Document Detail


Inhibition of renin: an updated review of the development of renin inhibitors.
MedLine Citation:
PMID:  17729187     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
As an important cascade involved in the regulation of blood pressure and volume homeostasis, the renin-angiotensin system (RAS) has been targeted for blood pressure control. In the last decades, the most successful strategy to control the RAS has been the inhibition of the angiotensin-converting enzyme (ACE) and the angiotensin type 1 (AT(1)) receptor. Small-molecule inhibitors targeting these steps have been widely used clinically. However, complete inhibition of the RAS is not achievable by blocking the ACE or the AT(1) because of the compensatory rise in plasma renin activity, which limits the efficacy of many RAS drugs. Direct inhibition of renin, the first and rate-limiting step in the RAS cascade, is the preferred strategy for controlling the RAS, and much progress has been made in the research and development of renin inhibitors. This review covers the evolution of renin inhibitors and discusses the advantages of renin inhibition at the enzymatic and biosynthetic levels for blood pressure control.
Authors:
Yan Chun Li
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Current opinion in investigational drugs (London, England : 2000)     Volume:  8     ISSN:  1472-4472     ISO Abbreviation:  Curr Opin Investig Drugs     Publication Date:  2007 Sep 
Date Detail:
Created Date:  2007-08-30     Completed Date:  2007-10-23     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  100965718     Medline TA:  Curr Opin Investig Drugs     Country:  England    
Other Details:
Languages:  eng     Pagination:  750-7     Citation Subset:  IM    
Affiliation:
The University of Chicago, Department of Medicine, MC 4076, 5841 S Maryland Avenue, Chicago, IL 60637, USA. cyan@medicine.bsd.uchicago.edu
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MeSH Terms
Descriptor/Qualifier:
Amides / pharmacology
Angiotensin II Type 1 Receptor Blockers / pharmacology
Angiotensin-Converting Enzyme Inhibitors / pharmacology
Animals
Antibodies / pharmacology
Antihypertensive Agents / pharmacology*,  therapeutic use
Blood Pressure / drug effects*
Drug Design
Enzyme Inhibitors / pharmacology
Fumarates / pharmacology
Humans
Hypertension / drug therapy*,  metabolism,  physiopathology
Molecular Structure
Peptides / pharmacology
Receptors, Cell Surface / metabolism
Renin / antagonists & inhibitors*,  chemistry,  immunology,  metabolism
Renin-Angiotensin System / drug effects*
Vacuolar Proton-Translocating ATPases / metabolism
Vitamin D / analogs & derivatives,  pharmacology
Chemical
Reg. No./Substance:
0/ATP6AP2 protein, human; 0/Amides; 0/Angiotensin II Type 1 Receptor Blockers; 0/Angiotensin-Converting Enzyme Inhibitors; 0/Antibodies; 0/Antihypertensive Agents; 0/Enzyme Inhibitors; 0/Fumarates; 0/Peptides; 0/Receptors, Cell Surface; 0/aliskiren; 1406-16-2/Vitamin D; EC 3.4.23.15/Renin; EC 3.6.1.-/Vacuolar Proton-Translocating ATPases

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