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De Novo Design, Synthesis, and Biological Evaluation of 3,4-Disubstituted Pyrrolidine Sulfonamides as Potent and Selective Glycine Transporter 1 Competitive Inhibitors.
Wang Y, Zhao H, Brewer JT, Li H, Lao Y, Amberg W, Behl B, Akritopoulou-Zanze I, Dietrich J, Lange UEW, Pohlki F, Hoft C, Hornberger W, Djuric SW, Sydor J, Mezler M, Relo AL, Vasudevan A. Wang Y, et al. Among authors: li h. J Med Chem. 2018 Sep 13;61(17):7486-7502. doi: 10.1021/acs.jmedchem.8b00295. Epub 2018 Jul 17. J Med Chem. 2018. PMID: 29969029
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: li f, li hq. Nat Chem Biol. 2017 Apr;13(4):389-395. doi: 10.1038/nchembio.2306. Epub 2017 Jan 30. Nat Chem Biol. 2017. PMID: 28135237
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: li hq. 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 of Novel Aminotetralines and Aminochromanes as Selective and Competitive Glycine Transporter 1 (GlyT1) Inhibitors.
Amberg W, Lange UEW, Ochse M, Pohlki F, Behl B, Relo AL, Hornberger W, Hoft C, Mezler M, Sydor J, Wang Y, Zhao H, Brewer JT, Dietrich J, Li H, Akritopoulou-Zanze I, Lao Y, Hannick SM, Ku YY, Vasudevan A. Amberg W, et al. Among authors: li h. J Med Chem. 2018 Sep 13;61(17):7503-7524. doi: 10.1021/acs.jmedchem.8b00300. Epub 2018 Aug 27. J Med Chem. 2018. PMID: 30080045
Piperazine sulfonamides as potent, selective, and orally available 11beta-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model.
Xiang J, Wan ZK, Li HQ, Ipek M, Binnun E, Nunez J, Chen L, McKew JC, Mansour TS, Xu X, Suri V, Tam M, Xing Y, Li X, Hahm S, Tobin J, Saiah E. Xiang J, et al. J Med Chem. 2008 Jul 24;51(14):4068-71. doi: 10.1021/jm8004948. Epub 2008 Jun 26. J Med Chem. 2008. PMID: 18578516
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