Gut hormone GPCRs: structure, function, drug discovery

Arnau Cordomí; Daniel Fourmy; Irina G Tikhonova

doi:10.1016/j.coph.2016.09.001

Gut hormone GPCRs: structure, function, drug discovery

Arnau Cordomí, Daniel Fourmy, Irina G Tikhonova

School of Pharmacy

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Abstract

Crystallization and determination of the high resolution three-dimensional structure of the β2-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.

Original language	English
Pages (from-to)	63-67
Number of pages	5
Journal	Current Opinion in Pharmacology
Volume	31
Early online date	16 Sep 2016
DOIs	https://doi.org/10.1016/j.coph.2016.09.001
Publication status	Published - Dec 2016

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Gut hormone GPCRs: structure, function, drug discovery
© 2016 Elsevier Ltd. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/, which permits distribution and reproduction for non-commercial purposes, provided the author and source are cited.
Accepted author manuscript, 376 KBLicence: CC BY-NC-ND

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abstract = "Crystallization and determination of the high resolution three-dimensional structure of the β2-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.",

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AB - Crystallization and determination of the high resolution three-dimensional structure of the β2-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.

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DO - 10.1016/j.coph.2016.09.001

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JO - Current Opinion in Pharmacology

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Gut hormone GPCRs: structure, function, drug discovery

Abstract

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