Mazitschek, Ralph, PhD

Assistant Professor

Phone: 617-643-6286
Email: rmazitschek@mgh.harvard.edu
Lab: Mazitschek, Ralph
Dr. Mazitschek is an Assistant Professor at Harvard Medical School and Co-Director of the Chemical Biology Platform at the Center for Systems Biology at Massachusetts General Hospital (MGH). Dr. Mazitschek is also a member of the Infectious Diseases Initiative at The Broad Institute of Harvard and MIT, associate Faculty at the Center for Human Genetic Research at MGH and Visiting Scientist at the Department of Immunology and Infectious Diseases at Harvard School of Public Health. Dr. Mazitschek graduated from the University of Leipzig in 2002 with a Ph.D. in Organic Chemistry. He continued hist research at the Institute of Chemistry and Cell Biology (ICCB) at Harvard Medical School first as postdoc and later as Institute Fellow, from which he joined the Chemical Biology Program at the newly founded Broad Institute of Harvard and MIT. In 2008 he joined the faculty of the Center for Systems Biology at the Massachusetts General Hospital to continue his independent research.

Publications

  • Yue 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 ES Rapid 'mix and read' assay for scalable detection of SARS-CoV-2 antibodies in patient plasma. medRxiv. 2020;:ePub - PMID: 32909004 - PMCID: PMC7480056 - DOI: 10.1101/2020.09.01.20184101

  • Liston SD, Whitesell L, McLellan CA, Mazitschek R, Petraitis V, Petraitiene R, Kavaliauskas P, Walsh TJ, Cowen LE Antifungal activity of gepinacin-scaffold GPI anchor biosynthesis inhibitors with improved metabolic stability. Antimicrob Agents Chemother. 2020;:ePub - PMID: 32661007 - DOI: 10.1128/AAC.00899-20

  • Badr 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 BA Obtusaquinone is a cysteine modifying compound that targets Keap1 for degradation. ACS Chem Biol. 2020;15(6):1445-1454 - PMID: 32338864 - DOI: 10.1021/acschembio.0c00104

  • Kim 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 TL Aminoacyl-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;117(16):8900-8911 - PMID: 32253314 - PMCID: PMC7183223 - DOI: 10.1073/pnas.1913788117

  • Ho 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 G Targeting histone deacetylase 3 (HDAC3) in the bone marrow microenvironment inhibits multiple myeloma proliferation by modulating exosomes and IL-6 trans-signaling. Leukemia. 2020;34(1):196-209 - PMID: 31142847 - PMCID: PMC6883144 - DOI: 10.1038/s41375-019-0493-x

  • Zhao WN, Hylton NK, Wang J, Chindavong PS, Alural B, Kurtser I, Subramanian A, Mazitschek R, Perlis RH, Haggarty SJ Activation 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;99:103386 - PMID: 31202891 - PMCID: PMC7001743 - DOI: 10.1016/j.mcn.2019.06.006

  • Choudhary A, Manna D, Maji B, Gangopadhyay SA, Cox KJ, Zhou Q, Law B, Mazitschek R A singular system with precise dosing and spatiotemporal control of CRISPR-Cas9. Angew Chem Int Ed Engl. 2019;58(19):6285-6289 - PMID: 30834641 - PMCID: PMC7067309 - DOI: 10.1002/anie.201900788

  • Fagbami L, Deik AA, Herman JD, Singh K, Santos SA, Bopp S, Lukens AK, Clish CB, Wirth DF, Mazitschek R The adaptive proline response in P. falciparum is independent of PfeIK1 and eIF2α signaling. ACS Infect Dis. 2019;5(4):515-520 - PMID: 30773881 - PMCID: PMC6747701 - DOI: 10.1021/acsinfecdis.8b00363

  • Zhao WN, Ghosh B, Tyler M, Lalonde J, Joseph NF, Kosaric N, Fass DM, Tsai LH, Mazitschek R, Haggarty SJ Class I Histone Deacetylase Inhibition by Tianeptinaline Modulates Neuroplasticity and Enhances Memory. ACS Chem Neurosci. 2018;9(9):2262-2273 - PMID: 29932631 - DOI: 10.1021/acschemneuro.8b00116

  • Vinegoni C, Feruglio PF, Gryczynski I, Mazitschek R, Weissleder R Fluorescence anisotropy imaging in drug discovery. Adv Drug Deliv Rev. 2018;151-152:262-288 - PMID: 29410158 - PMCID: PMC6072632 - DOI: 10.1016/j.addr.2018.01.019

  • 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;8(46):80109-80123 - PMID: 29113288 - PMCID: PMC5655183 - DOI: 10.18632/oncotarget.19019

