HOAT1: Difference between revisions
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===Full Mechanism of Binding and Inhibition in hOAT1=== | ===Full Mechanism of Binding and Inhibition in hOAT1=== | ||
[[Image:HOAT1mechanism.png | frame | upright= 1.5 |none | alt= | Fig.1. Mechanism of olmesartan binding and conformational inhibition by probenecid. A) When the transporter is in its outward-facing conformation, substrates or inhibitors enter the central binding pocket and undergo structural rearrangement to | [[Image:HOAT1mechanism.png | frame |300px| upright= 1.5 |none | alt= | Fig.1. Mechanism of olmesartan binding and conformational inhibition by probenecid. A) When the transporter is in its outward-facing conformation, substrates or inhibitors enter the central binding pocket and undergo structural rearrangement to | ||
the inward-facing conformation. When olmesartan interacts with the bottom gating residues M207 and F442, the side chains S203, Y230 (not shown here), and | the inward-facing conformation. When olmesartan interacts with the bottom gating residues M207 and F442, the side chains S203, Y230 (not shown here), and | ||
R466 appear to rearrange to coordinate with a chloride ion and drug compared to the apo structure. Whereas probenecid binding induces an additional | R466 appear to rearrange to coordinate with a chloride ion and drug compared to the apo structure. Whereas probenecid binding induces an additional | ||
