芋螺肽αD-FrXXA，一种电压门控钾通道抑制剂。

The Conopeptide αD-FrXXA, an Inhibitor of Voltage-Gated Potassium Channels.

作者信息

Martínez-Hernández Luis, López-Vera Estuardo, Rodriguez-Ruiz Ximena C, Ortíz-Arellano Mónica A

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

Mar Drugs. 2025 May 30;23(6):237. doi: 10.3390/md23060237.

DOI:10.3390/md23060237

PMID:40559646

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12194669/

Abstract

The conopeptide αD-FrXXA was previously isolated by our team from the venom of the vermivorous snail . This toxin is composed of two chains of 47 amino acids and inhibits neuronal and muscular subtypes of nAChR. In this study, we explored its effects on voltage-gated potassium channels heterologously expressed in oocytes using the two-electrode voltage-clamp technique (TEVC). At a concentration of 15 μM, αD-FrXXA was able to inhibit by 50% or more the currents of four subtypes of the Kv1 subfamily and slightly inhibit (<20%) two subtypes of the EAG subfamily. The conopeptide αD-FrXXA inhibits in a concentration-dependent manner the subtypes Kv1.3 (IC 0.38 ± 0.06 μM) and Kv1.6 (IC 0.52 ± 0.14 μM). The results reported here are noteworthy because this α-conopeptide behaves similarly to the α/κJ-PlXIVA conopeptide that inhibits nAChR and Kv channels.

摘要

芋螺毒素αD-FrXXA先前由我们团队从食虫蜗牛的毒液中分离得到。这种毒素由两条含47个氨基酸的链组成，可抑制烟碱型乙酰胆碱受体（nAChR）的神经元和肌肉亚型。在本研究中，我们使用双电极电压钳技术（TEVC），探究了其对在卵母细胞中异源表达的电压门控钾通道的影响。在15 μM的浓度下，αD-FrXXA能够抑制Kv1亚家族四个亚型电流的50%或更多，并轻微抑制（<20%）EAG亚家族的两个亚型。芋螺毒素αD-FrXXA以浓度依赖的方式抑制Kv1.3（IC 0.38 ± 0.06 μM）和Kv1.6（IC 0.52 ± 0.14 μM）亚型。此处报道的结果值得关注，因为这种α-芋螺毒素的行为与抑制nAChR和Kv通道的α/κJ-PlXIVA芋螺毒素相似。