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Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor.
Johns DG, Campeau LC, Banka P, Bautmans A, Bueters T, Bianchi E, Branca D, Bulger PG, Crevecoeur I, Ding FX, Garbaccio RM, Guetschow ED, Guo Y, Ha SN, Johnston JM, Josien H, Kauh EA, Koeplinger KA, Kuethe JT, Lai E, Lanning CL, Lee AYH, Li L, Nair AG, O'Neill EA, Stoch SA, Thaisrivongs DA, Tucker TJ, Vachal P, van Dyck K, Vanhoutte FP, Volckaert B, Wolford DG, Xu A, Zhao T, Zhou D, Zhou S, Zhu X, Zokian HJ, Walji AM, Wood HB. Johns DG, et al. Among authors: nair ag. Circulation. 2023 Jul 11;148(2):144-158. doi: 10.1161/CIRCULATIONAHA.122.063372. Epub 2023 May 1. Circulation. 2023. PMID: 37125593 Free PMC article.
Discovery of potent macrocyclic HCV NS5A inhibitors.
Yu W, Vibulbhan B, Rosenblum SB, Martin GS, Vellekoop AS, Holst CL, Coburn CA, Wong M, Selyutin O, Ji T, Zhong B, Hu B, Chen L, Dwyer MP, Jiang Y, Nair AG, Tong L, Zeng Q, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Fells J, Kozlowski JA. Yu W, et al. Among authors: nair ag. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3793-9. doi: 10.1016/j.bmcl.2016.05.042. Epub 2016 May 17. Bioorg Med Chem Lett. 2016. PMID: 27282743
MK-8325: A silyl proline-containing NS5A inhibitor with pan-genotype activity for treatment of HCV.
Nair AG, Zeng Q, Selyutin O, Rosenblum SB, Jiang Y, Yang DY, Keertikar K, Zhou G, Dwyer M, Kim SH, Shankar B, Yu W, Tong L, Chen L, Mazzola R, Caldwell J, Tang H, Agrawal S, Liu R, Kong R, Ingravallo P, Xia E, Zhai Y, Nomeir A, Asante-Appiah E, Kozlowski JA. Nair AG, et al. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1954-1957. doi: 10.1016/j.bmcl.2018.03.049. Epub 2018 Mar 20. Bioorg Med Chem Lett. 2018. PMID: 29653894
Discovery of novel tricyclic indole derived inhibitors of HCV NS5B RNA dependent RNA polymerase.
Venkatraman S, Velazquez F, Gavalas S, Wu W, Chen KX, Nair AG, Bennett F, Huang Y, Pinto P, Jiang Y, Selyutin O, Vibulbhan B, Zeng Q, Lesburg C, Duca J, Huang HC, Agrawal S, Jiang CK, Ferrari E, Li C, Kozlowski J, Rosenblum S, Shih NY, Njoroge FG. Venkatraman S, et al. Among authors: nair ag. Bioorg Med Chem. 2013 Apr 1;21(7):2007-17. doi: 10.1016/j.bmc.2013.01.024. Epub 2013 Jan 23. Bioorg Med Chem. 2013. PMID: 23434368
Alkyl substituted aminal derivatives of HCV NS5A inhibitor MK-8742.
Yu W, Coburn CA, Nair AG, Wong M, Tong L, Dwyer MP, Hu B, Zhong B, Hao J, Yang DY, Selyutin O, Jiang Y, Rosenblum SB, Kim SH, Lavey BJ, Zhou G, Rizvi R, Shankar BB, Zeng Q, Chen L, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Nomeir A, Kozlowski JA. Yu W, et al. Among authors: nair ag. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3800-5. doi: 10.1016/j.bmcl.2016.05.041. Epub 2016 May 14. Bioorg Med Chem Lett. 2016. PMID: 27282742
Alternative core development around the tetracyclic indole class of HCV NS5A inhibitors.
Tong L, Yu W, Coburn CA, Meinke PT, Nair AG, Dwyer MP, Chen L, Selyutin O, Rosenblum SB, Jiang Y, Fells J, Hu B, Zhong B, Soll RM, Liu R, Agrawal S, Xia E, Zhai Y, Kong R, Ingravallo P, Nomeir A, Asante-Appiah E, Kozlowski JA. Tong L, et al. Among authors: nair ag. Bioorg Med Chem Lett. 2016 Oct 15;26(20):5132-5137. doi: 10.1016/j.bmcl.2016.07.057. Epub 2016 Jul 25. Bioorg Med Chem Lett. 2016. PMID: 27634194 Free article.
Structure-activity relationships of proline modifications around the tetracyclic-indole class of NS5A inhibitors.
Tong L, Yu W, Coburn CA, Chen L, Selyutin O, Zeng Q, Dwyer MP, Nair AG, Shankar BB, Kim SH, Yang DY, Rosenblum SB, Ruck RT, Davies IW, Hu B, Zhong B, Hao J, Ji T, Zan S, Liu R, Agrawal S, Carr D, Curry S, McMonagle P, Bystol K, Lahser F, Ingravallo P, Chen S, Asante-Appiah E, Kozlowski JA. Tong L, et al. Among authors: nair ag. Bioorg Med Chem Lett. 2016 Nov 1;26(21):5354-5360. doi: 10.1016/j.bmcl.2016.08.097. Epub 2016 Sep 2. Bioorg Med Chem Lett. 2016. PMID: 27680588
Discovery of fused tricyclic core containing HCV NS5A inhibitors with pan-genotype activity.
Yu W, Coburn CA, Yang DY, Meinke PT, Wong M, Rosenblum SB, Chen KX, Njoroge GF, Chen L, Dwyer MP, Jiang Y, Nair AG, Selyutin O, Tong L, Zeng Q, Zhong B, Ji T, Hu B, Agrawal S, Xia E, Zhai Y, Liu R, Kong R, Ingravallo P, Asante-Appiah E, Nomeir A, Fells J, Kozlowski JA. Yu W, et al. Among authors: nair ag. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3158-3162. doi: 10.1016/j.bmcl.2016.04.084. Epub 2016 Apr 30. Bioorg Med Chem Lett. 2016. PMID: 27180013
Discovery of an irreversible HCV NS5B polymerase inhibitor.
Zeng Q, Nair AG, Rosenblum SB, Huang HC, Lesburg CA, Jiang Y, Selyutin O, Chan TY, Bennett F, Chen KX, Venkatraman S, Sannigrahi M, Velazquez F, Duca JS, Gavalas S, Huang Y, Pu H, Wang L, Pinto P, Vibulbhan B, Agrawal S, Ferrari E, Jiang CK, Li C, Hesk D, Gesell J, Sorota S, Shih NY, Njoroge FG, Kozlowski JA. Zeng Q, et al. Among authors: nair ag. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6585-7. doi: 10.1016/j.bmcl.2013.10.060. Epub 2013 Nov 6. Bioorg Med Chem Lett. 2013. PMID: 24252545
Aryl or heteroaryl substituted aminal derivatives of HCV NS5A inhibitor MK-8742.
Yu W, Coburn CA, Nair AG, Wong M, Rosenblum SB, Zhou G, Dwyer MP, Tong L, Hu B, Zhong B, Hao J, Ji T, Zan S, Kim SH, Zeng Q, Selyutin O, Chen L, Masse F, Agrawal S, Liu R, Xia E, Zhai Y, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Lin M, Kozlowski JA. Yu W, et al. Among authors: nair ag. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3414-20. doi: 10.1016/j.bmcl.2016.06.056. Epub 2016 Jun 22. Bioorg Med Chem Lett. 2016. PMID: 27394665
198 results