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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: ha sn. 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.
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. Among authors: ha sn. 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
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. Among authors: ha sn. 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
From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9.
Petrilli WL, Adam GC, Erdmann RS, Abeywickrema P, Agnani V, Ai X, Baysarowich J, Byrne N, Caldwell JP, Chang W, DiNunzio E, Feng Z, Ford R, Ha S, Huang Y, Hubbard B, Johnston JM, Kavana M, Lisnock JM, Liang R, Lu J, Lu Z, Meng J, Orth P, Palyha O, Parthasarathy G, Salowe SP, Sharma S, Shipman J, Soisson SM, Strack AM, Youm H, Zhao K, Zink DL, Zokian H, Addona GH, Akinsanya K, Tata JR, Xiong Y, Imbriglio JE. Petrilli WL, et al. Cell Chem Biol. 2020 Jan 16;27(1):32-40.e3. doi: 10.1016/j.chembiol.2019.10.002. Epub 2019 Oct 22. Cell Chem Biol. 2020. PMID: 31653597 Free article.
Discovery and Structure-Based Design of Macrocyclic Peptides Targeting STUB1.
Ng S, Brueckner AC, Bahmanjah S, Deng Q, Johnston JM, Ge L, Duggal R, Habulihaz B, Barlock B, Ha S, Sadruddin A, Yeo C, Strickland C, Peier A, Henry B, Sherer EC, Partridge AW. Ng S, et al. J Med Chem. 2022 Jul 19. doi: 10.1021/acs.jmedchem.2c00406. Online ahead of print. J Med Chem. 2022. PMID: 35853179
Synthesis and biological evaluation of platensimycin analogs.
Shen HC, Ding FX, Singh SB, Parthasarathy G, Soisson SM, Ha SN, Chen X, Kodali S, Wang J, Dorso K, Tata JR, Hammond ML, Maccoss M, Colletti SL. Shen HC, et al. Among authors: ha sn. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1623-7. doi: 10.1016/j.bmcl.2009.02.006. Epub 2009 Feb 7. Bioorg Med Chem Lett. 2009. PMID: 19233644
A proprotein convertase subtilisin-like/kexin type 9 (PCSK9) C-terminal domain antibody antigen-binding fragment inhibits PCSK9 internalization and restores low density lipoprotein uptake.
Ni YG, Condra JH, Orsatti L, Shen X, Di Marco S, Pandit S, Bottomley MJ, Ruggeri L, Cummings RT, Cubbon RM, Santoro JC, Ehrhardt A, Lewis D, Fisher TS, Ha S, Njimoluh L, Wood DD, Hammond HA, Wisniewski D, Volpari C, Noto A, Lo Surdo P, Hubbard B, Carfí A, Sitlani A. Ni YG, et al. J Biol Chem. 2010 Apr 23;285(17):12882-91. doi: 10.1074/jbc.M110.113035. Epub 2010 Feb 19. J Biol Chem. 2010. PMID: 20172854 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. 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
From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9.
Petrilli WL, Adam GC, Erdmann RS, Abeywickrema P, Agnani V, Ai X, Baysarowich J, Byrne N, Caldwell JP, Chang W, DiNunzio E, Feng Z, Ford R, Ha S, Huang Y, Hubbard B, Johnston JM, Kavana M, Lisnock JM, Liang R, Lu J, Lu Z, Meng J, Orth P, Palyha O, Parthasarathy G, Salowe SP, Sharma S, Shipman J, Soisson SM, Strack A, Youm H, Zhao K, Zink DL, Zokian H, Addona GH, Akinsanya K, Tata JR, Xiong Y, Imbriglio JE. Petrilli WL, et al. Cell Chem Biol. 2021 Feb 18;28(2):243. doi: 10.1016/j.chembiol.2021.01.019. Cell Chem Biol. 2021. PMID: 33607006 Free article. No abstract available.
45 results