5KW2

The extra-helical binding site of GPR40 and the structural basis for allosteric agonism and incretin stimulation

Summary for 5KW2

• Entry DOI: 10.2210/pdb5kw2/pdb
• Descriptor: Free fatty acid receptor 1,Lysozyme,Free fatty acid receptor 1, (3~{S})-3-cyclopropyl-3-[2-[1-[2-[2,2-dimethylpropyl-(6-methylpyridin-2-yl)carbamoyl]-5-methoxy-phenyl]piperidin-4-yl]-1-benzofuran-6-yl]propanoic acid (3 entities in total)
• Functional Keywords: g-protein coupled receptor, free fatty acid receptor 1, lipid-binding protein, fatty acid binding protein-hydrolase complex, fatty acid binding protein/hydrolase
• Biological source: Homo sapiens (Human); More
• Cellular location: Cell membrane ; Multi-pass membrane protein : O14842
• Total number of polymer chains: 1
• Total formula weight: 53725.97

Authors

Ho, J.D.,Chau, B.,Rodgers, L.,Lu, F.,Wilbur, K.L.,Otto, K.A.,Chen, Y.,Song, M.,Riley, J.P.,Yang, H.-C.,Reynolds, N.A.,Kahl, S.D.,Lewis, A.P.,Groshong, C.,Madsen, R.E.,Conners, K.,Linswala, J.P.,Gheyi, T.,Saflor, M.D.,Lee, M.R.,Benach, J.,Baker, K.A.,Montrose-Rafizadeh, C.,Genin, M.J.,Miller, A.R.,Hamdouchi, C. (deposition date: 2016-07-15, release date: 2018-05-02, Last modification date: 2023-10-04)

• Primary citation: Ho, J.D.,Chau, B.,Rodgers, L.,Lu, F.,Wilbur, K.L.,Otto, K.A.,Chen, Y.,Song, M.,Riley, J.P.,Yang, H.C.,Reynolds, N.A.,Kahl, S.D.,Lewis, A.P.,Groshong, C.,Madsen, R.E.,Conners, K.,Lineswala, J.P.,Gheyi, T.,Saflor, M.D.,Lee, M.R.,Benach, J.,Baker, K.A.,Montrose-Rafizadeh, C.,Genin, M.J.,Miller, A.R.,Hamdouchi, C.; Structural basis for GPR40 allosteric agonism and incretin stimulation.; Nat Commun, 9:1645-1645, 2018; PubMed: 29695780; DOI: 10.1038/s41467-017-01240-w

Experimental method

X-RAY DIFFRACTION (2.76 Å)