World Library  
Flag as Inappropriate
Email this Article

Positive allosteric modulator

Article Id: WHEBN0023047816
Reproduction Date:

Title: Positive allosteric modulator  
Author: World Heritage Encyclopedia
Language: English
Subject: Hypnotic, PAM, GABAA receptor
Collection:
Publisher: World Heritage Encyclopedia
Publication
Date:
 

Positive allosteric modulator

In biochemistry and pharmacology, an allosteric modulator is a substance which indirectly influences (modulates) the effects of an agonist or inverse agonist at a target protein, for example a receptor. Allosteric modulators bind to a site distinct from that of the orthosteric agonist binding site. Usually they induce a conformational change within the protein structure. A positive allosteric modulator (PAM) induces an amplification, a negative modulator (NAM) an attenuation of the effects of the orthosteric ligand without triggering a functional activity on its own in the absence of the orthosteric ligand. Substances that occupy the allosteric binding site and behave functionally neutral are called silent allosteric modulators (SAMs). Classic benzodiazepines are well-known PAMs.

From modulators the allosteric agonists are to be distinguished. They are able to directly activate a receptor via an allosteric binding site in the absence of an orthosteric ligand.

An ago-allosteric modulator both activates and modulates a receptor allosterically.

See also

References

es:Modulador alostérico negativo

sr:Negativni alosterni modulator

This article was sourced from Creative Commons Attribution-ShareAlike License; additional terms may apply. World Heritage Encyclopedia content is assembled from numerous content providers, Open Access Publishing, and in compliance with The Fair Access to Science and Technology Research Act (FASTR), Wikimedia Foundation, Inc., Public Library of Science, The Encyclopedia of Life, Open Book Publishers (OBP), PubMed, U.S. National Library of Medicine, National Center for Biotechnology Information, U.S. National Library of Medicine, National Institutes of Health (NIH), U.S. Department of Health & Human Services, and USA.gov, which sources content from all federal, state, local, tribal, and territorial government publication portals (.gov, .mil, .edu). Funding for USA.gov and content contributors is made possible from the U.S. Congress, E-Government Act of 2002.
 
Crowd sourced content that is contributed to World Heritage Encyclopedia is peer reviewed and edited by our editorial staff to ensure quality scholarly research articles.
 
By using this site, you agree to the Terms of Use and Privacy Policy. World Heritage Encyclopedia™ is a registered trademark of the World Public Library Association, a non-profit organization.
 



Copyright © World Library Foundation. All rights reserved. eBooks from World eBook Library are sponsored by the World Library Foundation,
a 501c(4) Member's Support Non-Profit Organization, and is NOT affiliated with any governmental agency or department.