Published May 2019 | Version v1
Journal article

Emerging role of proprotein convertase subtilisin/kexin type-9 (PCSK-9) in inflammation and diseases

  • 1. Department of Pharmaceutical Sciences, Washington State University College of Pharmacy, Spokane, WA (United States)
  • 2. Division of Rheumatology, University of Washington School of Medicine, Seattle, WA (United States)

Description

Proprotein convertase subtilisin/kexin type-9 (PCSK9) is most recognized serine protease for its role in cardiovascular diseases (CVD). PCSK9 regulates plasma low-density lipoprotein cholesterol (LDL-C) levels by selectively targeting hepatic LDL receptors (LDLR) for degradation, thereby serving as a potential therapeutic target for CVD. New pharmacological agents under development aim to lower the risk of CVD by inhibiting PCSK9 extracellularly, although secondary effects of this approach are not yet studied. Here we review the history of PCSK9 and rationale behind developing inhibitors for CVD. Importantly, we summarized the studies investigating the role and impact of modulated PCSK9 levels in inflammation, specifically in sepsis, rheumatoid arthritis and other chronic inflammatory conditions. Furthermore, we summarized studies that investigated the interactions of PCSK9 with pro-inflammatory pathways, such as scavenger receptor CD36 and thrombospondin 1 (TSP-1) in inflammatory diseases. This review highlights the conflicting role that PCSK9 plays in different inflammatory disease states and postulates that any unwanted effects of PCSK9 inhibition in early clinical testing should critically be examined.

Additional details

Identifiers

DOI
10.1016/j.taap.2019.03.018;
PII
S0041008X19301085;

Publishing Information

Journal Title
Toxicology and Applied Pharmacology
Journal Volume
370
Journal Page Range
p. 170-177
ISSN
0041-008X
CODEN
TXAPA9

Optional Information

Copyright
Copyright (c) 2019 Elsevier Inc. All rights reserved.