Recent Publications

2018

Class I Histone Deacetylase Inhibition by Tianeptinaline Modulates Neuroplasticity and Enhances Memory.

Zhao WN, Ghosh B, Tyler M, Lalonde J, Joseph NF, Kosaric N, Fass DM, Tsai LH, Mazitschek R, Haggarty SJ.

ACS Chem Neurosci. 2018 Jun 22. doi: 10.1021/acschemneuro.8b00116. [Epub ahead of print]

PMID:29932631

Fluorescence anisotropy imaging in drug discovery.

Vinegoni C, Feruglio PF, Gryczynski I, Mazitschek R, Weissleder R.

Adv Drug Deliv Rev. 2018 Feb 2. pii: S0169-409X(18)30027-9. doi: 10.1016/j.addr.2018.01.019. [Epub ahead of print]

PMID: 29410158

2017

Synthesis and biological evaluation of Santacruzamate-A based analogues.

Randino R, Gazzerro P, Mazitschek R, Rodriquez M.

Bioorg Med Chem. 2017 Dec 15;25(24):6486-6491. doi: 10.1016/j.bmc.2017.10.026. Epub 2017 Oct 20.

PMID: 29100734

Treatment with a selective histone deacetylase 6 inhibitor decreases lupus nephritis in NZB/W mice.

Vieson MD, Gojmerac AM, Khan D, Dai R, van Duzer JH, Mazitschek R, Caudell DL, Liao X, Luo XM, Reilly CM.

Histol Histopathol. 2017 Dec;32(12):1317-1332. doi: 10.14670/HH-11-885. Epub 2017 Feb 28.

PMID: 28245046

HDAC3 regulates DNMT1 expression in multiple myeloma: therapeutic implications.

Harada T, Ohguchi H, Grondin Y, Kikuchi S, Sagawa M, Tai YT, Mazitschek R, Hideshima T, Anderson KC.

Leukemia. 2017 Dec;31(12):2670-2677. doi: 10.1038/leu.2017.144. Epub 2017 May 11.

PMID: 28490812

Modular Bi-Directional One-Pot Strategies for the Diastereoselective Synthesis of Structurally Diverse Collections of Constrained β-Carboline-Benzoxazepines.

Srinivasulu V, Mazitschek R, Kariem NM, Reddy A, Rabeh WM, Li L, O'Connor MJ, Al-Tel TH.

Chemistry. 2017 Oct 12;23(57):14182-14192. doi: 10.1002/chem.201702495. Epub 2017 Sep 7.

PMID:28770556

Lysine Deacetylation by HDAC6 Regulates the Kinase Activity of AKT in Human Neural Progenitor Cells.

Iaconelli J, Lalonde J, Watmuff B, Liu B, Mazitschek R, Haggarty SJ, Karmacharya R.

ACS Chem Biol. 2017 Aug 18;12(8):2139-2148. doi: 10.1021/acschembio.6b01014. Epub 2017 Jul 10.

PMID: 28628306

Selectivity and Kinetic Requirements of HDAC Inhibitors as Progranulin Enhancers for Treating Frontotemporal Dementia.

She A, Kurtser I, Reis SA, Hennig K, Lai J, Lang A, Zhao WN, Mazitschek R, Dickerson BC, Herz J, Haggarty SJ.

Cell Chem Biol. 2017 Jul 20;24(7):892-906.e5. doi: 10.1016/j.chembiol.2017.06.010. Epub 2017 Jul 14.

PMID: 28712747

HDAC6 inhibitor WT161 downregulates growth factor receptors in breast cancer.

Hideshima T, Mazitschek R, Qi J, Mimura N, Tseng JC, Kung AL, Bradner JE, Anderson KC.

Oncotarget. 2017 Jul 5;8(46):80109-80123. doi: 10.18632/oncotarget.19019. eCollection 2017 Oct 6.

PMID: 29113288

Measurement of drug-target engagement in live cells by two-photon fluorescence anisotropy imaging.

Vinegoni C, Fumene Feruglio P, Brand C, Lee S, Nibbs AE, Stapleton S, Shah S, Gryczynski I, Reiner T, Mazitschek R, Weissleder R.

Nat Protoc. 2017 Jul;12(7):1472-1497. doi: 10.1038/nprot.2017.043. Epub 2017 Jun 29.

PMID: 28686582

HDAC6 inhibition effectively reverses chemotherapy-induced peripheral neuropathy.

Krukowski K, Ma J, Golonzhka O, Laumet GO, Gutti T, van Duzer JH, Mazitschek R, Jarpe MB, Heijnen CJ, Kavelaars A.

