Discovery of Inhibitors of Insulin-Regulated Aminopeptidase as Cognitive Enhancers
Joint Authors
Hallberg, Mathias
Andersson, Hanna
Source
International Journal of Hypertension
Issue
Vol. 2012, Issue 2012 (31 Dec. 2012), pp.1-18, 18 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2012-12-04
Country of Publication
Egypt
No. of Pages
18
Main Subjects
Abstract EN
The hexapeptide angiotensin IV (Ang IV) is a metabolite of angiotensin II (Ang II) and plays a central role in the brain.
It was reported more than two decades ago that intracerebroventricular injection of Ang IV improved memory and learning in the rat.
Several hypotheses have been put forward to explain the positive effects of Ang IV and related analogues on cognition.
It has been proposed that the insulin-regulated aminopeptidase (IRAP) is the main target of Ang IV.
This paper discusses progress in the discovery of inhibitors of IRAP as potential enhancers of cognitive functions.
Very potent inhibitors of the protease have been synthesised, but pharmacokinetic issues (including problems associated with crossing the blood-brain barrier) remain to be solved.
The paper also briefly presents an overview of the status in the discovery of inhibitors of ACE and renin, and of AT1R antagonists and AT2R agonists, in order to enable other discovery processes within the RAS system to be compared.
The paper focuses on the relationship between binding affinities/inhibition capacity and the structures of the ligands that interact with the target proteins.
American Psychological Association (APA)
Andersson, Hanna& Hallberg, Mathias. 2012. Discovery of Inhibitors of Insulin-Regulated Aminopeptidase as Cognitive Enhancers. International Journal of Hypertension،Vol. 2012, no. 2012, pp.1-18.
https://search.emarefa.net/detail/BIM-498229
Modern Language Association (MLA)
Andersson, Hanna& Hallberg, Mathias. Discovery of Inhibitors of Insulin-Regulated Aminopeptidase as Cognitive Enhancers. International Journal of Hypertension No. 2012 (2012), pp.1-18.
https://search.emarefa.net/detail/BIM-498229
American Medical Association (AMA)
Andersson, Hanna& Hallberg, Mathias. Discovery of Inhibitors of Insulin-Regulated Aminopeptidase as Cognitive Enhancers. International Journal of Hypertension. 2012. Vol. 2012, no. 2012, pp.1-18.
https://search.emarefa.net/detail/BIM-498229
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-498229