6a91 | pdb_00006a91

Complex of voltage-gated sodium channel NavPaS from American cockroach Periplaneta americana bound with saxitoxin and Dc1a

Loading... Status: waiting for Mol* initialization Structural highlights 6a91 is a 2 chain structure with sequence from American cockroach and Digca. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 9SL, NAG, PC1 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function [SCNA1_PERAM] Mediates the voltage-dependent sodium ion permeability of excitable membranes.[RuleBase:RU361132] Publication Abstract from PubMed Animal toxins that modulate the activity of Nav channels are broadly divided into two categories-pore blockers and gating modifiers. The pore blockers tetrodotoxin (TTX) and saxitoxin (STX) are responsible for pufferfish and shellfish poisoning in humans, respectively. Here we present structures of the insect Nav channel NavPaS bound to a gating modifier toxin Dc1a at 2.8 A and in the presence of TTX or STX at 2.6 A and 3.2 A resolution, respectively. Dc1a inserts into the cleft between VSDII and the pore of NavPaS, making key contacts with both domains. The structures with bound TTX or STX reveal the molecular details for the specific blockade of Na(+) access to the selectivity filter from the extracellular side by these guanidinium toxins. The structures shed light on structure-based development of Nav channel drugs. Structural basis for the modulation of voltage-gated sodium channels by animal toxins.,Shen H, Li Z, Jiang Y, Pan X, Wu J, Cristofori-Armstrong B, Smith JJ, Chin YKY, Lei J, Zhou Q, King GF, Yan N Science. 2018 Jul 26. pii: science.aau2596. doi: 10.1126/science.aau2596. PMID:30049784 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Ion channels 3D structures

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