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

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作者： Douglas G,Johns ^[1] ; Louis-Charles,Campeau ^[1] ; Puja,Banka ^[1] ; An,Bautmans ^[1] ; Tjerk,Bueters ^[1] ; Elisabetta,Bianchi ^[2] ; Danila,Branca ^[2] ; Paul G,Bulger ^[1] ; Inne,Crevecoeur ^[1] ; Fa-Xiang,Ding ^[1] ; Robert M,Garbaccio ^[1] ; Erik D,Guetschow ^[1] ; Yan,Guo ^[3] ; Sookhee N,Ha ^[1] ; Jennifer M,Johnston ^[1] ; Hubert,Josien ^[1] ; Eunkyung A,Kauh ^[1] ; Kenneth A,Koeplinger ^[1] ; Jeffrey T,Kuethe ^[1] ; Eseng,Lai ^[1] ; Christine L,Lanning ^[1] ; Anita Y H,Lee ^[1] ; Li,Li ^[1] ; Anilkumar G,Nair ^[1] ; Edward A,O'Neill ^[1] ; S Aubrey,Stoch ^[1] ; David A,Thaisrivongs ^[1] ; Thomas J,Tucker ^[1] ; Petr,Vachal ^[1] ; Kristien,van Dyck ^[1] ; Frederic P,Vanhoutte ^[1] ; Bram,Volckaert ^[4] ; Dennis G,Wolford ^[4] ; Andy,Xu ^[1] ; Tian,Zhao ^[1] ; Dan,Zhou ^[1] ; Susan,Zhou ^[1] ; Xiaohong,Zhu ^[1] ; Hratch J,Zokian ^[1] ; Abbas M,Walji ^[1] ; Harold B,Wood ^[1]

作者单位： MRL, Merck & Co., Inc., Rahway, NJ (D.G.J., L.-C.C., P.B., A.B., T.B., P.G.B., I.C., F.-X.D., R.M.G., E.D.G., Y.G., S.N.H., J.M.J., H.J., E.A.K., K.A.K., J.T.K., E.L., C.L.L., A.Y.H.L., L.L., A.G.N., E.A.O., S.A.S., D.A.T., T.J.T., P.V., K.v.D., D.G.W., A.X., T.Z., D.Z., S.Z., X.Z., H.J.Z., A.M.W., H.B.W.). ^[1] Peptide & Small Molecules R&D, IRBM S.p.A., Pomezia (RM), Italy (E.B., D.B.). ^[2] Now with Cayman Chemical Company, Ann Arbor, MI (E.D.G.). ^[3] Clinical Pharmacology Unit, SGS Life Sciences, Antwerp, Belgium (F.P.V., B.V.). ^[4]

关键词 PCSK9 inhibitors atherosclerosis cholesterol clinical trial hypercholesterolemia low density lipoprotein mRNA display technology macrocyclic peptide