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SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Curtin ML, Pliushchev MA, Li HQ, Torrent M, Dietrich JD, Jakob CG, Zhu H, Zhao H, Wang Y, Ji Z, Clark RF, Sarris KA, Selvaraju S, Shaw B, Algire MA, He Y, Richardson PL, Sweis RF, Sun C, Chiang GG, Michaelides MR. Curtin ML, et al. Among authors: zhu h. Bioorg Med Chem Lett. 2017 Apr 1;27(7):1576-1583. doi: 10.1016/j.bmcl.2017.02.030. Epub 2017 Feb 20. Bioorg Med Chem Lett. 2017. PMID: 28254486
The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.
He Y, Selvaraju S, Curtin ML, Jakob CG, Zhu H, Comess KM, Shaw B, The J, Lima-Fernandes E, Szewczyk MM, Cheng D, Klinge KL, Li HQ, Pliushchev M, Algire MA, Maag D, Guo J, Dietrich J, Panchal SC, Petros AM, Sweis RF, Torrent M, Bigelow LJ, Senisterra G, Li F, Kennedy S, Wu Q, Osterling DJ, Lindley DJ, Gao W, Galasinski S, Barsyte-Lovejoy D, Vedadi M, Buchanan FG, Arrowsmith CH, Chiang GG, Sun C, Pappano WN. He Y, et al. Among authors: zhu h. Nat Chem Biol. 2017 Apr;13(4):389-395. doi: 10.1038/nchembio.2306. Epub 2017 Jan 30. Nat Chem Biol. 2017. PMID: 28135237
Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8.
Judge RA, Zhu H, Upadhyay AK, Bodelle PM, Hutchins CW, Torrent M, Marin VL, Yu W, Vedadi M, Li F, Brown PJ, Pappano WN, Sun C, Petros AM. Judge RA, et al. Among authors: zhu h. ACS Med Chem Lett. 2016 Oct 11;7(12):1102-1106. doi: 10.1021/acsmedchemlett.6b00303. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994746 Free PMC article.
Erratum: The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.
He Y, Selvaraju S, Curtin ML, Jakob CG, Zhu H, Comess KM, Shaw B, The J, Lima-Fernandes E, Szewczyk MM, Cheng D, Klinge KL, Li HQ, Pliushchev M, Algire MA, Maag D, Guo J, Dietrich J, Panchal SC, Petros AM, Sweis RF, Torrent M, Bigelow LJ, Senisterra G, Li F, Kennedy S, Wu Q, Osterling DJ, Lindley DJ, Gao W, Galasinski S, Barsyte-Lovejoy D, Vedadi M, Buchanan FG, Arrowsmith CH, Chiang GG, Sun C, Pappano WN. He Y, et al. Among authors: zhu h. Nat Chem Biol. 2017 Jul 18;13(8):922. doi: 10.1038/nchembio0817-922b. Nat Chem Biol. 2017. PMID: 28853738 No abstract available.
Identification and structure-based drug design of cell-active inhibitors of interleukin 17A at a novel C-terminal site.
Goedken ER, Argiriadi MA, Dietrich JD, Petros AM, Krishnan N, Panchal SC, Qiu W, Wu H, Zhu H, Adams AM, Bodelle PM, Goguen L, Richardson PL, Slivka PF, Srikumaran M, Upadhyay AK, Wu B, Judge RA, Vasudevan A, Gopalakrishnan SM, Cox PB, Stoll VS, Sun C. Goedken ER, et al. Among authors: zhu h. Sci Rep. 2022 Aug 26;12(1):14561. doi: 10.1038/s41598-022-18760-1. Sci Rep. 2022. PMID: 36028520 Free PMC article.
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