Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents-Reference-Cited by-同舟云学术

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

Published:2018-06-07 Issue:13 Volume:61 Page:5704-5718
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Londregan Allyn T.¹,Wei Liuqing¹,Xiao Jun¹,Lintner Nathanael G.²,Petersen Donna³,Dullea Robert G.⁴,McClure Kim F.⁵,Bolt Michael W.⁶,Warmus Joseph S.¹,Coffey Steven B.¹,Limberakis Chris¹,Genovino Julien¹^ORCID,Thuma Benjamin A.¹,Hesp Kevin D.¹,Aspnes Gary E.⁵,Reidich Benjamin⁴,Salatto Christopher T.⁴,Chabot Jeffrey R.⁷,Cate Jamie H. D.²⁸⁹¹⁰^ORCID,Liras Spiros⁵,Piotrowski David W.¹^ORCID

Affiliation:

1. Pfizer Medicinal Chemistry, Groton, Connecticut 06340, United States

2. Department of Molecular and Cell Biology, University of California, Berkeley, Berkeley, California 94720, United States

3. Primary Pharmacology Group, Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research and Development, Groton, Connecticut 06340, United States

4. Internal Medicine Research Unit, Pfizer Worldwide Research and Development, Cambridge, Massachusetts 02139, United States

5. Pfizer Medicinal Chemistry, Internal Medicine Research Unit, Pfizer Worldwide Research and Development, Cambridge, Massachusetts 02139, United States

6. Drug Safety Research & Development, Pfizer Worldwide Research & Development, Cambridge, Massachusetts 02139, United States

7. Pfizer Pharmacokinetics, Dynamics and Metabolism Modeling and Simulation, Pfizer Worldwide Research and Development, Cambridge, Massachusetts 02139, United States

8. QB3 Institute, University of California, Berkeley, Berkeley, California 94720, United States

9. Department of Chemistry, University of California, Berkeley, Berkeley, California 94720, United States

10. Physical Biosciences Division, Lawrence Berkeley National Laboratory, Berkeley, California 94720, United States

Funder

Pfizer

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.8b00650

Reference36 articles.

1. Post-transcriptional Regulation of Low Density Lipoprotein Receptor Protein by Proprotein Convertase Subtilisin/Kexin Type 9a in Mouse Liver

2. Structural and biophysical studies of PCSK9 and its mutants linked to familial hypercholesterolemia

3. The Crystal Structure of PCSK9: A Regulator of Plasma LDL-Cholesterol

4. Mechanistic implications for LDL receptor degradation from the PCSK9/LDLR structure at neutral pH

5. Binding of Proprotein Convertase Subtilisin/Kexin Type 9 to Epidermal Growth Factor-like Repeat A of Low Density Lipoprotein Receptor Decreases Receptor Recycling and Increases Degradation

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