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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: he y. 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
Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors.
Wilsbacher JL, Cheng M, Cheng D, Trammell SAJ, Shi Y, Guo J, Koeniger SL, Kovar PJ, He Y, Selvaraju S, Heyman HR, Sorensen BK, Clark RF, Hansen TM, Longenecker KL, Raich D, Korepanova AV, Cepa S, Towne DL, Abraham VC, Tang H, Richardson PL, McLoughlin SM, Badagnani I, Curtin ML, Michaelides MR, Maag D, Buchanan FG, Chiang GG, Gao W, Rosenberg SH, Brenner C, Tse C. Wilsbacher JL, et al. Among authors: he y. Mol Cancer Ther. 2017 Jul;16(7):1236-1245. doi: 10.1158/1535-7163.MCT-16-0819. Epub 2017 May 3. Mol Cancer Ther. 2017. PMID: 28468779
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. Nat Chem Biol. 2017 Apr;13(4):389-395. doi: 10.1038/nchembio.2306. Epub 2017 Jan 30. Nat Chem Biol. 2017. PMID: 28135237
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