  • Randino R, Gazzerro P, Mazitschek R, Rodriquez M Synthesis and biological evaluation of Santacruzamate-A based analogues. Bioorg Med Chem. 2017;25(24):6486-6491 - PMID: 29100734 - DOI: 10.1016/j.bmc.2017.10.026

  • Vunnam S, Mazitschek R, Kariem NM, Reddy A, Rabeh W, Li L, O'Connor MJ, Al-Tel TH Modular Bi-Directional One-Pot Strategies for the Diastereoselective Synthesis of Structurally Diverse Collections of Constrained β-Carboline-Benzoxazepines. Chemistry. 2017;23(57):14182-14192 - PMID: 28770556 - DOI: 10.1002/chem.201702495

  • 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;24(7):892-906.e5 - PMID: 28712747 - PMCID: PMC5695697 - DOI: 10.1016/j.chembiol.2017.06.010

  • 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;:ePub - PMID: 28708596

  • 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;12(7):1472-1497 - PMID: 28686582 - PMCID: PMC5928516 - DOI: 10.1038/nprot.2017.043

  • 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;12(8):2139-2148 - PMID: 28628306 - PMCID: PMC6747705 - DOI: 10.1021/acschembio.6b01014

  • 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;31(12):2670-2677 - PMID: 28490812 - PMCID: PMC5681897 - DOI: 10.1038/leu.2017.144

  • 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;158(6):1126-1137 - PMID: 28267067 - PMCID: PMC5435512 - DOI: 10.1097/j.pain.0000000000000893

  • 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;:11885 - PMID: 28245046 - DOI: 10.14670/HH-11-885

  • Vunnam S, Reddy A, Mazitschek R, Lukens AK, Wirth DF, Li L, Naumov P, O'Connor MJ, Al-Tel TH Intramolecular Diaza-Diels-Alder Protocol: A Novel Diastereoselective and Modular One-Step Synthesis of Constrained Polycyclic Frameworks. Chemistry. 2017;23(17):4137-4148 - PMID: 27997727 - DOI: 10.1002/chem.201605231

  • 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;8(2):2694-2707 - PMID: 27926524 - PMCID: PMC5356834 - DOI: 10.18632/oncotarget.13738

  • 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;113(46):13162-13167 - PMID: 27799547 - PMCID: PMC5135369 - DOI: 10.1073/pnas.1608067113

  • Carrasco MP, Machado M, Gonçalves L, Sharma M, Gut J, Lukens AK, Wirth DF, André V, Duarte MT, Guedes RC, J V A Dos Santos D, Rosenthal PJ, Mazitschek R, Prudêncio M, Moreira R Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites. ChemMedChem. 2016;11(19):2194-2204 - PMID: 27538856 - DOI: 10.1002/cmdc.201600327

  • 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;12(5):317-323 - PMID: 26974814 - PMCID: PMC4836974 - DOI: 10.1038/nchembio.2042

  • 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;26(4):1265-71 - PMID: 26804233 - PMCID: PMC4753070 - DOI: 10.1016/j.bmcl.2016.01.022

  • 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;102:320-333 - PMID: 26295174 - DOI: 10.1016/j.ejmech.2015.07.047

  • Vinegoni C, Dubach JM, Thurber GM, Miller MA, Mazitschek R, Weissleder R Advances in measuring single-cell pharmacokinetics and pharmacology in vivo. Drug Discov Today. 2015;20(9):1087-92 - PMID: 26024776 - PMCID: PMC4567932 - DOI: 10.1016/j.drudis.2015.05.011

  • 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;7(288):288ra77 - PMID: 25995223 - PMCID: PMC4675670 - DOI: 10.1126/scitranslmed.aaa3575

  • Liu J, Lee J, Salazar Hernandez MA, Mazitschek R, Ozcan U Treatment of obesity with celastrol. Cell. 2015;161(5):999-1011 - PMID: 26000480 - PMCID: PMC4768733 - DOI: 10.1016/j.cell.2015.05.011

  • 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 β-Catenin in Human iPSC-Derived Neuronal Cells. ACS Chem Biol. 2015;10(3):883-90 - PMID: 25546293 - PMCID: PMC4372110 - DOI: 10.1021/cb500838r

  • 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 Multi-Photon Fluorescence Correlation Spectroscopy with an Improved Large Stokes Shift Fluorescent Protein. Mol Biol Cell. 2015;26(11):2054-66 - PMID: 25877871 - PMCID: PMC4472016 - DOI: 10.1091/mbc.E14-10-1473