Pain. 2017 Jun;158(6):1126-1137. doi: 10.1097/j.pain.0000000000000893.

PMID: 28267067

Intramolecular Diaza-Diels-Alder Protocol: A New Diastereoselective and Modular One-Step Synthesis of Constrained Polycyclic Frameworks.

Srinivasulu V, Reddy A, Mazitschek R, Lukens AK, Wirth DF, Li L, Naumov P, O'Connor MJ, Al-Tel TH.

Chemistry. 2017 Mar 23;23(17):4137-4148. doi: 10.1002/chem.201605231. Epub 2017 Feb 17.

PMID: 27997727

Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models.

Huang P, Almeciga-Pinto I, Jarpe M, van Duzer JH, Mazitschek R, Yang M, Jones SS, Quayle SN.

Oncotarget. 2017 Jan 10;8(2):2694-2707. doi: 10.18632/oncotarget.13738.

PMID: 27926524

2016

Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma.

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.

Proc Natl Acad Sci U S A. 2016 Oct 31. pii: 201608067. PMID: 27799547

Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites.

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.

ChemMedChem. 2016 Oct 6;11(19):2194-2204. doi: 10.1002/cmdc.201600327. PMID: 27538856

Light-controlled modulation of gene expression by chemical optoepigenetic probes.

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.

Nat Chem Biol. 2016 Mar 14. doi: 10.1038/nchembio.2042. PMID: 26974814

Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation.

Ghosh B, Zhao WN, Reis SA, Patnaik D, Fass DM, Tsai LH, Mazitschek R, Haggarty SJ.

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1265-71. doi: 10.1016/j.bmcl.2016.01.022. PMID: 26804233

2015

Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype.

Santos SA, Lukens AK, Coelho L, Nogueira F, Wirth DF, Mazitschek R, Moreira R, Paulo A.

Eur J Med Chem. 2015 Sep 18;102:320-33. doi: 10.1016/j.ejmech.2015.07.047. PMID: 26295174

Advances in measuring single-cell pharmacokinetics and pharmacology in vivo.

Vinegoni C, Dubach JM, Thurber GM, Miller MA, Mazitschek R, Weissleder R.

Drug Discov Today. 2015 May 26. pii: S1359-6446(15)00219-6. doi: 10.1016/j.drudis.2015.05.011. PMID:26024776

Treatment of obesity with celastrol.

Liu J, Lee J, Salazar Hernandez MA, Mazitschek R, Ozcan U.

Cell. 2015 May 21;161(5):999-1011. doi: 10.1016/j.cell.2015.05.011. PMID:26000480

The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs.

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 Jr, Zhou H, Bopp SE, Schimmel P, Lindquist S, Clardy J, Mota MM, Keller TL, Whitman M, Wiest O, Wirth DF, Mazitschek R.

Sci Transl Med. 2015 May 20;7(288):288ra77. doi: 10.1126/scitranslmed.aaa3575. PMID: 25995223

Live-cell multiphoton fluorescence correlation spectroscopy with an improved large Stokes shift fluorescent protein.

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.

Mol Biol Cell. 2015 Jun 1;26(11):2054-66. doi: 10.1091/mbc.E14-10-1473. Epub 2015 Apr 15. PMID: 25877871

Targeting class I histone deacetylase 2 in MYC amplified group 3 medulloblastoma.

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.

Acta Neuropathol Commun. 2015 Apr 3;3(1):22. doi: 10.1186/s40478-015-0201-7. PMID: 25853389

Inhibition of histone deacetylase 6 improves long-term survival in a lethal septic model.

Li Y, Zhao T, Liu B, Halaweish I, Mazitschek R, Duan X, Alam HB.

J Trauma Acute Care Surg. 2015 Feb;78(2):378-85. doi: 10.1097/TA.0000000000000510. PMID: 25757125

HDAC6 inhibitors modulate Lys49 acetylation and membrane localization of β-catenin in human iPSC-derived neuronal cells.

Iaconelli J, Huang JH, Berkovitch SS, Chattopadhyay S, Mazitschek R, Schreiber SL, Haggarty SJ, Karmacharya R.

ACS Chem Biol. 2015 Mar 20;10(3):883-90. doi: 10.1021/cb500838r. Epub 2015 Jan 8. PMID: 25546293

Protective effect of suberoylanilide hydroxamic acid against lipopolysaccharide-induced liver damage in rodents.

Zhao Y, Zhou P, Liu B, Bambakidis T, Mazitschek R, Alam HB, Li Y.

