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Page 1
The development of highly potent and selective small molecule correctors of Z α1-antitrypsin misfolding.
Liddle J, Pearce AC, Arico-Muendel C, Belyanskaya S, Brewster A, Brown M, Chung CW, Denis A, Dodic N, Dossang A, Eddershaw P, Klimaszewska D, Haq I, Holmes DS, Jagger A, Jakhria T, Jigorel E, Lind K, Messer J, Neu M, Olszewski A, Ronzoni R, Rowedder J, Rüdiger M, Skinner S, Smith KJ, Trottet L, Uings I, Zhu Z, Irving JA, Lomas DA. Liddle J, et al. Among authors: belyanskaya s. Bioorg Med Chem Lett. 2021 Jun 1;41:127973. doi: 10.1016/j.bmcl.2021.127973. Epub 2021 Mar 19. Bioorg Med Chem Lett. 2021. PMID: 33753261
Development of a small molecule that corrects misfolding and increases secretion of Z α1 -antitrypsin.
Lomas DA, Irving JA, Arico-Muendel C, Belyanskaya S, Brewster A, Brown M, Chung CW, Dave H, Denis A, Dodic N, Dossang A, Eddershaw P, Klimaszewska D, Haq I, Holmes DS, Hutchinson JP, Jagger AM, Jakhria T, Jigorel E, Liddle J, Lind K, Marciniak SJ, Messer J, Neu M, Olszewski A, Ordonez A, Ronzoni R, Rowedder J, Rüdiger M, Skinner S, Smith KJ, Terry R, Trottet L, Uings I, Wilson S, Zhu Z, Pearce AC. Lomas DA, et al. Among authors: belyanskaya s. EMBO Mol Med. 2021 Mar 5;13(3):e13167. doi: 10.15252/emmm.202013167. Epub 2021 Jan 29. EMBO Mol Med. 2021. PMID: 33512066 Free PMC article.
Discovery and Optimization of Potent, Selective, and in Vivo Efficacious 2-Aryl Benzimidazole BCATm Inhibitors.
Deng H, Zhou J, Sundersingh F, Messer JA, Somers DO, Ajakane M, Arico-Muendel CC, Beljean A, Belyanskaya SL, Bingham R, Blazensky E, Boullay AB, Boursier E, Chai J, Carter P, Chung CW, Daugan A, Ding Y, Herry K, Hobbs C, Humphries E, Kollmann C, Nguyen VL, Nicodeme E, Smith SE, Dodic N, Ancellin N. Deng H, et al. ACS Med Chem Lett. 2016 Feb 8;7(4):379-84. doi: 10.1021/acsmedchemlett.5b00389. eCollection 2016 Apr 14. ACS Med Chem Lett. 2016. PMID: 27096045 Free PMC article.
Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library.
Deng H, Zhou J, Sundersingh FS, Summerfield J, Somers D, Messer JA, Satz AL, Ancellin N, Arico-Muendel CC, Sargent Bedard KL, Beljean A, Belyanskaya SL, Bingham R, Smith SE, Boursier E, Carter P, Centrella PA, Clark MA, Chung CW, Davie CP, Delorey JL, Ding Y, Franklin GJ, Grady LC, Herry K, Hobbs C, Kollmann CS, Morgan BA, Pothier Kaushansky LJ, Zhou Q. Deng H, et al. Among authors: belyanskaya sl. ACS Med Chem Lett. 2015 Jul 21;6(8):919-24. doi: 10.1021/acsmedchemlett.5b00179. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288694 Free PMC article.
Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT).
Deng H, O'Keefe H, Davie CP, Lind KE, Acharya RA, Franklin GJ, Larkin J, Matico R, Neeb M, Thompson MM, Lohr T, Gross JW, Centrella PA, O'Donovan GK, Bedard KL, van Vloten K, Mataruse S, Skinner SR, Belyanskaya SL, Carpenter TY, Shearer TW, Clark MA, Cuozzo JW, Arico-Muendel CC, Morgan BA. Deng H, et al. Among authors: belyanskaya sl. J Med Chem. 2012 Aug 23;55(16):7061-79. doi: 10.1021/jm300449x. Epub 2012 Aug 14. J Med Chem. 2012. PMID: 22891645
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.
Gentile G, Merlo G, Pozzan A, Bernasconi G, Bax B, Bamborough P, Bridges A, Carter P, Neu M, Yao G, Brough C, Cutler G, Coffin A, Belyanskaya S. Gentile G, et al. Among authors: belyanskaya s. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1989-94. doi: 10.1016/j.bmcl.2012.01.034. Epub 2012 Jan 21. Bioorg Med Chem Lett. 2012. PMID: 22310227
22 results