Secretin Receptor Dimerization: A Possible Functionally Important Paradigm for Family B G Protein‐Coupled Receptors

Harikumar, Kaleeckal G.; Dong, Maoqing; Miller, Laurence J.

doi:10.1002/9780470627327.ch6

Cited by 1 publication

(1 citation statement)

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“…The potential to form oligomers seems to differ based on the class of GPCR, with obligate and sometimes covalently stabilized dimers observed for class C GPCRs, and with more transient association events described for a subset of the class A GPCRs. Class B GPCRs seem to be intermediate between these two groups (72), with what appears to represent relatively stable dimers that are structurally specific along the lipid face of TM4 (73). These can have functional effects, such as to increase ligand affinity and potency, but this has not been present in all such complexes, and the tendency to dimerize has been variable across this family.…”

Section: Endogenous Potential Allosteric Ligandsmentioning

confidence: 99%

Structural Basis for Allosteric Modulation of Class B G Protein–Coupled Receptors

Wootten

Miller

2020

Annu. Rev. Pharmacol. Toxicol.

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Recent advances in our understanding of the structure and function of class B G protein–coupled receptors (GPCRs) provide multiple opportunities for targeted development of allosteric modulators. Given the pleiotropic signaling patterns emanating from these receptors in response to a variety of natural agonist ligands, modulators have the potential to sculpt the responses to meet distinct needs of different groups of patients. In this review, we provide insights into how this family of GPCRs differs from the rest of the superfamily, how orthosteric agonists bind and activate these receptors, the potential for allosteric modulators to interact with various regions of these targets, and the allosteric influence of endogenous proteins on the pharmacology of these receptors, all of which are important considerations when developing new therapies.

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Section: Endogenous Potential Allosteric Ligandsmentioning

confidence: 99%