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Guan D, Men Y, Bartlett A, Hernández MAS, Xu J, Yi X, Li HS, Kong D, Mazitschek R, Ozcan U
Central inhibition of HDAC6 re-sensitizes leptin signaling during obesity to induce profound weight loss.
Cell Metab. 2024;36(4):857-876.e10 - PMID: 38569472 - DOI: 10.1016/j.cmet.2024.02.007
Carrow 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 NC
Inhibiting the Keap1/Nrf2 Protein-Protein Interaction with Protein-Like Polymers.
Adv Mater. 2024;:e2311467 - PMID: 38241649 - DOI: 10.1002/adma.202311467
Ichikawa S, Payne NC, Xu W, Chang CF, Vallavoju N, Frome S, Flaxman HA, Mazitschek R, Woo CM
The cyclimids: Degron-inspired cereblon binders for targeted protein degradation.
Cell Chem Biol. 2024;:ePub - PMID: 38320555 - DOI: 10.1016/j.chembiol.2024.01.003
Rosenthal ZC, Fass DM, Payne NC, She A, Patnaik D, Hennig KM, Tesla R, Werthmann GC, Guhl C, Reis SA, Wang X, Chen Y, Placzek M, Williams NS, Hooker J, Herz J, Mazitschek R, Haggarty SJ
Epigenetic modulation through BET bromodomain inhibitors as a novel therapeutic strategy for progranulin-deficient frontotemporal dementia.
Sci Rep. 2024;14(1):9064 - PMID: 38643236 - PMCID: PMC11032351 - DOI: 10.1038/s41598-024-59110-7
Pryce 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 V
Oxycodone withdrawal induces HDAC1/HDAC2-dependent transcriptional maladaptations in the reward pathway in a mouse model of peripheral nerve injury.
Nat Neurosci. 2023;26(7):1229-1244 - PMID: 37291337 - PMCID: PMC10752505 - DOI: 10.1038/s41593-023-01350-3
Kurata K, Bott AJ, 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 U
Prolyl-tRNA synthetase as a novel therapeutic target in multiple myeloma.
Blood Cancer J. 2023;13(1):12 - PMID: 36631435 - PMCID: PMC9834298 - DOI: 10.1038/s41408-023-00787-w
Armstrong 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 JA
Advances in Malaria Pharmacology and the online Guide to MALARIA PHARMACOLOGY: IUPHAR Review X.
Br J Pharmacol. 2023;180(15):1899-1929 - PMID: 37197802 - DOI: 10.1111/bph.16144
Yue 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 ES
Diagnostic TR-FRET assays for detection of antibodies in patient samples.
Cell Rep Methods. 2023;3(3):100421 - PMID: 37056371 - PMCID: PMC10088089 - DOI: 10.1016/j.crmeth.2023.100421
Mandt REK, Luth MR, Tye MA, Mazitschek R, Ottilie S, Winzeler EA, Lafuente-Monasterio MJ, Gamo FJ, Wirth DF, Lukens AK
Diverse evolutionary pathways challenge the use of collateral sensitivity as a strategy to suppress resistance.
eLife. 2023;12:ePub - PMID: 37737220 - PMCID: PMC10695565 - DOI: 10.7554/eLife.85023
Adamson RJ, Payne NC, Bartual SG, Mazitschek R, Bullock AN
Structural and biochemical characterization establishes a detailed understanding of KEAP1-CUL3 complex assembly.
Free Radic Biol Med. 2023;204:215-225 - PMID: 37156295 - PMCID: PMC10564622 - DOI: 10.1016/j.freeradbiomed.2023.04.021
Michelson 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 S
A randomized, double-blind, placebo-controlled study of histone deacetylase type 6 inhibition for the treatment of painful diabetic peripheral neuropathy.
Pain Rep. 2023;8(6):e1114 - PMID: 37899940 - PMCID: PMC10611336 - DOI: 10.1097/PR9.0000000000001114
Kitson SL, Watters W, Moody TS, Chappell T, Mazitschek R
Nitrilase 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;66(7-8):172-179 - PMID: 37186406 - DOI: 10.1002/jlcr.4026
Tye 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 R
Elucidating the path to Plasmodium prolyl-tRNA synthetase inhibitors that overcome halofuginone resistance.
Nat Commun. 2022;13(1):4976 - PMID: 36008486 - PMCID: PMC9403976 - DOI: 10.1038/s41467-022-32630-4
Payne NC, Maksoud S, Tannous BA, Mazitschek R
A direct high-throughput protein quantification strategy facilitates discovery and characterization of a celastrol-derived BRD4 degrader.
