NPM : 2A214304
Kelas : 3EB24
Kelas : 3EB24
Chemical Tools for Studying Lipid-Binding Class A G
Protein–Coupled Receptors
Anna Cooper, Sameek Singh, Sarah Hook, Joel D. A.
Tyndall and Andrea J. Vernall
Stephen P. H. Alexander, ASSOCIATE EDITOR
Pharmacological Reviews July 2017, 69 (3) 316-353;
DOI: https://doi.org/10.1124/pr.116.01324
Abstract
Cannabinoid,
free fatty acid, lysophosphatidic acid, sphingosine 1-phosphate, prostanoid,
leukotriene, bile acid, and platelet-activating factor receptor families are
class A G protein–coupled receptors with endogenous lipid ligands.
Pharmacological tools are crucial for studying these receptors and addressing
the many unanswered questions surrounding expression of these receptors in
normal and diseased tissues. An inherent challenge for developing tools for
these lipid receptors is balancing the often lipophilic requirements of the
receptor-binding pharmacophore with favorable physicochemical properties to
optimize highly specific binding. In this study, we review the radioligands,
fluorescent ligands, covalent ligands, and antibodies that have been used to
study these lipid-binding receptors. For each tool type, the characteristics
and design rationale along with in vitro and in vivo applications are detailed.
Footnotes
Received September 8, 2016.
Accepted May 15, 2017.
A.C. and S.S. contributed equally to this work.
sumber : http://pharmrev.aspetjournals.org/content/69/3/316
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