title: Gut hormone GPCRs: structure, function, drug discovery.
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.
authors.affiliation: Laboratori de Medicina Computacional, Unitat de Bioestadística, Facultat de Medicina, Universitat Autònoma de Barcelona, Barcelona, Spain.
authors.forename: Arnau
authors.initials: A
authors.lastname: Cordomí
authors.affiliation: Laboratory of Chemistry and Physics of Nano-objects, ERL1226 INSERM, University of Toulouse, CNRS, INSERM, Toulouse, France. Electronic address: Daniel.Fourmy@inserm.fr.
authors.forename: Daniel
authors.initials: D
authors.lastname: Fourmy
authors.affiliation: Molecular Modelling Laboratory, School of Pharmacy, Queen's University Belfast, Northern Ireland, UK.
authors.forename: Irina G
authors.initials: IG
authors.lastname: Tikhonova
mesh_terms: D019390:Arrestins / Q000378:metabolism; D003460:Crystallization; D015195:Drug Design; D055808:Drug Discovery / Q000379:methods*; D019204:GTP-Binding Proteins / Q000378:metabolism; D005768:Gastrointestinal Hormones / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D018343:Receptors, Adrenergic, beta-2 / Q000737:chemistry / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D019390:Arrestins; D005768:Gastrointestinal Hormones; D008024:Ligands; D018343:Receptors, Adrenergic, beta-2; D043562:Receptors, G-Protein-Coupled; D019204:GTP-Binding Proteins