Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor.

Douglas G Johns,Louis-Charles Campeau,Puja Banka,An Bautmans,Tjerk Bueters,Elisabetta Bianchi,Danila Branca,Paul G Bulger, Inne Crevecoeur,Fa-Xiang Ding,Robert M Garbaccio,Erik D Guetschow, Yan Guo,Sookhee N Ha,Jennifer M Johnston, Hubert Josien,Eunkyung A Kauh,Kenneth A Koeplinger,Jeffrey T Kuethe,Eseng Lai, Christine L Lanning,Anita Y H Lee,Li Li, Anilkumar G Nair, Edward A O'Neill,S Aubrey Stoch,David A Thaisrivongs,Thomas J Tucker,Petr Vachal,Kristien van Dyck,Frederic P Vanhoutte,Bram Volckaert,Dennis G Wolford, Andy Xu,Tian Zhao, Dan Zhou,Susan Zhou,Xiaohong Zhu,Hratch J Zokian,Abbas Walji,Harold B Wood

Circulation（2023）

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摘要

This work validates the use of mRNA display technology for identification of novel oral therapeutic agents, exemplified by the identification of an oral PCSK9 inhibitor, which has the potential to be a highly effective cholesterol lowering therapy for patients in need.

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关键词

bioavailable macrocyclic peptide,low density lipoprotein receptor,pcsk9

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