, Paulmurugan R, Gambhir SS. Syntheses 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. PMID: 25320008; PMCID: PMC4315624.
  25. Derbyshire 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 J. Chemical interrogation of the malaria kinome. Chembiochem. 2014 Sep 05; 15(13):1920-30. PMID: 25111632; PMCID: PMC4237307.
  26. Dubach JM, Vinegoni C, Mazitschek R, Fumene Feruglio P, Cameron LA, Weissleder R. In vivo imaging of specific drug-target binding at subcellular resolution. Nat Commun. 2014 May 28; 5:3946. PMID: 24867710; PMCID: PMC4362617.
  27. Courtis AM, Santos SA, Guan Y, Hendricks JA, Ghosh B, Szantai-Kis DM, Reis SA, Shah JV, Mazitschek R. Monoalkoxy BODIPYs--a fluorophore class for bioimaging. Bioconjug Chem. 2014 Jun 18; 25(6):1043-51. PMID: 24797834; PMCID: PMC4215867.
  28. McLellan CA, Whitesell L, King OD, Lancaster AK, Mazitschek R, Lindquist S. Correction to inhibiting GPI anchor biosynthesis in fungi stresses the endoplasmic reticulum and enhances immunogenicity. ACS Chem Biol. 2014 Apr 18; 9(4):1061. PMID: 24624974.
    View in: PubMed
  29. Keliher EJ, Klubnick JA, Reiner T, Mazitschek R, Weissleder R. Efficient acid-catalyzed (18) F/(19) F fluoride exchange of BODIPY dyes. ChemMedChem. 2014 Jul; 9(7):1368-73. PMID: 24596307; PMCID: PMC4145401.
  30. Zhao T, Li Y, Liu B, Halaweish I, Mazitschek R, Alam HB. Selective 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. PMID: 24613069; PMCID: PMC4267528.
  31. Herman JD, Rice DP, Ribacke U, Silterra J, Deik AA, Moss EL, Broadbent KM, Neafsey DE, Desai MM, Clish CB, Mazitschek R, Wirth DF. A genomic and evolutionary approach reveals non-genetic drug resistance in malaria. Genome Biol. 2014; 15(11):511. PMID: 25395010; PMCID: PMC4272547.
  32. Hideshima T, Mazitschek R, Santo L, Mimura N, Gorgun G, Richardson PG, Raje N, Anderson KC. Induction of differential apoptotic pathways in multiple myeloma cells by class-selective histone deacetylase inhibitors. Leukemia. 2014 Feb; 28(2):457-60. PMID: 24150220; PMCID: PMC4405100.
  33. Jochems J, Boulden J, Lee BG, Blendy JA, Jarpe M, Mazitschek R, Van Duzer JH, Jones S, Berton O. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology. 2014 Jan; 39(2):389-400. PMID: 23954848; PMCID: PMC3870780.
  34. Minami 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 KC. Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. Leukemia. 2014 Mar; 28(3):680-9. PMID: 23913134; PMCID: PMC4165599.
  35. Ageta-Ishihara N, Miyata T, Ohshima C, Watanabe M, Sato Y, Hamamura Y, Higashiyama T, Mazitschek R, Bito H, Kinoshita M. Septins promote dendrite and axon development by negatively regulating microtubule stability via HDAC6-mediated deacetylation. Nat Commun. 2013; 4:2532. PMID: 24113571; PMCID: PMC3826633.
  36. Mak AB, Nixon AM, Kittanakom S, Stewart JM, Chen GI, Curak J, Gingras AC, Mazitschek R, Neel BG, Stagljar I, Moffat J. Regulation of CD133 by HDAC6 promotes ß-catenin signaling to suppress cancer cell differentiation. Cell Rep. 2012 Oct 25; 2(4):951-63. PMID: 23084749; PMCID: PMC3590846.
