Ontology highlight
ABSTRACT:
SUBMITTER: Ho JD
PROVIDER: S-EPMC5917010 | biostudies-literature | 2018 Apr
REPOSITORIES: biostudies-literature
Ho Joseph D JD Chau Betty B Rodgers Logan L Lu Frances F Wilbur Kelly L KL Otto Keith A KA Chen Yanyun Y Song Min M Riley Jonathan P JP Yang Hsiu-Chiung HC Reynolds Nichole A NA Kahl Steven D SD Lewis Anjana Patel AP Groshong Christopher C Madsen Russell E RE Conners Kris K Lineswala Jayana P JP Gheyi Tarun T Saflor Melbert-Brian Decipulo MD Lee Matthew R MR Benach Jordi J Baker Kenton A KA Montrose-Rafizadeh Chahrzad C Genin Michael J MJ Miller Anne R AR Hamdouchi Chafiq C
Nature communications 20180425 1
Activation of free fatty acid receptor 1 (GPR40) by synthetic partial and full agonists occur via distinct allosteric sites. A crystal structure of GPR40-TAK-875 complex revealed the allosteric site for the partial agonist. Here we report the 2.76-Å crystal structure of human GPR40 in complex with a synthetic full agonist, compound 1, bound to the second allosteric site. Unlike TAK-875, which acts as a Gα<sub>q</sub>-coupled partial agonist, compound 1 is a dual Gα<sub>q</sub> and Gα<sub>s</sub> ...[more]