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Incorporation of Putative Helix-Breaking Amino Acids in the Design of Novel Stapled Peptides: Exploring Biophysical and Cellular Permeability Properties.
Partridge AW, Kaan HYK, Juang YC, Sadruddin A, Lim S, Brown CJ, Ng S, Thean D, Ferrer F, Johannes C, Yuen TY, Kannan S, Aronica P, Tan YS, Pradhan MR, Verma CS, Hochman J, Chen S, Wan H, Ha S, Sherborne B, Lane DP, Sawyer TK. Partridge AW, et al. Among authors: chen s. Molecules. 2019 Jun 20;24(12):2292. doi: 10.3390/molecules24122292. Molecules. 2019. PMID: 31226791 Free PMC article.
Macrocyclic α helical peptide therapeutic modality: A perspective of learnings and challenges.
Sawyer TK, Partridge AW, Kaan HYK, Juang YC, Lim S, Johannes C, Yuen TY, Verma C, Kannan S, Aronica P, Tan YS, Sherborne B, Ha S, Hochman J, Chen S, Surdi L, Peier A, Sauvagnat B, Dandliker PJ, Brown CJ, Ng S, Ferrer F, Lane DP. Sawyer TK, et al. Among authors: chen s. Bioorg Med Chem. 2018 Jun 1;26(10):2807-2815. doi: 10.1016/j.bmc.2018.03.008. Epub 2018 Mar 16. Bioorg Med Chem. 2018. PMID: 29598901
Macrocyclization of an all-d linear α-helical peptide imparts cellular permeability.
Kannan S, Aronica PGA, Ng S, Gek Lian DT, Frosi Y, Chee S, Shimin J, Yuen TY, Sadruddin A, Kaan HYK, Chandramohan A, Wong JH, Tan YS, Chang ZW, Ferrer-Gago FJ, Arumugam P, Han Y, Chen S, Rénia L, Brown CJ, Johannes CW, Henry B, Lane DP, Sawyer TK, Verma CS, Partridge AW. Kannan S, et al. Among authors: chen s. Chem Sci. 2020 May 11;11(21):5577-5591. doi: 10.1039/c9sc06383h. eCollection 2020 Jun 7. Chem Sci. 2020. PMID: 32874502 Free PMC article.
2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.
Dai C, Li D, Popovici-Muller J, Zhao L, Girijavallabhan VM, Rosner KE, Lavey BJ, Rizvi R, Shankar BB, Wong MK, Guo Z, Orth P, Strickland CO, Sun J, Niu X, Chen S, Kozlowski JA, Lundell DJ, Piwinski JJ, Shih NY, Siddiqui MA. Dai C, et al. Among authors: chen s. Bioorg Med Chem Lett. 2011 May 15;21(10):3172-6. doi: 10.1016/j.bmcl.2011.01.002. Epub 2011 Jan 6. Bioorg Med Chem Lett. 2011. PMID: 21458257
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: chen l, chen s. 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
Development of a prodrug of hydantoin based TACE inhibitor.
Tong L, Kim SH, Chen L, Kosinski A, Shankar BB, Girijavallabhan V, Yang DY, Yu W, Zhou G, Shih NY, Chen S, Hu M, Lundell D, Niu X, Umland S, Kozlowski JA. Tong L, et al. Among authors: chen l, chen s. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3704-3708. doi: 10.1016/j.bmcl.2017.07.007. Epub 2017 Jul 3. Bioorg Med Chem Lett. 2017. PMID: 28711352
Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors.
Tong L, Kim SH, Rosner K, Yu W, Shankar BB, Chen L, Li D, Dai C, Girijavallabhan V, Popovici-Muller J, Yang L, Zhou G, Kosinski A, Siddiqui MA, Shih NY, Guo Z, Orth P, Chen S, Lundell D, Niu X, Umland S, Kozlowski JA. Tong L, et al. Among authors: chen l, chen s. Bioorg Med Chem Lett. 2017 Jul 15;27(14):3037-3042. doi: 10.1016/j.bmcl.2017.05.062. Epub 2017 May 22. Bioorg Med Chem Lett. 2017. PMID: 28558971
Structure and activity relationships of tartrate-based TACE inhibitors.
Li D, Popovici-Muller J, Belanger DB, Caldwell J, Dai C, David M, Girijavallabhan VM, Lavey BJ, Lee JF, Liu Z, Mazzola R, Rizvi R, Rosner KE, Shankar B, Spitler J, Ting PC, Vaccaro H, Yu W, Zhou G, Zhu Z, Niu X, Sun J, Guo Z, Orth P, Chen S, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Shipps GW Jr, Siddiqui MA, Strickland CO. Li D, et al. Among authors: chen s. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4812-5. doi: 10.1016/j.bmcl.2010.06.104. Epub 2010 Jun 25. Bioorg Med Chem Lett. 2010. PMID: 20638281
Discovery of Chromane Containing Hepatitis C Virus (HCV) NS5A Inhibitors with Improved Potency against Resistance-Associated Variants.
Yu W, Tong L, Hu B, Zhong B, Hao J, Ji T, Zan S, Coburn CA, Selyutin O, Chen L, Rokosz L, Agrawal S, Liu R, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Chen S, Kozlowski JA. Yu W, et al. Among authors: chen l, chen s. J Med Chem. 2016 Nov 23;59(22):10228-10243. doi: 10.1021/acs.jmedchem.6b01234. Epub 2016 Nov 9. J Med Chem. 2016. PMID: 27792320
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