Channels · 2 authors, 1 centre
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This review summarizes recent structural pharmacology studies that have uncovered the molecular mechanisms by which various small molecules inhibit the calcium channel TRPV6. The central result is the identification of two major inhibition mechanisms: direct pore block and allosteric inhibition involving lipid displacement.
This narrative review synthesizes recent advances in the structural pharmacology of the TRPV6 calcium channel. The central finding is the classification of inhibitors into two major mechanisms: direct block of the ion channel pore (e.g., by PCHPDs, ruthenium red) and allosteric inhibition with lipid displacement (e.g., by 2-APB, econazole). The review discusses how these mechanisms relate to distinct conformational states of the channel pore—open, closed, and inactivated.
