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Yeo MJR, Zhang O, Xie X, Nam E, Payne NC, Gosavi PM, Kwok HS, Iram I, Lee C, Li J, Chen NJ, Nguyen K, Jiang H, Wang ZA, Lee K, Mao H, Harry SA, Barakat IA, Takahashi M, Waterbury AL, Barone M, Mattevi A, Carr SA, Udeshi ND, Bar-Peled L, Cole PA, Mazitschek R, Liau BB, Zheng N

UM171 glues asymmetric CRL3-HDAC1/2 assembly to degrade CoREST corepressors.
Nature. 2025;639(8053):232-240 - PMID: 39939761 - PMCID: PMC11882444 - DOI: 10.1038/s41586-024-08532-4

Xie X, Zhang O, Yeo MJR, Lee C, Tao R, Harry SA, Payne NC, Nam E, Paul L, Li Y, Kwok HS, Jiang H, Mao H, Hadley JL, Lin H, Batts M, Gosavi PM, D'Angiolella V, Cole PA, Mazitschek R, Northcott PA, Zheng N, Liau BB

Converging mechanism of UM171 and KBTBD4 neomorphic cancer mutations.
Nature. 2025;639(8053):241-249 - PMID: 39939763 - PMCID: PMC11882451 - DOI: 10.1038/s41586-024-08533-3

Zhu Q, Fischer G, Cheng SS, Payne NC, Peter D, Mody AC, Arce-Solano S, Shen D, Lin Z, Mazitschek R, Kessler D, Woo CM

Enzyme-Activated Sugar-Coated Bifunctional Degraders.
J Am Chem Soc. 2025;147(38):34672-34680 - PMID: 40937862 - DOI: 10.1021/jacs.5c09843

Amako Y, Ichikawa S, Lloyd HC, Payne NC, Lin Z, Boghossian AS, Rees MG, Ronan MM, Roth JA, Zhu Q, Budnik B, Mazitschek R, Woo CM

The contribution of cyclic imide stereoisomers on cereblon-dependent activity.
Chem Sci. 2025;16(25):11519-11529 - PMID: 40443985 - PMCID: PMC12117711 - DOI: 10.1039/d5sc01371b

Bopp S, Fagbami L, Deik A, Taccheri C, Pant A, Luth M, Chen D, Tye MA, Ullah I, Kreuzer J, Morris R, Haas W, Winzeler EA, Clish C, Lukens AK, Mazitschek R, Wirth DF

Disruption of P. falciparum amino acid transporter elevates intracellular proline and induces resistance to Prolyl-tRNA synthetase inhibitors.
Cell Chem Biol. 2025;32(10):1293-1302.e5 - PMID: 41061700 - DOI: 10.1016/j.chembiol.2025.09.007

Lloyd HC, Li Y, Payne NC, Zhao Z, Xu W, Kroupova A, Zollman D, Long T, Kabir F, Chen M, Freeman R, Feng EY, Xi SY, Hsu YC, Ciulli A, Mazitschek R, Woo CM

A method for the detection and enrichment of endogenous cereblon substrates.
Cell Chem Biol. 2025;32(8):1028-1041.e13 - PMID: 40782806 - PMCID: PMC12360616 - DOI: 10.1016/j.chembiol.2025.07.002

Stopka SA, Bodineau C, Baquer G, Lin JR, Hossain MA, Martinez CJ, Regan MS, Ruiz D, Fletcher SM, Pourquié O, Lutsenko S, Payne CN, Agar JN, Mazitschek R, McDannold NJ, Sorger PK, Santagata S, Agar NYR

Spatial Profiling of Elements through Matrix-Assisted Laser Desorption Ionization Mass Spectrometry Imaging.
Anal Chem. 2025;97(45):25334-25345 - PMID: 41201007 - DOI: 10.1021/acs.analchem.5c05632

Merz ML, Shoba VM, Pergu R, Severance ZC, Munkanatta Godage DNP, Deb A, Kwok HS, Singh P, Singh S, Allen JB, Tian W, Gosavi PM, Chaudhary SK, Anokhina V, Weisberg EL, Payne NC, He Y, Osadchey R, Shekhar M, Mazitschek R, Rees MG, Roth JA, Cui Q, Griffin JD, Liau BB, Choudhary A

Phosphorylation-inducing chimera rewires oncogenic kinase to trigger apoptosis.
bioRxiv. 2025;:ePub - PMID: 40661463 - PMCID: PMC12259158 - DOI: 10.1101/2025.06.13.659082

Lloyd HC, Li Y, Payne N, Zhao Z, Xu W, Kroupova A, Zollman D, Long T, Kabir F, Chen M, Freeman R, Feng EY, Xi S, Hsu YC, Ciulli A, Mazitschek R, Woo CM

A method for the detection and enrichment of endogenous cereblon substrates.
bioRxiv. 2025;:ePub - PMID: 40196695 - PMCID: PMC11974815 - DOI: 10.1101/2025.03.24.645063

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;36(21):e2311467 - PMID: 38241649 - PMCID: PMC11257647 - DOI: 10.1002/adma.202311467

Hammel FA, Payne NC, Marando VM, Mazitschek R, Walker S

Identification of a Polypeptide Inhibitor of O-GlcNAc Transferase with Picomolar Affinity.
J Am Chem Soc. 2024;146(38):26320-26330 - PMID: 39276112 - PMCID: PMC11440498 - DOI: 10.1021/jacs.4c08656

Antolin AA, Aye Y, Bar-Peled L, De Vita E, Dudkina N, Jewett MC, Kiely-Collins H, Mazitschek R, Zhang ZJ

What is chemical biology?
Cell Chem Biol. 2024;31(9):1562-1565 - PMID: 39303695 - DOI: 10.1016/j.chembiol.2024.08.011

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;31(6):1162-1175.e10 - PMID: 38320555 - PMCID: PMC12136240 - 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

Payne NC, Ichikawa S, Woo CM, Mazitschek R

Protocol for the comprehensive biochemical and cellular profiling of small-molecule degraders using CoraFluor TR-FRET technology.
STAR Protoc. 2024;5(2):103129 - PMID: 38857155 - PMCID: PMC11193044 - DOI: 10.1016/j.xpro.2024.103129

Xie X, Zhang O, Yeo MJR, Lee C, Harry SA, Paul L, Li Y, Payne NC, Nam E, Kwok HS, Jiang H, Mao H, Hadley JL, Lin H, Batts M, Gosavi PM, D'Angiolella V, Cole PA, Mazitschek R, Northcott PA, Zheng N, Liau BB

KBTBD4 Cancer Hotspot Mutations Drive Neomorphic Degradation of HDAC1/2 Corepressor Complexes.
bioRxiv. 2024;:ePub - PMID: 38798357 - PMCID: PMC11118371 - DOI: 10.1101/2024.05.14.593970

Yeo MJ, Zhang O, Xie X, Nam E, Payne NC, Gosavi PM, Kwok HS, Iram I, Lee C, Li J, Chen NJ, Jiang H, Wang ZA, Lee K, Mao H, Harry SA, Barakat IA, Takahashi M, Waterbury AL, Barone M, Mattevi A, Bar-Peled L, Cole PA, Mazitschek R, Liau BB, Zheng N

Asymmetric Engagement of Dimeric CRL3 KBTBD4 by the Molecular Glue UM171 Licenses Degradation of HDAC1/2 Complexes.
bioRxiv. 2024;:ePub - PMID: 38798619 - PMCID: PMC11118476 - DOI: 10.1101/2024.05.14.593897

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

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

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

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

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

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

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

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

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

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

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

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

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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