Potassium channel blockers from the venom of the Brazilian scorpion Tityus serrulatus (Lutz and Mello, 1922)

被引:16
作者
Martin-Eauclaire, Marie-France [1 ]
Pimenta, Adriano M. C. [2 ]
Bougis, Pierre E. [1 ]
De Lima, Maria-Elena [2 ]
机构
[1] Aix Marseille Univ, CNRS, CRN2M, UMR7286, F-13344 Marseille, France
[2] Univ Fed Minas Gerais, Inst Ciencias Biol, Dept Bioquim & Imunol, Lab Venenos & Toxinas Anim, BR-31270901 Belo Horizonte, MG, Brazil
关键词
Potassium channels; Tityus serrulatus; Scorpion toxins; Blockers; CA2+-ACTIVATED K+ CHANNELS; MOVING PIECES; THERAPEUTIC TARGET; ALPHA-DENDROTOXIN; PEPTIDE TOXINS; APAMIN-BINDING; HIGH-AFFINITY; BETA-TOXIN; RAT-BRAIN; PURIFICATION;
D O I
10.1016/j.toxicon.2016.06.016
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Potassium (K+) channels are trans-membrane proteins, which play a key role in cellular excitability and signal transduction pathways. Scorpion toxins blocking the ion-conducting pore from the external side have been invaluable probes to elucidate the structural, functional, and physio-pathological characteristics of these ion channels. This review will focus on the interaction between K+ channels and their peptide blockers isolated from the venom of the scorpion Tityus serrulatus, which is considered as the most dangerous scorpion in Brazil, in particular in Minas-Gerais State, where many casualties are described each year. The primary mechanisms of action of these K+ blockers will be discussed in correlation with their structure, very often non-canonical compared to those of other well known K+ channels blockers purified from other scorpion venoms. Also, special attention will be brought to the most recent data obtained by proteomic and transcriptomic analyses on Tityus serrulatus venoms and venom glands. (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码:253 / 265
页数:13
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