Fig. 5: Conformational changes and mechanism of TRPV6 inhibition by THCV. | Nature Communications

Fig. 5: Conformational changes and mechanism of TRPV6 inhibition by THCV.

From: Molecular pathway and structural mechanism of human oncochannel TRPV6 inhibition by the phytocannabinoid tetrahydrocannabivarin

Fig. 5

a Superposition of TRPV6THCV (green) and apo-state TRPV6Open (purple, PDB ID: 7S89) structures. THCV molecule at site 1 (yellow) as well as residues contributing to THCV binding and forming the gate (M578) are shown as sticks. Conformational changes induced by THCV binding are indicated by red arrows. The region that undergoes the π-to-α transition in S6 upon THCV binding is highlighted (pink). b, c Core of the transmembrane domain in TRPV6Open (b) and TRPV6THCV (c), with elongated S6 and TRP helices indicated by double arrows, respectively. Open-state stabilizing interactions between Q473 and R589 as well as D489 and T581 are shown as dotted lines. Only two of four subunits are shown, with the front and back subunits removed for clarity. d, e Intracellular views of the gate region in TRPV6Open (d) and TRPV6THCV (e), with the surface shown in the corresponding color and M578 labeled.

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