  37. Fass 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 SJ. Crebinostat: a novel cognitive enhancer that inhibits histone deacetylase activity and modulates chromatin-mediated neuroplasticity. Neuropharmacology. 2013 Jan; 64:81-96. PMID: 22771460; PMCID: PMC3447535.
  38. McLellan CA, Whitesell L, King OD, Lancaster AK, Mazitschek R, Lindquist S. Inhibiting GPI anchor biosynthesis in fungi stresses the endoplasmic reticulum and enhances immunogenicity. ACS Chem Biol. 2012 Sep 21; 7(9):1520-8. PMID: 22724584.
    View in: PubMed
  39. Hendricks JA, Keliher EJ, Wan D, Hilderbrand SA, Weissleder R, Mazitschek R. 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. PMID: 22473535; PMCID: PMC3343182.
  40. Derbyshire ER, Mazitschek R, Clardy J. Characterization of Plasmodium liver stage inhibition by halofuginone. ChemMedChem. 2012 May; 7(5):844-9. PMID: 22438279; PMCID: PMC3359061.
  41. Keller 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 M. Halofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase. Nat Chem Biol. 2012 Feb 12; 8(3):311-7. PMID: 22327401; PMCID: PMC3281520.
  42. Santo 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 N. Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. Blood. 2012 Mar 15; 119(11):2579-89. PMID: 22262760; PMCID: PMC3337713.
  43. Dong 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 R. Identification and validation of tetracyclic benzothiazepines as Plasmodium falciparum cytochrome bc1 inhibitors. Chem Biol. 2011 Dec 23; 18(12):1602-10. PMID: 22195562; PMCID: PMC3474356.
  44. Shi P, Scott MA, Ghosh B, Wan D, Wissner-Gross Z, Mazitschek R, Haggarty SJ, Yanik MF. Synapse microarray identification of small molecules that enhance synaptogenesis. Nat Commun. 2011 Oct 25; 2:510. PMID: 22027590; PMCID: PMC3544154.
  45. Kamberov YG, Kim J, Mazitschek R, Kuo WP, Whitman M. Microarray profiling reveals the integrated stress response is activated by halofuginone in mammary epithelial cells. BMC Res Notes. 2011 Oct 05; 4:381. PMID: 21974968; PMCID: PMC3197508.
  46. Hendricks JA, Keliher EJ, Marinelli B, Reiner T, Weissleder R, Mazitschek R. In vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA). J Med Chem. 2011 Aug 11; 54(15):5576-82. PMID: 21721525; PMCID: PMC3150598.
  47. Aldana-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 KM. Tubacin suppresses proliferation and induces apoptosis of acute lymphoblastic leukemia cells. Leuk Lymphoma. 2011 Aug; 52(8):1544-55. PMID: 21699378; PMCID: PMC4113006.
  48. Santo 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 NS. The 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. PMID: 28023028.
    View in: PubMed
  49. de Zoeten EF, Wang L, Butler K, Beier UH, Akimova T, Sai H, Bradner JE, Mazitschek R, Kozikowski AP, Matthias P, Hancock WW. Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells. Mol Cell Biol. 2011 May; 31(10):2066-78. PMID: 21444725; PMCID: PMC3133361.
  50. Barker RH, Urgaonkar S, Mazitschek R, Celatka C, Skerlj R, Cortese JF, Tyndall E, Liu H, Cromwell M, Sidhu AB, Guerrero-Bravo JE, Crespo-Llado KN, Serrano AE, Lin JW, Janse CJ, Khan SM, Duraisingh M, Coleman BI, Angulo-Barturen I, Jiménez-Díaz MB, Magán N, Gomez V, Ferrer S, Martínez MS, Wittlin S, Papastogiannidis P, O'Shea T, Klinger JD, Bree M, Lee E, Levine M, Wiegand RC, Munoz B, Wirth DF, Clardy J, Bathurst I, Sybertz E. Aminoindoles, a novel scaffold with potent activity against Plasmodium falciparum. Antimicrob Agents Chemother. 2011 Jun; 55(6):2612-22. PMID: 21422215; PMCID: PMC3101419.
