doi: 10.1016/j.bmcl.2014.06.082.
Epub 2014 Jul 4.
Allosteric modulation of the G protein-coupled US28 receptor of human cytomegalovirus: are the small-weight inverse agonist of US28 'camouflaged' agonists?
Affiliations
- PMID: 25052428
- DOI: 10.1016/j.bmcl.2014.06.082
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Allosteric modulation of the G protein-coupled US28 receptor of human cytomegalovirus: are the small-weight inverse agonist of US28 'camouflaged' agonists?
Bioorg Med Chem Lett.
.
Abstract
The highly constitutively active G protein-coupled receptor US28 of human cytomegalovirus (HCMV) is thought to camouflage agonism by mediating constitutive endocytosis. With the use of the US28Δ300 mutant, which is largely devoid of constitutive internalization, I have demonstrated that the coupling of the receptor to its downstream signaling partners is responsible for the inverse agonism to agonism efficacy switch in some small-weight ligands of US28.
Keywords: Allosteric modulation; Efficacy switch; G protein-coupled receptor; Human cytomegalovirus; Inverse agonism; US28.
Copyright © 2014 Elsevier Ltd. All rights reserved.
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