Recent Publications

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