Article
Engineering a "steric doorstop" in rhodopsin: converting an inverse agonist to an agonist.
Biochemistry - 30 Oct 2007
McKee Timothy D, Lewis Margaret R, Kono Masahiro
Abstract excerpt
The crystal structures of rhodopsin depict the inactive conformation of rhodopsin in the dark. The 11-cis retinoid chromophore, the inverse agonist holding rhodopsin inactive, is well-resolved. Thr118 in helix 3 is the closest amino acid residue next to the 9-methyl group of the chromophore. The 9-methyl group of retinal facilitates the transition from an inactive metarhodopsin I to the active metarhodopsin II...
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