Tuning Scorpion Toxin Selectivity: Switching From K_V1.1 to K_V1.3.

ABSTRACT: Voltage-gated potassium channels (K_Vs) perform vital physiological functions and are targets in different disorders ranging from ataxia and arrhythmia to autoimmune diseases. An important issue is the search for and production of selective ligands of these channels. Peptide toxins found in scorpion venom named KTx excel in both potency and selectivity with respect to some potassium channel isoforms, which may present only minute differences in their structure. Despite several decades of research the molecular determinants of KTx selectivity are still poorly understood. Here we analyze MeKTx13-3 (Kalium ID: α-KTx 3.19) from the lesser Asian scorpion Mesobuthus eupeus, a high-affinity K_V1.1 blocker (IC₅₀ ~2 nM); it also affects K_V1.2 (IC

SUBMITTER: Gigolaev AM 

PROVIDER: S-EPMC7358528 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature