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Sphingosine-1-phosphate receptors are the targets for treating many human diseases and selectivity is one of the major hindrances during drug development. Two crystal structures of human sphingosine-1-phosphate receptor 3 in complex with one bitopic ligand SPM-242 as well as allosteric ligands Cpd-32 or CYM52581 bound simultaneously was reported, and together with cryo-electron microscopy structures of S1P2 and S1P3 in complex with heterotrimeric Gi protein, the activation process of Sphingosine-1-phosphate receptors is revealed and the key sites for designation of better selective S1P ligands are proposed.
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HIGHER EDUCATION PRESS
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