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Discovery of cell active macrocyclic peptides with on-target inhibition of KRAS signaling.
Lim S, Boyer N, Boo N, Huang C, Venkatachalam G, Angela Juang YC, Garrigou M, Kaan HYK, Duggal R, Peh KM, Sadruddin A, Gopal P, Yuen TY, Ng S, Kannan S, Brown CJ, Verma CS, Orth P, Peier A, Ge L, Yu X, Bhatt B, Chen F, Wang E, Li NJ, Gonzales RJ, Stoeck A, Henry B, Sawyer TK, Lane DP, Johannes CW, Biswas K, Partridge AW. Lim S, et al. Among authors: li nj. Chem Sci. 2021 Nov 25;12(48):15975-15987. doi: 10.1039/d1sc05187c. eCollection 2021 Dec 15. Chem Sci. 2021. PMID: 35024121 Free PMC article.
Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design.
Alleyne C, Amin RP, Bhatt B, Bianchi E, Blain JC, Boyer N, Branca D, Embrey MW, Ha SN, Jette K, Johns DG, Kerekes AD, Koeplinger KA, LaPlaca D, Li N, Murphy B, Orth P, Ricardo A, Salowe S, Seyb K, Shahripour A, Stringer JR, Sun Y, Tracy R, Wu C, Xiong Y, Youm H, Zokian HJ, Tucker TJ. Alleyne C, et al. J Med Chem. 2020 Nov 25;63(22):13796-13824. doi: 10.1021/acs.jmedchem.0c01084. Epub 2020 Nov 10. J Med Chem. 2020. PMID: 33170686
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors.
Tucker TJ, Embrey MW, Alleyne C, Amin RP, Bass A, Bhatt B, Bianchi E, Branca D, Bueters T, Buist N, Ha SN, Hafey M, He H, Higgins J, Johns DG, Kerekes AD, Koeplinger KA, Kuethe JT, Li N, Murphy B, Orth P, Salowe S, Shahripour A, Tracy R, Wang W, Wu C, Xiong Y, Zokian HJ, Wood HB, Walji A. Tucker TJ, et al. J Med Chem. 2021 Nov 25;64(22):16770-16800. doi: 10.1021/acs.jmedchem.1c01599. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34704436
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
Dong S, Zhao Z, Tang H, Li G, Pan J, Gu X, Jiang J, Xiao L, Scapin G, Hunter DN, Yang D, Huang Y, Bennett F, Yang SW, Mandal M, Tang H, Su J, Tudge C, deJesus RK, Ding FX, Lombardo M, Hicks JD, Fischmann T, Mirza A, Dayananth P, Painter RE, Villafania A, Garlisi CG, Zhang R, Mayhood TW, Si Q, Li N, Amin RP, Bhatt B, Chen F, Regan CP, Regan H, Lin X, Wu J, Leithead A, Pollack SR, Scott JD, Nargund RP, Therien AG, Black T, Young K, Pasternak A. Dong S, et al. J Med Chem. 2024 Mar 14;67(5):3400-3418. doi: 10.1021/acs.jmedchem.3c01614. Epub 2024 Feb 22. J Med Chem. 2024. PMID: 38387069
Guiding Chemically Synthesized Peptide Drug Lead Optimization by Derisking Mast Cell Degranulation-Related Toxicities of a NaV1.7 Peptide Inhibitor.
Morissette P, Li N, Ballard JE, Vavrek M, Adams GL, Regan C, Regan H, Lee KJ, Wang W, Burton A, Chen F, Gerenser P, Li Y, Kraus RL, Tellers D, Palani A, Zhu Y, Sun C, Bianchi E, Colarusso S, De Simone D, Frattarelli T, Pasquini NM, Amin RP. Morissette P, et al. Toxicol Sci. 2022 Jan 24;185(2):170-183. doi: 10.1093/toxsci/kfab138. Toxicol Sci. 2022. PMID: 34897513
Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Nav1.7 for the Treatment of Pain.
Adams GL, Pall PS, Grauer SM, Zhou X, Ballard JE, Vavrek M, Kraus RL, Morissette P, Li N, Colarusso S, Bianchi E, Palani A, Klein R, John CT, Wang D, Tudor M, Nolting AF, Biba M, Nowak T, Makarov AA, Reibarkh M, Buevich AV, Zhong W, Regalado EL, Wang X, Gao Q, Shahripour A, Zhu Y, de Simone D, Frattarelli T, Pasquini NM, Magotti P, Iaccarino R, Li Y, Solly K, Lee KJ, Wang W, Chen F, Zeng H, Wang J, Regan H, Amin RP, Regan CP, Burgey CS, Henze DA, Sun C, Tellers DM. Adams GL, et al. J Med Chem. 2022 Jan 13;65(1):485-496. doi: 10.1021/acs.jmedchem.1c01570. Epub 2021 Dec 21. J Med Chem. 2022. PMID: 34931831
66 results