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Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design.

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Title: Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design.
Authors: Alleyne C; Discovery Pharmaceutical Sciences, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Amin RP; Safety Assessment, Merck & Comapny, Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States., Bhatt B; Safety Assessment, Merck & Comapny, Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States., Bianchi E; IRBM S.p.A., Via Pontina km 30600, Pomezia, Rome 00071, Italy., Blain JC; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States., Boyer N; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States., Branca D; IRBM S.p.A., Via Pontina km 30600, Pomezia, Rome 00071, Italy., Embrey MW; Departments of Medicinal Chemistry, Merck & Company, Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States., Ha SN; Modeling and Informatics, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Jette K; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States., Johns DG; Discovery Biology, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Kerekes AD; Departments of Medicinal Chemistry, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Koeplinger KA; Pharmacokinetics Pharmacodynamics and Drug Metabolism, Merck & Company, Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States., LaPlaca D; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States., Li N; Safety Assessment, Merck & Comapny, Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States., Murphy B; Discovery Biology, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Orth P; Structural Sciences, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Ricardo A; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States., Salowe S; Discovery Biology, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Seyb K; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States., Shahripour A; Departments of Medicinal Chemistry, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Stringer JR; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States., Sun Y; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States., Tracy R; Pharmacokinetics Pharmacodynamics and Drug Metabolism, Merck & Company, Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States., Wu C; Departments of Medicinal Chemistry, Merck & Company, Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States., Xiong Y; Departments of Medicinal Chemistry, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Youm H; Departments of Medicinal Chemistry, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Zokian HJ; Discovery Biology, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Tucker TJ; Departments of Medicinal Chemistry, Merck & Company, Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States.
Source: Journal of medicinal chemistry [J Med Chem] 2020 Nov 25; Vol. 63 (22), pp. 13796-13824. Date of Electronic Publication: 2020 Nov 10.
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
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  Data: <searchLink fieldCode="AU" term="%22Alleyne+C%22">Alleyne C</searchLink>; Discovery Pharmaceutical Sciences, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.<br /><searchLink fieldCode="AU" term="%22Amin+RP%22">Amin RP</searchLink>; Safety Assessment, Merck & Comapny, Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States.<br /><searchLink fieldCode="AU" term="%22Bhatt+B%22">Bhatt B</searchLink>; Safety Assessment, Merck & Comapny, Inc., 770 Sumneytown Pike, P.O. 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Box 4, West Point, Pennsylvania 19486, United States.<br /><searchLink fieldCode="AU" term="%22Ha+SN%22">Ha SN</searchLink>; Modeling and Informatics, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.<br /><searchLink fieldCode="AU" term="%22Jette+K%22">Jette K</searchLink>; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States.<br /><searchLink fieldCode="AU" term="%22Johns+DG%22">Johns DG</searchLink>; Discovery Biology, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.<br /><searchLink fieldCode="AU" term="%22Kerekes+AD%22">Kerekes AD</searchLink>; Departments of Medicinal Chemistry, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.<br /><searchLink fieldCode="AU" term="%22Koeplinger+KA%22">Koeplinger KA</searchLink>; Pharmacokinetics Pharmacodynamics and Drug Metabolism, Merck & Company, Inc., 770 Sumneytown Pike, P.O. 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Box 4, West Point, Pennsylvania 19486, United States.<br /><searchLink fieldCode="AU" term="%22Murphy+B%22">Murphy B</searchLink>; Discovery Biology, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.<br /><searchLink fieldCode="AU" term="%22Orth+P%22">Orth P</searchLink>; Structural Sciences, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.<br /><searchLink fieldCode="AU" term="%22Ricardo+A%22">Ricardo A</searchLink>; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States.<br /><searchLink fieldCode="AU" term="%22Salowe+S%22">Salowe S</searchLink>; Discovery Biology, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.<br /><searchLink fieldCode="AU" term="%22Seyb+K%22">Seyb K</searchLink>; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States.<br /><searchLink fieldCode="AU" term="%22Shahripour+A%22">Shahripour A</searchLink>; Departments of Medicinal Chemistry, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.<br /><searchLink fieldCode="AU" term="%22Stringer+JR%22">Stringer JR</searchLink>; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States.<br /><searchLink fieldCode="AU" term="%22Sun+Y%22">Sun Y</searchLink>; UCB Ra Pharma, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States.<br /><searchLink fieldCode="AU" term="%22Tracy+R%22">Tracy R</searchLink>; Pharmacokinetics Pharmacodynamics and Drug Metabolism, Merck & Company, Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States.<br /><searchLink fieldCode="AU" term="%22Wu+C%22">Wu C</searchLink>; Departments of Medicinal Chemistry, Merck & Company, Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States.<br /><searchLink fieldCode="AU" term="%22Xiong+Y%22">Xiong Y</searchLink>; Departments of Medicinal Chemistry, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.<br /><searchLink fieldCode="AU" term="%22Youm+H%22">Youm H</searchLink>; Departments of Medicinal Chemistry, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.<br /><searchLink fieldCode="AU" term="%22Zokian+HJ%22">Zokian HJ</searchLink>; Discovery Biology, Merck & Company, Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.<br /><searchLink fieldCode="AU" term="%22Tucker+TJ%22">Tucker TJ</searchLink>; Departments of Medicinal Chemistry, Merck & Company, Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States.
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  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2020 Nov 25; Vol. 63 (22), pp. 13796-13824. <i>Date of Electronic Publication: </i>2020 Nov 10.
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