Discovery of KV1.3 ion channel inhibitors: Medicinal chemistry approaches and challenges

Š Gubič, LA Hendrickx, Ž Toplak… - Medicinal research …, 2021 - Wiley Online Library
Abstract The KV1. 3 voltage‐gated potassium ion channel is involved in many physiological
processes both at the plasma membrane and in the mitochondria, chiefly in the immune and …

Treating autoimmune disorders with venom-derived peptides

B Shen, Z Cao, W Li, JM Sabatier… - Expert opinion on …, 2017 - Taylor & Francis
Introduction: The effective treatment of autoimmune diseases remains a challenge. Voltage-
gated potassium Kv1. 3 channels, which are expressed in lymphocytes, are a new …

Characterization and chemical synthesis of Cm39 (α-KTx 4.8): a scorpion toxin that inhibits voltage-gated K+ channel KV1. 2 and small-and intermediate-conductance …

MU Naseem, G Gurrola-Briones, MR Romero-Imbachi… - Toxins, 2023 - mdpi.com
A novel peptide, Cm39, was identified in the venom of the scorpion Centruroides
margaritatus. Its primary structure was determined. It consists of 37 amino acid residues with …

Kv1. 3: a multifunctional channel with many pathological implications

A Serrano-Albarrás, I Estadella… - Expert opinion on …, 2018 - Taylor & Francis
Ion channels are transmembrane proteins that form aqueous pores driving ions through the
plasma membrane in favor of an electrochemical gradient. Thus, voltage-dependent …

The Kv1.3 K+ channel in the immune system and its “precision pharmacology” using peptide toxins

Z Varga, G Tajti, G Panyi - Biologia futura, 2021 - Springer
Since the discovery of the Kv1. 3 voltage-gated K+ channel in human T cells in 1984, ion
channels are considered crucial elements of the signal transduction machinery in the …

A Fluorescent Peptide Toxin for Selective Visualization of the Voltage-Gated Potassium Channel KV1.3

DCC Wai, MU Naseem, G Mocsár… - Bioconjugate …, 2022 - ACS Publications
Upregulation of the voltage-gated potassium channel KV1. 3 is implicated in a range of
autoimmune and neuroinflammatory diseases, including rheumatoid arthritis, psoriasis …

Fighting rheumatoid arthritis: Kv1. 3 as a therapeutic target

A Serrano-Albarrás, S Cirera-Rocosa, D Sastre… - Biochemical …, 2019 - Elsevier
Rheumatoid arthritis (RA) is a serious autoimmune disease that has severe impacts on both
the wellbeing of patients and the economy of the health system. Similar to many …

Investigation of the molecular details of the interactions of selenoglycosides and human galectin-3

M Raics, ÁK Balogh, C Kishor, I Timári… - International Journal of …, 2022 - mdpi.com
Human galectin-3 (h Gal-3) is involved in a variety of biological processes and is implicated
in wide range of diseases. As a result, targeting h Gal-3 for clinical applications has become …

[HTML][HTML] sVmKTx, a transcriptome analysis-based synthetic peptide analogue of Vm24, inhibits Kv1. 3 channels of human T cells with improved selectivity

A Csoti, RCN Meza, F Bogár, G Tajti, TG Szanto… - Biochemical …, 2022 - Elsevier
Abstract Kv1. 3 K+ channels play a central role in the regulation of T cell activation and Ca
2+ signaling under physiological and pathophysiological conditions. Peptide toxins targeting …

Optimization of Pichia pastoris Expression System for High-Level Production of Margatoxin

MU Naseem, G Tajti, A Gaspar, TG Szanto… - Frontiers in …, 2021 - frontiersin.org
Margatoxin (MgTx) is a high-affinity blocker of voltage-gated potassium (Kv) channels. It
inhibits Kv1. 1–Kv1. 3 ion channels in picomolar concentrations. This toxin is widely used to …