Description: GX-936, also known as PF-05196233, is a Nav1.7 inhibitor. GX-936 inhibit Nav1.7 through a voltage-sensor trapping mechanism, ...
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GX-936 (PF 05196233) is a potent Nav1.7 inhibitor that binds to the activated state of voltage-sensor domain IV (VSD4), exhibits robust inhibition of the ...
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The GX-936 sticks deep into the extracellular aqueous cleft of the VSD IV , and its negatively-charged warhead engages the fourth gating-charge (R4), locking ...
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GX-936 (GX936; PF-05196233; PF 05196233) is a novel and potent Nav1.7 inhibitor with the potential to be used to treat cardiovascular and neurological ...
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GX-936 (PF 05196233) is a potent Nav1.7 inhibitor that binds to the activated state of voltage-sensor domain IV (VSD4), exhibits robust inhibition of the ...
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GX-936 (PF 05196233) is a potent Nav1.7 inhibitor that binds to the activated state of voltage-sensor domain IV (VSD4), exhibits robust inhibition of the ...
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Novel isoform-selective antagonist of voltage-gated sodium 1.7 (Nav1.7) channels, binding to Nav1.7 VSD4-NavAb.
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4 thg 2, 2022 · GX-936 (PF 05196233) is a potent Nav1.7 inhibitor that binds to the activated state of voltage-sensor domain IV (VSD4), exhibits robust ...
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3 thg 11, 2015 · Chimera of bacterial Ion transport protein and human Sodium channel protein type 9 subunit alpha1 ...
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18 thg 12, 2015 · GX-936 and related inhibitors bind to the activated state of voltage-sensor domain IV (VSD4), where their anionic aryl sulfonamide warhead ...
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9 thg 9, 2020 · (A) Cryo-EM structure of STX bound to human NaV1.7-β1-β2 complex (PDB: 6j8g) with GX-936 positioned approximately based on PDB: 5ek0 in ...
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11 thg 3, 2022 · This is consistent with the dramatic potency loss for GX936 when ... NaV1.3 and NaV1.1, while PF-04856264 and GX-936 inhibits NaV1.7.
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23 thg 12, 2015 · 5EK0 · Human Nav1.7-VSD4-NavAb in complex with GX-936. · Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist.
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