Nature Communications (Apr 2018)
Structural basis for GPR40 allosteric agonism and incretin stimulation
- 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
Affiliations
- Joseph D. Ho
- Lilly Biotechnology Center San Diego
- Betty Chau
- Lilly Biotechnology Center San Diego
- Logan Rodgers
- Lilly Biotechnology Center San Diego
- Frances Lu
- Lilly Biotechnology Center San Diego
- Kelly L. Wilbur
- Lilly Research Laboratories, Lilly Corporate Center
- Keith A. Otto
- Lilly Research Laboratories, Lilly Corporate Center
- Yanyun Chen
- Lilly Research Laboratories, Lilly Corporate Center
- Min Song
- Lilly Research Laboratories, Lilly Corporate Center
- Jonathan P. Riley
- Lilly Research Laboratories, Lilly Corporate Center
- Hsiu-Chiung Yang
- Lilly Research Laboratories, Lilly Corporate Center
- Nichole A. Reynolds
- Lilly Research Laboratories, Lilly Corporate Center
- Steven D. Kahl
- Lilly Research Laboratories, Lilly Corporate Center
- Anjana Patel Lewis
- Lilly Research Laboratories, Lilly Corporate Center
- Christopher Groshong
- Lilly Biotechnology Center San Diego
- Russell E. Madsen
- Lilly Biotechnology Center San Diego
- Kris Conners
- Lilly Biotechnology Center San Diego
- Jayana P. Lineswala
- Lilly Research Laboratories, Lilly Corporate Center
- Tarun Gheyi
- Lilly Biotechnology Center San Diego
- Melbert-Brian Decipulo Saflor
- Lilly Biotechnology Center San Diego
- Matthew R. Lee
- Lilly Biotechnology Center San Diego
- Jordi Benach
- Lilly Research Laboratories Collaborative Access Team, Advanced Photon Source, Argonne National Laboratory
- Kenton A. Baker
- Lilly Biotechnology Center San Diego
- Chahrzad Montrose-Rafizadeh
- Lilly Research Laboratories, Lilly Corporate Center
- Michael J. Genin
- Lilly Research Laboratories, Lilly Corporate Center
- Anne R. Miller
- Lilly Research Laboratories, Lilly Corporate Center
- Chafiq Hamdouchi
- Lilly Research Laboratories, Lilly Corporate Center
- DOI
- https://doi.org/10.1038/s41467-017-01240-w
- Journal volume & issue
-
Vol. 9,
no. 1
pp. 1 – 11
Abstract
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.
