Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a serine protease that belongs to the proprotein convertase family. PCSK9 is synthesized as a zymogen and its prodomain is cleaved by its own catalytic activity. The cleaved prodomain forms a protein complex with the rest of the PCSK9 carboxyl terminus within the endoplasmic reticulum and is secreted. Secreted PCSK9 has been shown to be able to reduce low-density lipoprotein receptor (LDLR) levels in vitro and in vivo. Thus PCSK9 has emerged as an important player modulating LDLR levels and plasma LDL cholesterol. Furthermore, PCSK9 deficiency leads to significantly lowered LDL cholesterol levels in humans and provides dramatic protection against coronary heart disease. We review here the current understanding of PCSK9 and its potential as a therapeutic target through which to reduce LDL cholesterol for prevention and treatment of coronary heart disease.
Keywords: PCSK9, LDL cholesterol, LDL receptor, endocytosis, proprotein convertase
Molecular Mechanisms Regulating mRNA Stability: Physiological and Pathological Significance
Current Genomics Mechanical Support in Cardiogenic Shock Complicating Acute Coronary Syndrome: Ready for Prime Time?
Current Vascular Pharmacology Cardiac Metabolism in Myocardial Ischemia
Current Pharmaceutical Design Inflammatory Arthritis and Heart Disease
Current Pharmaceutical Design BELFAST Centenarians: A Case of Optimal Cardiovascular Risk?
Current Pharmaceutical Design Cardiac Tissue Engineering
Recent Patents on Regenerative Medicine (Discontinued) Synthesis and Investigation of the Role of Benzopyran Dihydropyrimidinone Hybrids in Cell Proliferation, Migration and Tumor Growth
Anti-Cancer Agents in Medicinal Chemistry From CHD Susceptibility Genes to New Therapeutics
Current Pharmacogenomics Essential Fatty Acids - A Review
Current Pharmaceutical Biotechnology Statins as Anti-Inflammatory Agents in Atherogenesis: Molecular Mechanisms and Lessons from the Recent Clinical Trials
Current Pharmaceutical Design Value of Abnormal Fetal Cardiac Axis in the Fetal Congenital Heart Disease
Current Medical Imaging Analysis of Parallel SVM Based Classification Technique on Healthcare using Big Data Management in Cloud Storage
Recent Patents on Computer Science Genetic and Non-Genetic Determinants of the Pharmacological Activity of Statins
Current Drug Metabolism Role of Copper in Angiogenesis and Its Medicinal Implications
Current Medicinal Chemistry Cardiovascular Effects of Phosphodiesterase 5 Inhibitors
Current Pharmaceutical Design Arterial Duct Stenting in Congenital Heart Disease with Duct-Dependent Pulmonary Circulation
Current Pediatric Reviews Blood Pressure and White Matter Lesions in Patients with Vascular Disease: The SMART-MR Study
Current Neurovascular Research P2X Receptors in the Cardiovascular System and their Potential as Therapeutic Targets in Disease
Current Medicinal Chemistry Cytokine Gene Variants as Predictors of Type 2 Diabetes Mellitus
Current Diabetes Reviews Subclinical Thyroid Dysfunction and Cardiovascular Outcomes among Prospective Cohort Studies
Endocrine, Metabolic & Immune Disorders - Drug Targets