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This version published online on March 27, 2008
Molecular Endocrinology, doi:10.1210/me.2008-0025
Molecular Endocrinology Vol. 0, No. 2008 200800251-
doi:10.1210/me.2008-0025
Copyright © 2008 by the Endocrine Society.
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Submitted on January 22, 2008
Accepted on March 19, 2008

Insights into the Structural Basis of Endogenous Agonist Activation of Family B G Protein-Coupled Receptors

Maoqing Dong*, Fan Gao, Delia I. Pinon, and Laurence J. Miller*

Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Scottsdale, Scottsdale, AZ 85259

* To whom correspondence should be addressed. E-mail: dongmq{at}mayo.edu or miller{at}mayo.edu.

Agonist drugs targeting the glucagon-like peptide-1 (GLP1) receptor represent important additions to the clinical management of patients with diabetes mellitus. In the current report, we have explored whether the recently described concept of a receptor-active endogenous agonist sequence within the amino terminus of the secretin receptor may also be applicable to the GLP1 receptor. If so, this could provide a lead for the development of additional small molecule agonists targeting this and other important family members. Indeed, the region of the GLP1 receptor analogous to that containing the active WDN within the secretin receptor was found to possess full agonist activity at the GLP1 receptor. The minimal fragment within this region that had full agonist activity was NRTFD. Despite having no primary sequence identity with the WDN, it was also active at the secretin receptor, where it had similar potency and efficacy to WDN, suggesting common structural features. Molecular modeling demonstrated that an intradomain salt bridge between the side chains of arginine and aspartate could yield similarities in structure with cyclic WDN. This directly supports the relevance of the endogenous agonist concept to the GLP1 receptor and provides new insights into the rational development and refinement of new types of drugs activating this important receptor.


Key words: G protein-coupled receptor • glucagon-like peptide-1 • glucagon-like peptide-1 receptor • secretin receptor • receptor activation







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