  • 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;3(1):22 - PMID: 25853389 - PMCID: PMC4382927 - DOI: 10.1186/s40478-015-0201-7

  • 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;78(2):378-85 - PMID: 25757125 - PMCID: PMC4357277 - DOI: 10.1097/TA.0000000000000510

  • 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;194(2):544-550 - PMID: 25479907 - PMCID: PMC4361238 - DOI: 10.1016/j.jss.2014.10.056

  • 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 - DOI: 10.1186/PREACCEPT-1067113631444973

  • Chan CT, Qi J, Smith W, Paranal 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 (HDAC) Inhibitors by Multimodality Molecular Imaging in Living Subjects. Cancer Res. 2014;74(24):7475-86 - PMID: 25320008 - PMCID: PMC4315624 - DOI: 10.1158/0008-5472.CAN-14-0197

  • 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;15(13):1920-30 - PMID: 25111632 - PMCID: PMC4237307 - DOI: 10.1002/cbic.201400025

  • 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;5:3946 - PMID: 24867710 - PMCID: PMC4362617 - DOI: 10.1038/ncomms4946

  • 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;25(6):1043-51 - PMID: 24797834 - PMCID: PMC4215867 - DOI: 10.1021/bc400575w

  • 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;190(2):647-54 - PMID: 24613069 - PMCID: PMC4267528 - DOI: 10.1016/j.jss.2014.01.056

  • 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;28(2):457-60 - PMID: 24150220 - PMCID: PMC4405100 - DOI: 10.1038/leu.2013.301

  • 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 (HDAC3) as a novel therapeutic target in multiple myeloma. Leukemia. 2014;28(3):680-9 - PMID: 23913134 - PMCID: PMC4165599 - DOI: 10.1038/leu.2013.231

  • 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 - DOI: 10.1038/ncomms3532

  • Fass DM, Reis SA, Ghosh B, Hennig KM, Joseph NF, Zhao WN, Nieland TJ, Guan JS, Groves 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;64(1):81-96 - PMID: 22771460 - PMCID: PMC3447535 - DOI: 10.1016/j.neuropharm.2012.06.043

  • 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. 2012;9(4):1061 - PMID: 22724584 - DOI: 10.1021/cb300235m

  • 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 β-Catenin Signaling to Suppress Cancer Cell Differentiation. Cell Rep. 2012;2(4):951-63 - PMID: 23084749 - PMCID: PMC3590846 - DOI: 10.1016/j.celrep.2012.09.016

  • 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;7(9):1520-8 - PMID: 22724584 - DOI: 10.1021/cb300235m

  • Hendricks JA, Keliher EJ, Wan D, Hilderbrand SA, Weissleder R, Mazitschek R Synthesis of [(18) F]BODIPY: Bifunctional Reporter for Hybrid Optical/Positron Emission Tomography Imaging. Angew Chem Int Ed Engl. 2012;51(19):4603-6 - PMID: 22473535 - PMCID: PMC3343182 - DOI: 10.1002/anie.201107957

  • Derbyshire ER, Mazitschek R, Clardy J Characterization of Plasmodium Liver Stage Inhibition by Halofuginone. ChemMedChem. 2012;7(5):844-9 - PMID: 22438279 - PMCID: PMC3359061 - DOI: 10.1002/cmdc.201200045

  • 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;8(3):311-7 - PMID: 22327401 - PMCID: PMC3281520 - DOI: 10.1038/nchembio.790

  • 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;119(11):2579-89 - PMID: 22262760 - PMCID: PMC3337713 - DOI: 10.1182/blood-2011-10-387365

  • 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;29(15_suppl):e18569 - PMID: 28023028

  • 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 bc(1) Inhibitors. Chem Biol. 2011;18(12):1602-10 - PMID: 22195562 - PMCID: PMC3474356 - DOI: 10.1016/j.chembiol.2011.09.016

  • 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 - PMID: 22027590 - PMCID: PMC3544154 - DOI: 10.1038/ncomms1518

  • 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(1):381 - PMID: 21974968 - PMCID: PMC3197508 - DOI: 10.1186/1756-0500-4-381

  • 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;54(15):5576-82 - PMID: 21721525 - PMCID: PMC3150598 - DOI: 10.1021/jm200620f

  • 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;52(8):1544-55 - PMID: 21699378 - PMCID: PMC4113006 - DOI: 10.3109/10428194.2011.570821

  • de Zoeten EF, Wang L, Butler K, Beier UH, Akimova T, Sai H, Bradner JE, Mazitschek R, Kozikowski AP, Matthias P, Hancock WW HDAC6 and HSP90 Control The Functions Of Foxp3+ T-Regulatory Cells. Mol Cell Biol. 2011;31(10):2066-78 - PMID: 21444725 - PMCID: PMC3133361 - DOI: 10.1128/MCB.05155-11

