κO-SrVIA 短杆菌肽，一种新型的人类 EAG 钾通道家族两个成员的抑制肽。

κO-SrVIA Conopeptide, a Novel Inhibitor Peptide for Two Members of the Human EAG Potassium Channel Family.

机构信息

Posgrado en Ciencias Biológicas, Instituto de Ciencias del Mar y Limnología, Universidad Nacional Autónoma de México, Ciudad de México 04510, Mexico.

Laboratorio de Toxinología Marina, Unidad Académica de Ecología y Biodiversidad Acuática, Instituto de Ciencias del Mar y Limnología, Universidad Nacional Autónoma de México, Ciudad de México 04510, Mexico.

出版信息

Int J Mol Sci. 2023 Jul 15;24(14):11513. doi: 10.3390/ijms241411513.

DOI:10.3390/ijms241411513

PMID:37511269

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10380377/

Abstract

The first conotoxin affecting the voltage-gated potassium channels of the EAG family was identified and characterized from the venom of the vermivorous species from the Gulf of Mexico. This conopeptide, initially named Cs68 and later designated κO-SrVIA, is extremely hydrophobic and comprises 31 amino acid residues, including six Cysteines in the framework VI/VII, and a free C-terminus. It inhibits the currents mediated by two human EAG subtypes, Kv10.1 (IC = 1.88 ± 1.08 µM) and Kv11.1 (IC = 2.44 ± 1.06 µM), and also the human subtype Kv1.6 (IC = 3.6 ± 1.04 µM). Despite its clear effects on potassium channels, it shares a high sequence identity with δ-like-AtVIA and δ-TsVIA. Also, κO-SrVIA is the third conopeptide from the venom of with effects on potassium channels, and the seventh conotoxin that blocks Kv1.6 channels.

摘要

从来自墨西哥湾的食虫物种的毒液中鉴定并表征了第一个影响 EAG 家族电压门控钾通道的 conotoxin。这种 conopeptide，最初命名为 Cs68，后来被指定为 κO-SrVIA，是极其疏水的，由 31 个氨基酸残基组成，包括框架 VI/VII 中的六个半胱氨酸和游离的 C 末端。它抑制两种人类 EAG 亚型 Kv10.1（IC = 1.88 ± 1.08 μM）和 Kv11.1（IC = 2.44 ± 1.06 μM）以及人类亚型 Kv1.6（IC = 3.6 ± 1.04 μM）介导的电流。尽管它对钾通道有明显的影响，但它与 δ-like-AtVIA 和 δ-TsVIA 具有很高的序列同一性。此外，κO-SrVIA 是第三种来自毒液的对钾通道有影响的 conotoxin，也是第七种阻断 Kv1.6 通道的 conotoxin。