  51. Fass DM, Shah R, Ghosh B, Hennig K, Norton S, Zhao WN, Reis SA, Klein PS, Mazitschek R, Maglathlin RL, Lewis TA, Haggarty SJ. Effect 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. PMID: 21874153.
    View in: PubMed
  52. Urgaonkar S, Cortese JF, Barker RH, Cromwell M, Serrano AE, Wirth DF, Clardy J, Mazitschek R. A concise silylamine approach to 2-amino-3-hydroxy-indoles with potent in vivo antimalaria activity. Org Lett. 2010 Sep 17; 12(18):3998-4001. PMID: 20718474.
    View in: PubMed
  53. Bradner 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 BL. Chemical 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. PMID: 20616024; PMCID: PMC2906581.
  54. Estiu G, West N, Mazitschek R, Greenberg E, Bradner JE, Wiest O. On the inhibition of histone deacetylase 8. Bioorg Med Chem. 2010 Jun 01; 18(11):4103-10. PMID: 20472442; PMCID: PMC3245874.
  55. Devaraj NK, Hilderbrand S, Upadhyay R, Mazitschek R, Weissleder R. Bioorthogonal turn-on probes for imaging small molecules inside living cells. Angew Chem Int Ed Engl. 2010 Apr 06; 49(16):2869-72. PMID: 20306505; PMCID: PMC3433403.
  56. Bradner JE, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T, Mazitschek R. Chemical phylogenetics of histone deacetylases. Nat Chem Biol. 2010 Mar; 6(3):238-243. PMID: 20139990.
    View in: PubMed
  57. Ueno T, Kaneko K, Katano H, Sato Y, Mazitschek R, Tanaka K, Hattori S, Irie S, Sata T, Ogawa-Goto K. Expansion 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. PMID: 19932094.
    View in: PubMed
  58. Martyn DC, Nijjar A, Celatka CA, Mazitschek R, Cortese JF, Tyndall E, Liu H, Fitzgerald MM, O'Shea TJ, Danthi S, Clardy J. Synthesis and antiplasmodial activity of novel 2,4-diaminopyrimidines. Bioorg Med Chem Lett. 2010 Jan 01; 20(1):228-31. PMID: 19914064.
    View in: PubMed
  59. Martyn DC, Cortese JF, Tyndall E, Dick J, Mazitschek R, Munoz B, Clardy J. Antiplasmodial activity of piperazine sulfonamides. Bioorg Med Chem Lett. 2010 Jan 01; 20(1):218-21. PMID: 19914069.
    View in: PubMed
  60. Zilberman Y, Ballestrem C, Carramusa L, Mazitschek R, Khochbin S, Bershadsky A. Regulation of microtubule dynamics by inhibition of the tubulin deacetylase HDAC6. J Cell Sci. 2009 Oct 01; 122(Pt 19):3531-41. PMID: 19737819.
    View in: PubMed
  61. Moy TI, Conery AL, Larkins-Ford J, Wu G, Mazitschek R, Casadei G, Lewis K, Carpenter AE, Ausubel FM. High-throughput screen for novel antimicrobials using a whole animal infection model. ACS Chem Biol. 2009 Jul 17; 4(7):527-33. PMID: 19572548; PMCID: PMC2745594.
  62. Sundrud 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 A. Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response. Science. 2009 Jun 05; 324(5932):1334-8. PMID: 19498172; PMCID: PMC2803727.
  63. Guan 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 LH. HDAC2 negatively regulates memory formation and synaptic plasticity. Nature. 2009 May 07; 459(7243):55-60. PMID: 19424149; PMCID: PMC3498958.
  64. Patel V, Mazitschek R, Coleman B, Nguyen C, Urgaonkar S, Cortese J, Barker RH, Greenberg E, Tang W, Bradner JE, Schreiber SL, Duraisingh MT, Wirth DF, Clardy J. Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum. J Med Chem. 2009 Apr 23; 52(8):2185-7. PMID: 19317450; PMCID: PMC2669731.
