Russ. J. Bioorganic Chem., 2020, 46(6):1011-1017

Kv1 Potassium Channel Ligands Based On Hongotoxin 1 and Red Fluorescent Protein

Recombinant chimeras of hongotoxin 1 (HgTx1) fused through the N - or C-terminus with the redfluorescent protein TagRFP, RFP-HgTx1 and HgTx1-RFP were obtained. The properties of these fluores-cent chimeras as ligands of potassium voltage-gated Kv1 channels were studied using bioengineered cell sys-tems based on hybrid channels KcsA-Kv1.x (x = 1, 3, 6). It is shown that HgTx1-RFP and RFP-HgTx1 arehigh-affinity ligands of the external pore blocker binding sites of the Kv1.x (x = 1, 3) channels, and HgTx1-RFP is superior in activity to RFP-HgTx1. No specific interactions of HgTx1-RFP and RFP-HgTx1 withKcsA-Kv1. 6 were detected. It has been demonstrated that HgTx1-RFP and RFP-HgTx1 can be used in theKcsA-Kv1.x (x = 1, 3)-based cellular systems to search for Kv1.x (x = 1, 3) channel blockers and estimate theiraffinity.

Primak AL, Skutel MA, Nekrasova OV, Arseniev AS, Kirpichnikov MP, Feofanov AV

Department of structural biology, Laboratory of biomolecular NMR-spectroscopy, Laboratory of optical microscopy and spectroscopy of biomolecules, Bioengineering department, Laboratory of protein engineering

: 10.1134/S1068162020060266
Scopus: 2-s2.0-85098124318
IBCH: 8940
Кол-во цитирований на 07.2024: 3
Данные статьи проверены модераторами 2020-12-03

Список научных проектов, где отмечена публикация

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