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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Shen, Li Peng, Hongchun Xu, Danyan Zhao, Shuiping |
| Description | Author Affiliation: Shen L ( Department of Cardiology, Second Xiangya Hospital, Central South University, Changsha 410011, PR China.) |
| Abstract | Proprotein convertase subtilisin/kexin 9 (PCSK9) has been shown to degrade hepatic low-density lipoprotein receptors (LDLR). Gain-of-function mutations promote the development of familial hypercholesterolemia, whereas loss-of-function mutations are associated with lower levels of circulating low-density lipoprotein cholesterol (LDL-C) and significant protection against coronary heart disease. The major classes of commonly prescribed lipid-lowering medications, such as statins, increase serum PCSK9 levels, thus PCSK9 inhibition would increase the efficacy of statins on LDL-C lowering. Therefore, PCSK9 is an attractive therapeutic target for the new generation of cholesterol-lowering drugs. Here, we present a brief overview of the development of PCSK9 inhibitors and highlight the effect of currently prescribed LDL-C-lowering drugs on PCSK9, and the strategies that are being explored for its therapeutic inhibition. Current research and clinical trial results indicate that a PCSK9 inhibitor may be an exciting new therapeutic drug for the treatment of dyslipidemia and relevant cardiovascular diseases. |
| File Format | HTM / HTML |
| ISSN | 10436618 |
| Volume Number | 73 |
| e-ISSN | 10961186 |
| Journal | Pharmacological Research |
| Language | English |
| Publisher | Elsevier |
| Publisher Date | 2013-07-01 |
| Publisher Place | Netherlands |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Pharmacology Anticholesteremic Agents Therapeutic Use Hypercholesterolemia Drug Therapy Proprotein Convertases Antagonists & Inhibitors Serine Proteinase Inhibitors Animals Cholesterol, Ldl Blood Humans Genetics Mutation Physiology Serine Endopeptidases Journal Article Research Support, Non-u.s. Gov't Review |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology |
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