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KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR and BMYB-Regulated Genes.
Duan L, Rai G, Roggero C, Zhang QJ, Wei Q, Ma SH, Zhou Y, Santoyo J, Martinez ED, Xiao G, Raj GV, Jadhav A, Simeonov A, Maloney DJ, Rizo J, Hsieh JT, Liu ZP. Duan L, et al. Among authors: jadhav a. Chem Biol. 2015 Sep 17;22(9):1185-96. doi: 10.1016/j.chembiol.2015.08.007. Epub 2015 Sep 10. Chem Biol. 2015. PMID: 26364928 Free PMC article.
Structure-activity relationship studies and biological characterization of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors.
Duveau DY, Yasgar A, Wang Y, Hu X, Kouznetsova J, Brimacombe KR, Jadhav A, Simeonov A, Thomas CJ, Maloney DJ. Duveau DY, et al. Among authors: jadhav a. Bioorg Med Chem Lett. 2014 Jan 15;24(2):630-5. doi: 10.1016/j.bmcl.2013.11.081. Epub 2013 Dec 4. Bioorg Med Chem Lett. 2014. PMID: 24360556 Free PMC article.
4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-methoxypyridin-2-yl)piperazine-1-carbothioamide (ML267), a potent inhibitor of bacterial phosphopantetheinyl transferase that attenuates secondary metabolism and thwarts bacterial growth.
Foley TL, Rai G, Yasgar A, Daniel T, Baker HL, Attene-Ramos M, Kosa NM, Leister W, Burkart MD, Jadhav A, Simeonov A, Maloney DJ. Foley TL, et al. Among authors: jadhav a. J Med Chem. 2014 Feb 13;57(3):1063-78. doi: 10.1021/jm401752p. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24450337 Free PMC article.
Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer.
Dexheimer TS, Rosenthal AS, Luci DK, Liang Q, Villamil MA, Chen J, Sun H, Kerns EH, Simeonov A, Jadhav A, Zhuang Z, Maloney DJ. Dexheimer TS, et al. Among authors: jadhav a. J Med Chem. 2014 Oct 9;57(19):8099-110. doi: 10.1021/jm5010495. Epub 2014 Sep 17. J Med Chem. 2014. PMID: 25229643 Free PMC article.
A potent and selective inhibitor targeting human and murine 12/15-LOX.
Armstrong MM, Freedman CJ, Jung JE, Zheng Y, Kalyanaraman C, Jacobson MP, Simeonov A, Maloney DJ, van Leyen K, Jadhav A, Holman TR. Armstrong MM, et al. Among authors: jadhav a. Bioorg Med Chem. 2016 Mar 15;24(6):1183-90. doi: 10.1016/j.bmc.2016.01.042. Epub 2016 Jan 21. Bioorg Med Chem. 2016. PMID: 26899595 Free PMC article.
Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds.
Horton JR, Liu X, Gale M, Wu L, Shanks JR, Zhang X, Webber PJ, Bell JSK, Kales SC, Mott BT, Rai G, Jansen DJ, Henderson MJ, Urban DJ, Hall MD, Simeonov A, Maloney DJ, Johns MA, Fu H, Jadhav A, Vertino PM, Yan Q, Cheng X. Horton JR, et al. Among authors: jadhav a. Cell Chem Biol. 2016 Jul 21;23(7):769-781. doi: 10.1016/j.chembiol.2016.06.006. Epub 2016 Jul 14. Cell Chem Biol. 2016. PMID: 27427228 Free PMC article.
Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.
Horton JR, Liu X, Wu L, Zhang K, Shanks J, Zhang X, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Pohida K, Fang Y, Hu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Yan Q, Cheng X. Horton JR, et al. Among authors: jadhav a. J Med Chem. 2018 Apr 12;61(7):3193-3208. doi: 10.1021/acs.jmedchem.8b00261. Epub 2018 Mar 23. J Med Chem. 2018. PMID: 29537847 Free PMC article.
KDM5 histone demethylases repress immune response via suppression of STING.
Wu L, Cao J, Cai WL, Lang SM, Horton JR, Jansen DJ, Liu ZZ, Chen JF, Zhang M, Mott BT, Pohida K, Rai G, Kales SC, Henderson MJ, Hu X, Jadhav A, Maloney DJ, Simeonov A, Zhu S, Iwasaki A, Hall MD, Cheng X, Shadel GS, Yan Q. Wu L, et al. Among authors: jadhav a. PLoS Biol. 2018 Aug 6;16(8):e2006134. doi: 10.1371/journal.pbio.2006134. eCollection 2018 Aug. PLoS Biol. 2018. PMID: 30080846 Free PMC article.
1,042 results