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Page 1
A Target Class Ligandability Evaluation of WD40 Repeat-Containing Proteins.
Ackloo S, Li F, Szewczyk M, Seitova A, Loppnau P, Zeng H, Xu J, Ahmad S, Arnautova YA, Baghaie AJ, Beldar S, Bolotokova A, Centrella PA, Chau I, Clark MA, Cuozzo JW, Dehghani-Tafti S, Disch JS, Dong A, Dumas A, Feng JA, Ghiabi P, Gibson E, Gilmer J, Goldman B, Green SR, Guié MA, Guilinger JP, Harms N, Herasymenko O, Houliston S, Hutchinson A, Kearnes S, Keefe AD, Kimani SW, Kramer T, Kutera M, Kwak HA, Lento C, Li Y, Liu J, Loup J, Machado RAC, Mulhern CJ, Perveen S, Righetto GL, Riley P, Shrestha S, Sigel EA, Silva M, Sintchak MD, Slakman BL, Taylor RD, Thompson J, Torng W, Underkoffler C, von Rechenberg M, Walsh RT, Watson I, Wilson DJ, Wolf E, Yadav M, Yazdi AK, Zhang J, Zhang Y, Santhakumar V, Edwards AM, Barsyte-Lovejoy D, Schapira M, Brown PJ, Halabelian L, Arrowsmith CH. Ackloo S, et al. Among authors: chau i. J Med Chem. 2024 Nov 4. doi: 10.1021/acs.jmedchem.4c02010. Online ahead of print. J Med Chem. 2024. PMID: 39495097
Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor.
Shen Y, Li F, Szewczyk MM, Halabelian L, Park KS, Chau I, Dong A, Zeng H, Chen H, Meng F, Barsyte-Lovejoy D, Arrowsmith CH, Brown PJ, Liu J, Vedadi M, Jin J. Shen Y, et al. Among authors: chau i. J Med Chem. 2020 May 28;63(10):5477-5487. doi: 10.1021/acs.jmedchem.0c00406. Epub 2020 May 14. J Med Chem. 2020. PMID: 32367723 Free PMC article.
A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6.
Shen Y, Li F, Szewczyk MM, Halabelian L, Chau I, Eram MS, Dela Seña C, Park KS, Meng F, Chen H, Zeng H, Dong A, Wu H, Trush VV, McLeod D, Zepeda-Velázquez CA, Campbell RM, Mader MM, Watson BM, Schapira M, Arrowsmith CH, Al-Awar R, Barsyte-Lovejoy D, Kaniskan HÜ, Brown PJ, Vedadi M, Jin J. Shen Y, et al. Among authors: chau i. J Med Chem. 2021 Apr 8;64(7):3697-3706. doi: 10.1021/acs.jmedchem.0c02160. Epub 2021 Feb 16. J Med Chem. 2021. PMID: 33591753 Free PMC article.
Subpocket Similarity-Based Hit Identification for Challenging Targets: Application to the WDR Domain of LRRK2.
Eguida M, Bret G, Sindt F, Li F, Chau I, Ackloo S, Arrowsmith C, Bolotokova A, Ghiabi P, Gibson E, Halabelian L, Houliston S, Harding RJ, Hutchinson A, Loppnau P, Perveen S, Seitova A, Zeng H, Schapira M, Rognan D. Eguida M, et al. Among authors: chau i. J Chem Inf Model. 2024 Jul 8;64(13):5344-5355. doi: 10.1021/acs.jcim.4c00601. Epub 2024 Jun 25. J Chem Inf Model. 2024. PMID: 38916159
Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).
Xiong Y, Greschik H, Johansson C, Seifert L, Bacher J, Park KS, Babault N, Martini M, Fagan V, Li F, Chau I, Christott T, Dilworth D, Barsyte-Lovejoy D, Vedadi M, Arrowsmith CH, Brennan P, Fedorov O, Jung M, Farnie G, Liu J, Oppermann U, Schüle R, Jin J. Xiong Y, et al. Among authors: chau i. J Med Chem. 2019 Oct 24;62(20):8996-9007. doi: 10.1021/acs.jmedchem.9b00522. Epub 2019 Jul 24. J Med Chem. 2019. PMID: 31260300
SS148 and WZ16 inhibit the activities of nsp10-nsp16 complexes from all seven human pathogenic coronaviruses.
Li F, Ghiabi P, Hajian T, Klima M, Li ASM, Khalili Yazdi A, Chau I, Loppnau P, Kutera M, Seitova A, Bolotokova A, Hutchinson A, Perveen S, Boura E, Vedadi M. Li F, et al. Among authors: chau i. Biochim Biophys Acta Gen Subj. 2023 Apr;1867(4):130319. doi: 10.1016/j.bbagen.2023.130319. Epub 2023 Feb 9. Biochim Biophys Acta Gen Subj. 2023. PMID: 36764586 Free PMC article.
Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5.
Senisterra G, Wu H, Allali-Hassani A, Wasney GA, Barsyte-Lovejoy D, Dombrovski L, Dong A, Nguyen KT, Smil D, Bolshan Y, Hajian T, He H, Seitova A, Chau I, Li F, Poda G, Couture JF, Brown PJ, Al-Awar R, Schapira M, Arrowsmith CH, Vedadi M. Senisterra G, et al. Among authors: chau i. Biochem J. 2013 Jan 1;449(1):151-9. doi: 10.1042/BJ20121280. Biochem J. 2013. PMID: 22989411 Free PMC article.
Probing the SAM Binding Site of SARS-CoV-2 Nsp14 In Vitro Using SAM Competitive Inhibitors Guides Developing Selective Bisubstrate Inhibitors.
Devkota K, Schapira M, Perveen S, Khalili Yazdi A, Li F, Chau I, Ghiabi P, Hajian T, Loppnau P, Bolotokova A, Satchell KJF, Wang K, Li D, Liu J, Smil D, Luo M, Jin J, Fish PV, Brown PJ, Vedadi M. Devkota K, et al. Among authors: chau i. SLAS Discov. 2021 Oct;26(9):1200-1211. doi: 10.1177/24725552211026261. Epub 2021 Jul 1. SLAS Discov. 2021. PMID: 34192965 Free PMC article.
Trimethylation of histone H3 lysine 36 by human methyltransferase PRDM9 protein.
Eram MS, Bustos SP, Lima-Fernandes E, Siarheyeva A, Senisterra G, Hajian T, Chau I, Duan S, Wu H, Dombrovski L, Schapira M, Arrowsmith CH, Vedadi M. Eram MS, et al. Among authors: chau i. J Biol Chem. 2014 Apr 25;289(17):12177-12188. doi: 10.1074/jbc.M113.523183. Epub 2014 Mar 14. J Biol Chem. 2014. PMID: 24634223 Free PMC article.
426 results