Journal
TOXINS
Volume 6, Issue 3, Pages 892-913Publisher
MDPI
DOI: 10.3390/toxins6030892
Keywords
potassium channels; scorpion venom; alpha-KTx; neurotoxins; Tityus serrulatus
Categories
Funding
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP, The State of Sao Paulo Research Foundation) [2008/10761-0, 2012/13590-8]
- ConselhoNacional de DesenvolvimentoCientifico e Tecnologico (CNPq, The NationalCouncil for Scientific and Technological Development) [402508/2012-2, 133881/2010-5]
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES, Coordination of the Advancement of Higher Education
- PDEE) [MBP-BEX 1095/11-0]
- F.W.O. Vlaanderen [G.0433.12]
- Inter-University Attraction Poles Program, Belgian State, Belgian Science Policy [IUAP 7/10]
- KULeuven [OT/12/081]
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [12/13590-8] Funding Source: FAPESP
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In Brazil, Tityus serrulatus (Ts) is the species responsible for most of the scorpion related accidents. Among the Ts toxins, the neurotoxins with action on potassium channels (alpha-KTx) present high interest, due to their effect in the envenoming process and the ion channel specificity they display. The alpha-KTx toxins family is the most relevant because its toxins can be used as therapeutic tools for specific target cells. The improved isolation method provided toxins with high resolution, obtaining pure Ts6 and Ts7 in two chromatographic steps. The effects of Ts6 and Ts7 toxins were evaluated in 14 different types of potassium channels using the voltage-clamp technique with two-microelectrodes. Ts6 toxin shows high affinity for Kv1.2, Kv1.3 and Shaker IR, blocking these channels in low concentrations. Moreover, Ts6 blocks the Kv1.3 channel in picomolar concentrations with an IC50 of 0.55 nM and therefore could be of valuable assistance to further designing immunosuppressive therapeutics. Ts7 toxin blocks multiple subtypes channels, showing low selectivity among the channels analyzed. This work also stands out in its attempt to elucidate the residues important for interacting with each channel and, in the near future, to model a desired drug.
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