Structural basis for GPR40 allosteric agonism and incretin stimulation
GPR40 is a G-protein coupled receptor that binds to free fatty acids, mediating insulin and incretin secretion. Here, the authors present the crystal structure of human GPR40 with an agonist bound to an allosteric site located near the lipid-rich region that suggests a mechanism for biased agonism.
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Nature Portfolio
2018
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oai:doaj.org-article:5d745f39e74e44df919e15e9433e1c332021-12-02T16:56:53ZStructural basis for GPR40 allosteric agonism and incretin stimulation10.1038/s41467-017-01240-w2041-1723https://doaj.org/article/5d745f39e74e44df919e15e9433e1c332018-04-01T00:00:00Zhttps://doi.org/10.1038/s41467-017-01240-whttps://doaj.org/toc/2041-1723GPR40 is a G-protein coupled receptor that binds to free fatty acids, mediating insulin and incretin secretion. Here, the authors present the crystal structure of human GPR40 with an agonist bound to an allosteric site located near the lipid-rich region that suggests a mechanism for biased agonism.Joseph D. HoBetty ChauLogan RodgersFrances LuKelly L. WilburKeith A. OttoYanyun ChenMin SongJonathan P. RileyHsiu-Chiung YangNichole A. ReynoldsSteven D. KahlAnjana Patel LewisChristopher GroshongRussell E. MadsenKris ConnersJayana P. LineswalaTarun GheyiMelbert-Brian Decipulo SaflorMatthew R. LeeJordi BenachKenton A. BakerChahrzad Montrose-RafizadehMichael J. GeninAnne R. MillerChafiq HamdouchiNature PortfolioarticleScienceQENNature Communications, Vol 9, Iss 1, Pp 1-11 (2018) |
| institution |
DOAJ |
| collection |
DOAJ |
| language |
EN |
| topic |
Science Q |
| spellingShingle |
Science Q Joseph D. Ho Betty Chau Logan Rodgers Frances Lu Kelly L. Wilbur Keith A. Otto Yanyun Chen Min Song Jonathan P. Riley Hsiu-Chiung Yang Nichole A. Reynolds Steven D. Kahl Anjana Patel Lewis Christopher Groshong Russell E. Madsen Kris Conners Jayana P. Lineswala Tarun Gheyi Melbert-Brian Decipulo Saflor Matthew R. Lee Jordi Benach Kenton A. Baker Chahrzad Montrose-Rafizadeh Michael J. Genin Anne R. Miller Chafiq Hamdouchi Structural basis for GPR40 allosteric agonism and incretin stimulation |
| description |
GPR40 is a G-protein coupled receptor that binds to free fatty acids, mediating insulin and incretin secretion. Here, the authors present the crystal structure of human GPR40 with an agonist bound to an allosteric site located near the lipid-rich region that suggests a mechanism for biased agonism. |
| format |
article |
| author |
Joseph D. Ho Betty Chau Logan Rodgers Frances Lu Kelly L. Wilbur Keith A. Otto Yanyun Chen Min Song Jonathan P. Riley Hsiu-Chiung Yang Nichole A. Reynolds Steven D. Kahl Anjana Patel Lewis Christopher Groshong Russell E. Madsen Kris Conners Jayana P. Lineswala Tarun Gheyi Melbert-Brian Decipulo Saflor Matthew R. Lee Jordi Benach Kenton A. Baker Chahrzad Montrose-Rafizadeh Michael J. Genin Anne R. Miller Chafiq Hamdouchi |
| author_facet |
Joseph D. Ho Betty Chau Logan Rodgers Frances Lu Kelly L. Wilbur Keith A. Otto Yanyun Chen Min Song Jonathan P. Riley Hsiu-Chiung Yang Nichole A. Reynolds Steven D. Kahl Anjana Patel Lewis Christopher Groshong Russell E. Madsen Kris Conners Jayana P. Lineswala Tarun Gheyi Melbert-Brian Decipulo Saflor Matthew R. Lee Jordi Benach Kenton A. Baker Chahrzad Montrose-Rafizadeh Michael J. Genin Anne R. Miller Chafiq Hamdouchi |
| author_sort |
Joseph D. Ho |
| title |
Structural basis for GPR40 allosteric agonism and incretin stimulation |
| title_short |
Structural basis for GPR40 allosteric agonism and incretin stimulation |
| title_full |
Structural basis for GPR40 allosteric agonism and incretin stimulation |
| title_fullStr |
Structural basis for GPR40 allosteric agonism and incretin stimulation |
| title_full_unstemmed |
Structural basis for GPR40 allosteric agonism and incretin stimulation |
| title_sort |
structural basis for gpr40 allosteric agonism and incretin stimulation |
| publisher |
Nature Portfolio |
| publishDate |
2018 |
| url |
https://doaj.org/article/5d745f39e74e44df919e15e9433e1c33 |
| work_keys_str_mv |
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1718382683142225920 |