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Abstract
The adhesion family of G protein–coupled receptors (aGPCRs) comprises 33 members in humans. aGPCRs are characterized by their enormous size and complex modular structures. While the physiologic importance of many aGPCRs has been clearly demonstrated in recent years, the underlying molecular functions have only recently begun to be elucidated. In this minireview, we present an overview of our current knowledge on aGPCR activation and signal transduction with a focus on the latest findings regarding the interplay between ligand binding, mechanical force, and the tethered agonistic Stachel sequence, as well as implications on translational approaches that may derive from understanding aGPCR pharmacology.
Footnotes
- Received February 27, 2015.
- Accepted May 8, 2015.
Work in our laboratories was supported by grants from the National Institutes of Health to K.R.M. [R01-NS079445, R01-HD080601], the Muscular Dystrophy Association to K.R.M. [293295], the German Research Council to J.H., T.L., T.S., and I.L. [FOR2149], and the Netherlands Organization for Scientific Research to S.N. [NWO VENI Grant 722.014.011].
- Copyright © 2015 by The American Society for Pharmacology and Experimental Therapeutics
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