5i2p

Resonance assignments and NMR structure determination of tarantula toxin- W7A mutant of mu-TRTX-Pre1a (W6A in native sequence numbering)

spinqualitylabelsall models 5i2p Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 5i2p is a 1 chain structure with sequence from Psalmopoeus. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: Solution NMR, 20 models Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function NTA_PSARE Gating-modifier toxin that both inhibits the peak current of human Nav1.1/SCN1A, rat Nav1.2/SCN2A, human Nav1.6/SCN8A, and human Nav1.7/SCN9A and concurrently inhibits fast inactivation of human Nav1.1 and rat Nav1.3/SCN3A. The relative rank order potency for Nav modulation is Nav1.3 (inactivation EC(50)=45 nM) > Nav1.7 > Nav1.2 > Nav1.1 (inactivation) > Nav1.1 > Nav1.6 > Nav1.3 (IC(50)=8 uM). The DII and DIV S3-S4 loops of Nav channel voltage sensors are important for the interaction of this toxin with Nav channels but cannot account for its unique subtype selectivity. It is the variability of the S1-S2 loops between NaV channels which contributes substantially to the selectivity profile observed for this toxin, particularly with regards to fast inactivation. This toxin may bind the channel in the resting state (Probable).

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