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Last Name
Institution

Ralph Mazitschek, Ph.D.

TitleAssistant Professor of Radiology
InstitutionMassachusetts General Hospital
DepartmentRadiology
AddressMassachusetts General Hospital
Simches Research Building - 5.212
185 Cambridge St
Boston MA 02114
Phone617/643-6286
Other Positions
TitleAssistant Professor of Immunology and Infectious Diseases
InstitutionHarvard School of Public Health
DepartmentImmunology and Infectious Diseases


 Bibliographic 
 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. 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 Oct 11; 4:2532.
    View in: PubMed
  2. 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.
    View in: PubMed
  3. 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.
    View in: PubMed
  4. 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.
    View in: PubMed
  5. 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.
    View in: PubMed
  6. 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 7; 51(19):4603-6.
    View in: PubMed
  7. Derbyshire ER, Mazitschek R, Clardy J. Characterization of Plasmodium liver stage inhibition by halofuginone. ChemMedChem. 2012 May; 7(5):844-9.
    View in: PubMed
  8. 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 Mar; 8(3):311-7.
    View in: PubMed
  9. 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.
    View in: PubMed
  10. 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.
    View in: PubMed
  11. 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; 2:510.
    View in: PubMed
  12. 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; 4:381.
    View in: PubMed
  13. 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.
    View in: PubMed
  14. 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.
    View in: PubMed
  15. 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.
    View in: PubMed
  16. 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.
    View in: PubMed
  17. 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 8; 2(1):39-42.
    View in: PubMed
  18. 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.
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  19. 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.
    View in: PubMed
  20. Estiu G, West N, Mazitschek R, Greenberg E, Bradner JE, Wiest O. On the inhibition of histone deacetylase 8. Bioorg Med Chem. 2010 Jun 1; 18(11):4103-10.
    View in: PubMed
  21. 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 6; 49(16):2869-72.
    View in: PubMed
  22. 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.
    View in: PubMed
  23. 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 1; 316(3):329-40.
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  24. 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 1; 20(1):228-31.
    View in: PubMed
  25. 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 1; 20(1):218-21.
    View in: PubMed
  26. 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 1; 122(Pt 19):3531-41.
    View in: PubMed
  27. 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.
    View in: PubMed
  28. 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 5; 324(5932):1334-8.
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  29. 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 7; 459(7243):55-60.
    View in: PubMed
  30. 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.
    View in: PubMed
  31. 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.
    View in: PubMed
  32. 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.
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  33. 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.
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  34. 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.
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  35. 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.
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  36. 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.
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  37. 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.
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  38. 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 1; 18(9):2809-12.
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  39. 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.
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  40. 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.
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  41. 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.
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  42. 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 1; 108(12):3801-7.
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  43. 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.
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  44. 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.
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  45. Mazitschek R, Huwe A, Giannis A. Synthesis and biological evaluation of novel fumagillin and ovalicin analogues. Org Biomol Chem. 2005 Jun 7; 3(11):2150-4.
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  46. 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.
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  47. Mazitschek R, Giannis A. Inhibitors of angiogenesis and cancer-related receptor tyrosine kinases. Curr Opin Chem Biol. 2004 Aug; 8(4):432-41.
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  48. 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.
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  49. 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.
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  50. 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.
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  51. 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 3; 46(14):2917-31.
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  52. 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.
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  53. 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.
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  54. 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 4; 41(21):4059-61.
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  55. Addicks E, Mazitschek R, Giannis A. Synthesis and biological investigation of novel tricyclic benzodiazepinedione-based RGD analogues. Chembiochem. 2002 Nov 4; 3(11):1078-88.
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  56. Mazitschek R, Baumhof P, Giannis A. Peptidomimetics and angiogenesis. Mini Rev Med Chem. 2002 Oct; 2(5):491-506.
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  57. 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 2; 41(7):1174-8.
    View in: PubMed
  58. 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.
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  59. 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.
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  60. 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 1; 40(19):3672-3674.
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  61. 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 2; 38(21):3228-3231.
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