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Beyond hemostasis: a snake venom serine protease with potassium channel blocking and potential antitumor activities

Sci Rep. 2020; 
Johara Boldrini-França, Ernesto Lopes Pinheiro-Junior, Steve Peigneur, Manuela Berto Pucca, Felipe Augusto Cerni, Rafael Junqueira Borges, Tássia Rafaella Costa, Sante Emmanuel Imai Carone, Marcos Roberto de Mattos Fontes, Suely Vilela Sampaio, Eliane Candiani Arantes, Jan Tytgat
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Mutagenesis Services … use. Expression and purification of mutant Collinein-1 (rCollinein-mut). rCollinein-mut coding gene was synthesized and cloned into XhoI and NotI restriction sites of pPICZαA vector by GenScript®(New Jersey, USA). The recombinant … Get A Quote

摘要

Snake venom serine proteases (SVSPs) are complex and multifunctional enzymes, acting primarily on hemostasis. In this work, we report the hitherto unknown inhibitory effect of a SVSP, named collinein-1, isolated from the venom of Crotalus durissus collilineatus, on a cancer-relevant voltage-gated potassium channel (hEAG1). Among 12 voltage-gated ion channels tested, collinein-1 selectively inhibited hEAG1 currents, with a mechanism independent of its enzymatic activity. Corroboratively, we demonstrated that collinein-1 reduced the viability of human breast cancer cell line MCF7 (high expression of hEAG1), but does not affect the liver carcinoma and the non-tumorigenic epithelial breast cell lines (HepG2 and MCF... More

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