  65. Kawada J, Zou P, Mazitschek R, Bradner JE, Cohen JI. Tubacin 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):17102-9. PMID: 19386607; PMCID: PMC2719348.
  66. Rush MA, Baniecki ML, Mazitschek R, Cortese JF, Wiegand R, Clardy J, Wirth DF. Colorimetric high-throughput screen for detection of heme crystallization inhibitors. Antimicrob Agents Chemother. 2009 Jun; 53(6):2564-8. PMID: 19307367; PMCID: PMC2687197.
  67. Kim 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 LH. Deregulation of HDAC1 by p25/Cdk5 in neurotoxicity. Neuron. 2008 Dec 10; 60(5):803-17. PMID: 19081376; PMCID: PMC2912147.
  68. Bazzaro M, Lin Z, Santillan A, Lee MK, Wang MC, Chan KC, Bristow RE, Mazitschek R, Bradner J, Roden RB. Ubiquitin 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. PMID: 19010849; PMCID: PMC2744414.
  69. Hahn CK, Ross KN, Warrington IM, Mazitschek R, Kanegai CM, Wright RD, Kung AL, Golub TR, Stegmaier K. Expression-based screening identifies the combination of histone deacetylase inhibitors and retinoids for neuroblastoma differentiation. Proc Natl Acad Sci U S A. 2008 Jul 15; 105(28):9751-6. PMID: 18607002; PMCID: PMC2474517.
  70. Groen AC, Needleman D, Brangwynne C, Gradinaru C, Fowler B, Mazitschek R, Mitchison TJ. A 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. PMID: 18559893; PMCID: PMC2902979.
  71. Estiu G, Greenberg E, Harrison CB, Kwiatkowski NP, Mazitschek R, Bradner JE, Wiest O. Structural origin of selectivity in class II-selective histone deacetylase inhibitors. J Med Chem. 2008 May 22; 51(10):2898-906. PMID: 18412327.
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  72. Mazitschek R, Patel V, Wirth DF, Clardy J. Development of a fluorescence polarization based assay for histone deacetylase ligand discovery. Bioorg Med Chem Lett. 2008 May 01; 18(9):2809-12. PMID: 18430569; PMCID: PMC2408937.
  73. Schuetz 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 CH. Human 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. PMID: 18285338; PMCID: PMC2431080.
  74. Duan Z, Bradner J, Greenberg E, Mazitschek R, Foster R, Mahoney J, Seiden MV. 8-benzyl-4-oxo-8-azabicyclo[3.2.1]oct-2-ene-6,7-dicarboxylic acid (SD-1008), a novel janus kinase 2 inhibitor, increases chemotherapy sensitivity in human ovarian cancer cells. Mol Pharmacol. 2007 Nov; 72(5):1137-45. PMID: 17675586.
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  75. Tran AD, Marmo TP, Salam AA, Che S, Finkelstein E, Kabarriti R, Xenias HS, Mazitschek R, Hubbert C, Kawaguchi Y, Sheetz MP, Yao TP, Bulinski JC. HDAC6 deacetylation of tubulin modulates dynamics of cellular adhesions. J Cell Sci. 2007 Apr 15; 120(Pt 8):1469-79. PMID: 17389687.
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  76. Mosley AJ, Meekings KN, McCarthy C, Shepherd D, Cerundolo V, Mazitschek R, Tanaka Y, Taylor GP, Bangham CR. Histone deacetylase inhibitors increase virus gene expression but decrease CD8+ cell antiviral function in HTLV-1 infection. Blood. 2006 Dec 01; 108(12):3801-7. PMID: 16912225.
