2mva | pdb_00002mva

Solution structure of the toxin, RhTx

spinqualitylabelsall models 2mva Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2mva is a 1 chain structure with sequence from Scolopendra subspinipes. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: Solution NMR Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function TX41A_SCOMU Extremely potent agonist and potentiator of TRPV1 (EC(50)=470-521.5 nM (mouse)) (PubMed:26420335, PubMed:32097697). It strongly promotes the heat activation process by downshifting the activation threshold temperature (PubMed:26420335). It preferably binds to the activated channel and promotes its opening (PubMed:26420335). Holding the channel closed by cooling prevents binding of this toxin, leaving it ineffective (PubMed:26420335). The toxin binds to the charge-rich outer pore region of the channel where it directly interacts with the pore helix and turret, two adjacent structural elements known to be critical for activation gating of TRPV1 (PubMed:26420335). In comparison with Sm1b, induces a TRPV1 desensitization with slower kinetics (20 seconds) (PubMed:32097697). In vivo, induces pain in mice after intraplantar injection (PubMed:26420335). Potent agonist and probable potentiator of TRPV1 (EC(50)=38.35 uM (mouse)) (PubMed:32097697). Also binds to the outer pore region of TRPV1 (PubMed:32097697). In comparison with Sm1a, induces a TRPV1 desensitization with faster kinetics (2 seconds) and leads to a more complete TRPV1 desensitization (PubMed:32097697). Desensitization is achieved by reducing both the open probability and the single-channel conductance upon prolonged exposure (PubMed:32097697).

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