  • 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, Jimenez-Diaz MB, Magan N, Gomez V, Ferrer S, Santos Marti Aminoindoles: a Novel Scaffold with Potent Activity against Plasmodium falciparum. Antimicrob Agents Chemother. 2011;55(6):2612-22 - PMID: 21422215 - PMCID: PMC3101419 - DOI: 10.1128/AAC.01714-10

  • 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;2(1):39-42 - PMID: 21874153 - PMCID: PMC3161516 - DOI: 10.1021/ml1001954

  • 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;12(18):3998-4001 - PMID: 20718474 - PMCID: PMC7479540 - DOI: 10.1021/ol101566h

  • 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;107(28):12617-22 - PMID: 20616024 - PMCID: PMC2906581 - DOI: 10.1073/pnas.1006774107

  • Estiu G, West N, Mazitschek R, Greenberg E, Bradner JE, Wiest O On the inhibition of histone deacetylase 8. Bioorg Med Chem. 2010;18(11):4103-4110 - PMID: 20472442 - PMCID: PMC3245874 - DOI: 10.1016/j.bmc.2010.03.080

  • 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;19 (49):2869-2872 - PMID: 20306505 - PMCID: PMC3433403 - DOI: 10.1002/anie.200906120

  • Bradner JE, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T, Mazitschek R Chemical phylogenetics of histone deacetylases. Nat Chem Biol. 2010;6(3):238-243 - PMID: 20139990 - PMCID: PMC2822059 - DOI: 10.1038/nchembio.313

  • 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;316(3):329-40 - PMID: 19932094 - DOI: 10.1016/j.yexcr.2009.11.009

  • 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;20(1):228-31 - PMID: 19914064 - DOI: 10.1016/j.bmcl.2009.10.133

  • Martyn DC, Cortese JF, Tyndall E, Dick J, Mazitschek R, Munoz B, Clardy J Antiplasmodial activity of piperazine sulfonamides. Bioorg Med Chem Lett. 2010;20(1):218-21 - PMID: 19914069 - DOI: 10.1016/j.bmcl.2009.10.130

  • 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;122(Pt 19):3531-41 - PMID: 19737819 - DOI: 10.1242/jcs.046813

  • 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;4(7):527-33 - PMID: 19572548 - PMCID: PMC2745594 - DOI: 10.1021/cb900084v

  • 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;324(5932):1334-1338 - PMID: 19498172 - PMCID: PMC2803727 - DOI: 10.1126/science.1172638

  • 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;459(7243):55-60 - PMID: 19424149 - PMCID: PMC3498958 - DOI: 10.1038/nature07925

  • 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;284(25):17102-9 - PMID: 19386607 - PMCID: PMC2719348 - DOI: 10.1074/jbc.M809090200

  • 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;52(8):2185-7 - PMID: 19317450 - PMCID: PMC2669731 - DOI: 10.1021/jm801654y

  • Rush MA, Baniecki ML, Mazitschek R, Cortese JF, Wiegand R, Clardy J, Wirth DF A colorimetric high throughput screen for the detection of heme crystallization inhibitors. Antimicrob Agents Chemother. 2009;53(6):2564-8 - PMID: 19307367 - PMCID: PMC2687197 - DOI: 10.1128/AAC.01466-08

  • 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;14(22):7340-7 - PMID: 19010849 - PMCID: PMC2744414 - DOI: 10.1158/1078-0432.CCR-08-0642

  • 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. 2008;60(5):803-17 - PMID: 19081376 - PMCID: PMC2912147 - DOI: 10.1016/j.neuron.2008.10.015

  • Schuetz A, Min J, Allali-Hassani A, Schapira M, Shuen M, Loppnau P, Mazitschek R, Kwiatkowski N, Lewis T, Maglathin R, McLean T, Bochkarev A, Plotnikov A, Vedadi M, Arrowsmith C Human HDAC7 harbors a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity. J Biol Chem. 2008;283(17):11355-63 - PMID: 18285338 - PMCID: PMC2431080 - DOI: 10.1074/jbc.M707362200

  • Estiu G, Greenberg E, Harrison C, Kwiatkowski N, Mazitschek R, Bradner J, Wiest O Structural origin of selectivity in class II-selective histone deacetylase inhibitors. J Med Chem. 2008;51:2898-906 - PMID: 18412327 - DOI: 10.1021/jm7015254

