gptx-1 toxin and its application

Abstract

The invention primarily relates to Grammostola porter(Gptx-1) toxin and an application thereof. The polypeptide toxin can block Nav1.7 (an alpha subunit family of a voltage-gated sodium channel) effectively and selectively, so that the toxin can be used as a selective sodium ion channel blocking agent which is applied to the fields of molecular mechanism of the related Nav1.7 sodium ion channel, neural signal transfer, disease treatment and the like.

Description

technical field [0001] The present invention relates to a polypeptide substance and its use in medicine preparation, in particular to a polypeptide toxin capable of effectively and selectively blocking Nav1.7 (a voltage-gated sodium channel α subunit family) and its use. Background technique [0002] Voltage-gated sodium channels (VGSCs) are widely distributed and expressed in various tissues of both vertebrates and invertebrates. VGSCs play an important role in the generation and burst of action potentials and in the transmission of nerve signals. Many diseases are closely related to voltage-gated sodium ion channels, such as pain, epilepsy and so on. [0003] VGSCs are high molecular weight, multi-transmembrane glycoproteins on excitatory cell membranes. In 2003, the International Pharmacological Federation announced the nomenclature of VGSCs. The English abbreviation (NaV) means a voltage-sensitive sodium ion channel, where Na stands for a sodium ion channel, and V sta...

AI Technical Summary

Problems solved by technology

[0007] Currently used sodium channel blockers, such as carbamazepine, lidocaine, and the above-mentioned polypeptide toxins, have multiple types of non-selective effects on sodium channels, which easily cause central and circulatory side effects (such as dizziness, ataxia, insomnia, nausea and headache, etc.), or have defects of low effectiveness and low safety, thus limiting their clinical application and widespread use

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