TY - JOUR
T1 - Gut hormone GPCRs: structure, function, drug discovery
AU - Cordomí, Arnau
AU - Fourmy, Daniel
AU - Tikhonova, Irina G.
PY - 2016/12/1
Y1 - 2016/12/1
N2 - © 2016 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.
AB - © 2016 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.
U2 - 10.1016/j.coph.2016.09.001
DO - 10.1016/j.coph.2016.09.001
M3 - Review article
VL - 31
SP - 63
EP - 67
JO - Current Opinion in Pharmacology
JF - Current Opinion in Pharmacology
SN - 1471-4892
ER -