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  77. Cabrero JR, Serrador JM, Barreiro O, Mittelbrunn M, Naranjo-Suárez S, Martín-Cófreces N, Vicente-Manzanares M, Mazitschek R, Bradner JE, Avila J, Valenzuela-Fernández A, Sánchez-Madrid F. Lymphocyte chemotaxis is regulated by histone deacetylase 6, independently of its deacetylase activity. Mol Biol Cell. 2006 Aug; 17(8):3435-45. PMID: 16738306; PMCID: PMC1525231.
  78. Bradner 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 AN. A robust small-molecule microarray platform for screening cell lysates. Chem Biol. 2006 May; 13(5):493-504. PMID: 16720270.
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  79. Mazitschek R, Huwe A, Giannis A. Synthesis and biological evaluation of novel fumagillin and ovalicin analogues. Org Biomol Chem. 2005 Jun 07; 3(11):2150-4. PMID: 15917904.
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  80. Kirkin V, Thiele W, Baumann P, Mazitschek R, Rohde K, Fellbrich G, Weich H, Waltenberger J, Giannis A, Sleeman JP. MAZ51, 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. PMID: 15386354.
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  81. Mazitschek R, Giannis A. Inhibitors of angiogenesis and cancer-related receptor tyrosine kinases. Curr Opin Chem Biol. 2004 Aug; 8(4):432-41. PMID: 15288254.
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  82. Unsoeld AS, Junker B, Mazitschek R, Martin G, Hansen LL, Giannis A, Agostini HT. Local injection of receptor tyrosine kinase inhibitor MAE 87 reduces retinal neovascularization in mice. Mol Vis. 2004 Jul 15; 10:468-75. PMID: 15273654.
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  83. Rosenbaum C, Baumhof P, Mazitschek R, Müller O, Giannis A, Waldmann H. 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. PMID: 14695616.
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  84. Stieber F, Grether U, Mazitschek R, Soric N, Giannis A, Waldmann H. 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. PMID: 12866072.
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  85. Kissau L, Stahl P, Mazitschek R, Giannis A, Waldmann H. Development 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. PMID: 12825933.
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  86. Huwe A, Mazitschek R, Giannis A. Small molecules as inhibitors of cyclin-dependent kinases. Angew Chem Int Ed Engl. 2003 May 16; 42(19):2122-38. PMID: 12761741.
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  87. Stieber F, Mazitschek R, Soric N, Giannis A, Waldmann H. 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. PMID: 12481350.
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  88. Mazitschek R, Mülbaier M, Giannis A. IBX-mediated oxidation of primary alcohols and aldehydes to form carboxylic acids. Angew Chem Int Ed Engl. 2002 Nov 04; 41(21):4059-61. PMID: 12412081.
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  89. Addicks E, Mazitschek R, Giannis A. Synthesis and biological investigation of novel tricyclic benzodiazepinedione-based RGD analogues. Chembiochem. 2002 Nov 04; 3(11):1078-88. PMID: 12404633.
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  90. Mazitschek R, Baumhof P, Giannis A. Peptidomimetics and angiogenesis. Mini Rev Med Chem. 2002 Oct; 2(5):491-506. PMID: 12370049.
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  91. Stahl P, Kissau L, Mazitschek R, Giannis A, Waldmann H. 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. PMID: 12491250.
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  92. Stahl P, Kissau L, Mazitschek R, Huwe A, Furet P, Giannis A, Waldmann H. Total synthesis and biological evaluation of the nakijiquinones. J Am Chem Soc. 2001 Nov 28; 123(47):11586-93. PMID: 11716712.
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  93. Kirkin V, Mazitschek R, Krishnan J, Steffen A, Waltenberger J, Pepper MS, Giannis A, Sleeman JP. Characterization 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. PMID: 11683876.
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  94. Baumhof P, Mazitschek R, Giannis A. 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. PMID: 11592218.
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  95. Wernert N, Stanjek A, Kiriakidis S, Hügel A, Jha HC, Mazitschek R, Giannis A. 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. PMID: 10556911.
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