Cell Chem Biol. 2022;29(8):1333-1340.e5 - PMID: 35649410 - PMCID: PMC9391279 - DOI: 10.1016/j.chembiol.2022.05.003
Payne NC, Mazitschek R
Resolving the deceptive isoform and complex selectivity of HDAC1/2 inhibitors.
Cell Chem Biol. 2022;29(7):1140-1152.e5 - PMID: 35298895 - DOI: 10.1016/j.chembiol.2022.03.002
Srinivasulu V, Srikanth G, Khanfar MA, Abu-Yousef IA, Majdalawieh AF, Mazitschek R, Setty SC, Sebastian A, Al-Tel TH
Stereodivergent Complexity-to-Diversity Strategy en Route to the Synthesis of Nature-Inspired Skeleta.
J Org Chem. 2022;87(2):1377-1397 - PMID: 35014258 - DOI: 10.1021/acs.joc.1c02698
Payne NC, Kalyakina AS, Singh K, Tye MA, Mazitschek R
Bright and stable luminescent probes for target engagement profiling in live cells.
Nat Chem Biol. 2021;17(11):1168-1177 - PMID: 34675420 - PMCID: PMC8555866 - DOI: 10.1038/s41589-021-00877-5
Poli V, Pui-Yan Ma V, Di Gioia M, Broggi A, Benamar M, Chen Q, Mazitschek R, Haggarty SJ, Chatila TA, Karp JM, Zanoni I
Zinc-dependent histone deacetylases drive neutrophil extracellular trap formation and potentiate local and systemic inflammation.
iScience. 2021;24(11):103256 - PMID: 34761180 - PMCID: PMC8567386 - DOI: 10.1016/j.isci.2021.103256
El-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 TH
Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.
Bioorg Med Chem. 2021;42:116251 - PMID: 34116381 - DOI: 10.1016/j.bmc.2021.116251
Sandoval 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 PLSM
The Prolyl-tRNA Synthetase Inhibitor Halofuginone Inhibits SARS-CoV-2 Infection.
bioRxiv. 2021;:ePub - PMID: 33791697 - PMCID: PMC8010724 - DOI: 10.1101/2021.03.22.436522
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
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;64(10):ePub - PMID: 32661007 - PMCID: PMC7508603 - 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 - PMCID: PMC7995447 - DOI: 10.1021/acschembio.0c00104
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
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
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. 2019;34(1):196-209 - PMID: 31142847 - PMCID: PMC6883144 - DOI: 10.1038/s41375-019-0493-x
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, 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
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
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
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
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
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
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, 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
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
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
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
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
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
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
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;32(12):1317-1332 - PMID: 28245046 - DOI: 10.14670/HH-11-885
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
Keliher EJ, Klubnick JA Reiner T, Mazitschek R, Weissleder R
Efficient Acid-Catalyzed (18) F/(19) F Fluoride Exchange of BODIPY Dyes.
ChemMedChem. 2014;9(7):1368-73 - PMID: 24596307 - PMCID: PMC4145401 - DOI: 10.1002/cmdc.201300506
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. 2014;194(2):544-550 - PMID: 25479907 - PMCID: PMC4361238 - DOI: 10.1016/j.jss.2014.10.056
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
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
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. 2013;28(3):680-9 - PMID: 23913134 - PMCID: PMC4165599 - DOI: 10.1038/leu.2013.231
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. 2013;28(2):457-60 - PMID: 24150220 - PMCID: PMC4405100 - DOI: 10.1038/leu.2013.301
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
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
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
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
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
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
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. 2012;64(1):81-96 - PMID: 22771460 - PMCID: PMC3447535 - DOI: 10.1016/j.neuropharm.2012.06.043
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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. 2009;316(3):329-40 - PMID: 19932094 - DOI: 10.1016/j.yexcr.2009.11.009
Martyn DC, Cortese JF, Tyndall E, Dick J, Mazitschek R, Munoz B, Clardy J
Antiplasmodial activity of piperazine sulfonamides.
Bioorg Med Chem Lett. 2009;20(1):218-21 - PMID: 19914069 - DOI: 10.1016/j.bmcl.2009.10.130
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. 2009;20(1):228-31 - PMID: 19914064 - DOI: 10.1016/j.bmcl.2009.10.133
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
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
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
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
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
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
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
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
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
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
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
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
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
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, 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
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, Baumhof P, Giannis A
Peptidomimetics and angiogenesis.
Mini Rev Med Chem. 2002;2(5):491-506 - PMID: 12370049 - DOI: 10.2174/1389557023405710
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
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
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
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
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