  • Mazitschek R, Patel V, Wirth D, Clardy J Development of a fluorescence polarization based assay for histone deacetylase ligand discovery. Bioorg Med Chem Lett. 2008;18(9):2809-12 - PMID: 18430569 - PMCID: PMC2408937 - DOI: 10.1016/j.bmcl.2008.04.007

  • Groen A, Needleman D, Brangwynne C, Gradinaru C, Fowler B, Mazitschek R, Mitchison T A novel small-molecule inhibitor reveals a possible role of kinesin-5 in anastral spindle-pole assembly. J Cell Sci. 2008;121(Pt 14):2293-300 - PMID: 18559893 - PMCID: PMC2902979 - DOI: 10.1242/jcs.024018

  • Hahn C, Ross K, Warrington I, Mazitschek R, Kanegai C, Wright R, Kung A, Golub T, 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;105(28):9751-6 - PMID: 18607002 - PMCID: PMC2474517 - DOI: 10.1073/pnas.0710413105

  • 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;120(Pt 8):1469-79 - PMID: 17389687 - DOI: 10.1242/jcs.03431

  • 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;72(5):1137-45 - PMID: 17675586 - DOI: 10.1124/mol.107.038117

  • 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;13(5):493-504 - PMID: 16720270 - DOI: 10.1016/j.chembiol.2006.03.004

  • 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;17(8):3435-45 - PMID: 16738306 - PMCID: PMC1525231 - DOI: 10.1091/mbc.E06-01-0008

  • 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;108(12):3801-7 - PMID: 16912225 - DOI: 10.1182/blood-2006-03-013235

  • Mazitschek R, Huwe A, Giannis A Synthesis and biological evaluation of novel fumagillin and ovalicin analogues. Org Biomol Chem. 2005;3(11):2150-4 - PMID: 15917904 - DOI: 10.1039/b503163j

  • 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;43(2):224-8 - PMID: 14695616 - DOI: 10.1002/anie.200352582

  • 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. 2004;10:468-75 - PMID: 15273654

  • Mazitschek R, Giannis A Inhibitors of angiogenesis and cancer-related receptor tyrosine kinases. 2004;8(4):432-41 - PMID: 15288254 - DOI: 10.1016/j.cbpa.2004.06.009

  • 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;112(6):986-93 - PMID: 15386354 - DOI: 10.1002/ijc.20509

  • Huwe A, Mazitschek R, Giannis A Small molecules as inhibitors of cyclin-dependent kinases. Angew Chem Int Ed Engl. 2003;42(19):2122-38 - PMID: 12761741 - DOI: 10.1002/anie.200200540

  • 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;46(14):2917-31 - PMID: 12825933 - DOI: 10.1021/jm0307943

  • 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;9(14):3282-91 - PMID: 12866072 - DOI: 10.1002/chem.200304821

  • Mazitschek R, Baumhof P, Giannis A Peptidomimetics and angiogenesis. Mini Rev Med Chem. 2002;2(5):491-506 - PMID: 12370049 - DOI: 10.2174/1389557023405710

  • Addicks E, Mazitschek R, Giannis A Synthesis and biological investigation of novel tricyclic benzodiazepinedione-based RGD analogues. Chembiochem. 2002;3(11):1078-88 - PMID: 12404633 - DOI: 10.1002/1439-7633(20021104)3:11<1078::AID-CBIC1078>3.0.CO;2-2

  • Mazitschek R, Mülbaier M, Giannis A IBX-mediated oxidation of primary alcohols and aldehydes to form carboxylic acids. Angew Chem Int Ed Engl. 2002;41(21):4059-61 - PMID: 12412081 - DOI: 10.1002/1521-3773(20021104)41:21<4059::AID-ANIE4059>3.0.CO;2-R

  • 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;41(24):4757-61 - PMID: 12481350 - DOI: 10.1002/anie.200290040

  • 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;41(7):1174-8 - PMID: 12491250 - DOI: 10.1002/1521-3773(20020402)41:7<1174::aid-anie1174>3.0.co;2-v

  • 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;40(19):3672-3674 - PMID: 11592218 - DOI: 10.1002/1521-3773(20011001)40:19<3672::aid-anie3672>3.0.co;2-y

  • 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;268(21):5530-40 - PMID: 11683876 - DOI: 10.1046/j.1432-1033.2001.02476.x

  • 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;123(47):11586-93 - PMID: 11716712 - DOI: 10.1021/ja011413i

  • 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;38(21):3228-3231 - PMID: 10556911 - DOI: 10.1002/(sici)1521-3773(19991102)38:21<3228::aid-anie3228>3.0.co;2-8