Gut hormone GPCRs: structure, function, drug discovery

Arnau Cordomí

doi:10.1016/j.coph.2016.09.001

2016-12-01

Arnau Cordomí

Daniel Fourmy *

Irina G. Tikhonova

DOI：10.1016/j.coph.2016.09.001

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摘要

En 中文

Crystallization and determination of the high resolution three-dimensional structure of the beta 2-adrenergic receptor in 2007 was followed by structure elucidation of a number of other receptors, including those for neurotensin and glucagon. These major advances foster the understanding of structure-activity relationship of these receptors and structure-based rational design of new ligands having more predictable activity. At present, structure determination of gut hormone receptors in complex with their ligands (natural, synthetic) and interacting signalling proteins, for example, G-proteins, arrestins, represents a challenge which promises to revolutionize gut hormone endocrinonology.

Keyword:

PROTEIN-COUPLED RECEPTORS

2ND TRANSMEMBRANE HELIX

CLASS-B GPCRS

GLUCAGON RECEPTOR

CRYSTAL-STRUCTURE

NEUROTENSIN RECEPTOR

LIGAND-BINDING

AMINO-TERMINUS

RECOGNITION

ACTIVATION

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期刊

Current Opinion in Pharmacology

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4.2

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centre national de la recherche scientifique (cnrs)

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university of barcelona

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Autonomous University of Barcelona

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