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

Douglas G JohnsLouis-Charles CampeauPuja BankaAn BautmansTjerk BuetersElisabetta BianchiDanila BrancaPaul G BulgerInne CrevecoeurFa-Xiang DingRobert M GarbaccioErik D GuetschowYan GuoSookhee N HaJennifer M JohnstonHubert JosienEunkyung A KauhKenneth A KoeplingerJeffrey T KuetheEseng LaiChristine L LanningAnita Y H LeeLi LiAnilkumar G NairEdward A O'NeillS Aubrey StochDavid A ThaisrivongsThomas J TuckerPetr VachalKristien van DyckFrederic P VanhoutteBram VolckaertDennis G WolfordAndy XuTian ZhaoDan ZhouSusan ZhouXiaohong ZhuHratch J ZokianAbbas WaljiHarold B Wood
Published in: Circulation (2023)
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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