AM-6120   Click here for help

GtoPdb Ligand ID: 10119

Synonyms: AM6120 | peptide 41 [PMID: 30346167]
Immunopharmacology Ligand
Comment: AM-6120 is a peptidic voltage-gated sodium channel blocker with the sequence Glu-[Pra1;Nle6;Ala12;5-BrW24;Glu28]JzTx-V(1-29), where JzTx-V is a sodium channel inhibitor isolated from tarantula venom [2]. JzTx-V inhibits NaV1.7 activity by interacting with the second voltage sensor domain of the NaV1.7 pore forming α-subunit and thereby holding the ion channel in a closed conformation, but its action is non-selective [1].
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1. Moyer BD, Murray JK, Ligutti J, Andrews K, Favreau P, Jordan JB, Lee JH, Liu D, Long J, Sham K et al.. (2018)
Pharmacological characterization of potent and selective NaV1.7 inhibitors engineered from Chilobrachys jingzhao tarantula venom peptide JzTx-V.
PLoS ONE, 13 (5): e0196791. DOI: 10.1371/journal.pone.0196791 [PMID:29723257]
2. Wu B, Murray JK, Andrews KL, Sham K, Long J, Aral J, Ligutti J, Amagasu S, Liu D, Zou A et al.. (2018)
Discovery of Tarantula Venom-Derived NaV1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis.
J Med Chem, 61 (21): 9500-9512. [PMID:30346167]