J Surg Res. 2015 Apr;194(2):544-50. doi: 10.1016/j.jss.2014.10.056. Epub 2014 Nov 6. PMID: 25479907

2014

Syntheses and discovery of a novel class of cinnamic hydroxamates as histone deacetylase inhibitors by multimodality molecular imaging in living subjects.

Chan CT, Qi J, Smith W, Paranol R, Mazitschek R, West N, Reeves R, Chiosis G, Schreiber SL, Bradner JE, Paulmurugan R, Gambhir SS.

Cancer Res. 2014 Dec 15;74(24):7475-86. doi: 10.1158/0008-5472.CAN-14-0197. Epub 2014 Oct 15. PMID: 25320008.

Chemical interrogation of the malaria kinome.

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.

Chembiochem. 2014 Sep 5;15(13):1920-30. doi: 10.1002/cbic.201400025. Epub 2014 Aug 8. PMID: 25111632

Selective inhibition of histone deacetylase 6 alters the composition of circulating blood cells in a lethal septic model.

Zhao T, Li Y, Liu B, Halaweish I, Mazitschek R, Alam HB.

J Surg Res. 2014 Aug;190(2):647-54. doi: 10.1016/j.jss.2014.01.056. Epub 2014 Feb 4. PMID: 24613069

Efficient acid-catalyzed (18) F/(19) F fluoride exchange of BODIPY dyes.

Keliher EJ, Klubnick JA, Reiner T, Mazitschek R, Weissleder R.

ChemMedChem. 2014 Jul;9(7):1368-73. doi: 10.1002/cmdc.201300506. Epub 2014 Mar 5. PMID: 24596307

Monoalkoxy BODIPYs--a fluorophore class for bioimaging.

Courtis AM, Santos SA, Guan Y, Hendricks JA, Ghosh B, Szantai-Kis DM, Reis SA, Shah JV,Mazitschek R.

Bioconjug Chem. 2014 Jun 18;25(6):1043-51. doi: 10.1021/bc400575w. Epub 2014 May 14. PMID: 24797834

In vivo imaging of specific drug-target binding at subcellular resolution.

Dubach JM, Vinegoni C, Mazitschek R, Fumene Feruglio P, Cameron LA, Weissleder R.

Nat Commun. 2014 May 28;5:3946. doi: 10.1038/ncomms4946. PMID: 24867710

Histone deacetylase 3 as a novel therapeutic target in multiple myeloma.

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.

Leukemia. 2014 Mar;28(3):680-9. doi: 10.1038/leu.2013.231. Epub 2013 Aug 5. PMID: 23913134

Induction of differential apoptotic pathways in multiple myeloma cells by class-selective histone deacetylase inhibitors.

Hideshima T, Mazitschek R, Santo L, Mimura N, Gorgun G, Richardson PG, Raje N, Anderson KC.

Leukemia. 2014 Feb;28(2):457-60. doi: 10.1038/leu.2013.301. Epub 2013 Oct 22.  PMID: 24150220

A genomic and evolutionary approach reveals non-genetic drug resistance in malaria.

Herman JD, Rice DP, Ribacke U, Silterra J, Deik AA, Moss EL, Broadbent KM, Neafsey DE, Desai MM, Clish CB, Mazitschek R, Wirth DF.

Genome Biol. 2014;15(11):511. PMID: 25395010

Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability.

Jochems J, Boulden J, Lee BG, Blendy JA, Jarpe M, Mazitschek R, Van Duzer JH, Jones S, Berton O.

Neuropsychopharmacology. 2014 Jan;39(2):389-400. doi: 10.1038/npp.2013.207. Epub 2013 Aug 19.

PMID: 23954848

2013

Septins promote dendrite and axon development by negatively regulating microtubule stability via HDAC6-mediated deacetylation.

Ageta-Ishihara N, Miyata T, Ohshima C, Watanabe M, Sato Y, Hamamura Y, Higashiyama T,Mazitschek R, Bito H, Kinoshita M.

Nat Commun. 2013;4:2532. doi: 10.1038/ncomms3532. PMID: 24113571

Crebinostat: a novel cognitive enhancer that inhibits histone deacetylase activity and modulates chromatin-mediated neuroplasticity.

Fass DM, Reis SA, Ghosh B, Hennig KM, Joseph NF, Zhao WN, Nieland TJ, Guan JS, Kuhnle CE, Tang W, Barker DD, Mazitschek R, Schreiber SL, Tsai LH, Haggarty SJ.

Neuropharmacology. 2013 Jan;64:81-96. doi: 10.1016/j.neuropharm.2012.06.043. Epub 2012 Jul 4. PMID: 22771460