Informed development of drugs acting at Family B G protein-coupled receptors

Laurence J. Miller

doi:10.1196/annals.1418.001

Informed development of drugs acting at Family B G protein-coupled receptors

Laurence J. Miller

Gastroenterology and Hepatology

Research output: Chapter in Book/Report/Conference proceeding › Conference contribution

2 Scopus citations

Abstract

Rational refinement and development of receptor-active ligands can come from high-resolution insights into the structures of these potential drug targets. Structural insights for Family A G protein-coupled receptors (GPCRs) have been advanced substantially with the recently reported crystal structure of the intact β₂-adrenergic receptor. While high-resolution structural insights for Family B GPCRs are also advancing, this is currently limited to the functionally important extracellular amino-terminal tail domain of those receptors. The current report describes how these structures can provide leads for the development of small-molecule agonist drugs acting at Family B GPCRs. Endogenous agonist activity within the amino terminus of these receptors could be key for the development of such drugs.

Original language	English (US)
Title of host publication	Neural Signaling Opportunities for Novel Diagnostic Approaches and Therapies
Publisher	Blackwell Publishing Inc.
Pages	203-209
Number of pages	7
ISBN (Print)	9781573317047
DOIs	https://doi.org/10.1196/annals.1418.001
State	Published - Nov 2008

Publication series

Name	Annals of the New York Academy of Sciences
Volume	1144
ISSN (Print)	0077-8923
ISSN (Electronic)	1749-6632

Keywords

Activation mechanisms
G protein-coupled receptors
Ligand binding
Receptor structure
Secretin receptor

ASJC Scopus subject areas

General Neuroscience
General Biochemistry, Genetics and Molecular Biology
History and Philosophy of Science

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10.1196/annals.1418.001

Cite this

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title = "Informed development of drugs acting at Family B G protein-coupled receptors",

abstract = "Rational refinement and development of receptor-active ligands can come from high-resolution insights into the structures of these potential drug targets. Structural insights for Family A G protein-coupled receptors (GPCRs) have been advanced substantially with the recently reported crystal structure of the intact β2-adrenergic receptor. While high-resolution structural insights for Family B GPCRs are also advancing, this is currently limited to the functionally important extracellular amino-terminal tail domain of those receptors. The current report describes how these structures can provide leads for the development of small-molecule agonist drugs acting at Family B GPCRs. Endogenous agonist activity within the amino terminus of these receptors could be key for the development of such drugs.",

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AB - Rational refinement and development of receptor-active ligands can come from high-resolution insights into the structures of these potential drug targets. Structural insights for Family A G protein-coupled receptors (GPCRs) have been advanced substantially with the recently reported crystal structure of the intact β2-adrenergic receptor. While high-resolution structural insights for Family B GPCRs are also advancing, this is currently limited to the functionally important extracellular amino-terminal tail domain of those receptors. The current report describes how these structures can provide leads for the development of small-molecule agonist drugs acting at Family B GPCRs. Endogenous agonist activity within the amino terminus of these receptors could be key for the development of such drugs.

KW - Activation mechanisms

KW - G protein-coupled receptors

KW - Ligand binding

KW - Receptor structure

KW - Secretin receptor

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BT - Neural Signaling Opportunities for Novel Diagnostic Approaches and Therapies

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ER -

Informed development of drugs acting at Family B G protein-coupled receptors

Abstract

Publication series

Keywords

ASJC Scopus subject areas

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