Further LDL cholesterol lowering through targeting PCSK9 for coronary artery disease.
Endocr Metab Immune Disord Drug Targets
; 8(4): 238-43, 2008 Dec.
Article
in En
| MEDLINE
| ID: mdl-19075777
ABSTRACT
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.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Coronary Artery Disease
/
Serine Endopeptidases
/
Cholesterol, LDL
/
Anticholesteremic Agents
Limits:
Animals
/
Humans
Language:
En
Journal:
Endocr Metab Immune Disord Drug Targets
Journal subject:
ALERGIA E IMUNOLOGIA
/
ENDOCRINOLOGIA
/
METABOLISMO
/
TERAPIA POR MEDICAMENTOS
Year:
2008
Document type:
Article
Affiliation country:
United States