A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors-Reference-Cited by-同舟云学术

A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors

Published:2021-10-27 Issue:22 Volume:64 Page:16770-16800
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Tucker Thomas J.¹^ORCID,Embrey Mark W.¹,Alleyne Candice²,Amin Rupesh P.³,Bass Alan³,Bhatt Bhavana³,Bianchi Elisabetta⁴^ORCID,Branca Danila⁴,Bueters Tjerk⁵,Buist Nicole²,Ha Sookhee N.⁶,Hafey Mike⁵,He Huaibing⁵,Higgins John²,Johns Douglas G.⁷,Kerekes Angela D.⁸,Koeplinger Kenneth A.⁵,Kuethe Jeffrey T.⁹,Li Nianyu³,Murphy BethAnn⁷,Orth Peter¹⁰,Salowe Scott⁷,Shahripour Aurash⁸,Tracy Rodger⁵,Wang Weixun⁵,Wu Chengwei¹,Xiong Yusheng⁸,Zokian Hratch J.⁷,Wood Harold B.⁸,Walji Abbas⁸

Affiliation:

1. Department of Medicinal Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486 United States

2. Department of Discovery Pharmaceutical Sciences, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 United States

3. Department of Safety Assessment and Laboratory Animal Resources, Merck & Co., Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486 United States

4. Peptides and Small Molecule Research and Development Department, IRBM S.p.A., Via Pontina km 30600, 00071 Pomezia (RM), Italy

5. Department of Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, Merck & Co., Inc., 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486 United States

6. Department of Modeling and Informatics, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 United States

7. Department of Discovery Biology, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 United States

8. Department of Medicinal Chemistry, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 United States

9. Department of Process Chemistry, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 United States

10. Department of Structural Sciences, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 United States

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.1c01599

Reference37 articles.

1. PCSK9

2. A Systematic Review of PCSK9 Inhibitors Alirocumab and Evolocumab

3. Small Molecule Inhibitors of the PCSK9·LDLR Interaction

4. Disrupting the PCSK9/LDLR protein–protein interaction by an imidazole-based minimalist peptidomimetic

5. Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents

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