Synthesis of potential potent antagonist of G-Protein coupled receptors

UNCG Author/Contributor (non-UNCG co-authors, if there are any, appear on document)
Sommayah Sayed (Creator)
The University of North Carolina at Greensboro (UNCG )
Web Site:
Mitchell Croatt

Abstract: GPR55, is a G-protein coupled receptor (GPCR), that was first discovered in 1990 and deorphanized in 2006. The homology model of the receptor in the active and inactive state is based off of the ß – adrenergic receptor. A potent agonist of GPR55 is the endogenous LPI and one antagonist is ML192. Due to the biological diseases associated with GPR55 a more potent antagonist or agonist is needed that can deactivate or activate the receptor in order to further elucidate the role and function of GPR55 in the body. The focus of the research presented is to synthesize a variety of analogs of GPR55 with the goal of finding a more potent antagonist then ML192. The analogs that synthesized were subjected to biological assay testing and computational analysis. Five different novel analogues were synthesized that further probed the role of one section of the molecule and acquire some structure-activity relationships.

Additional Information

Language: English
Date: 2016
GPR55, Synthesis
G proteins $x Receptors $x Research

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