Heterochannels Kv(1.1-1.2)2 and their interactions with pore blockers

Efremenko, A.V.; Kryukova, E.V.; Kazakov, O.V.; Ignatova, A.A.; Shmatin, I.I.; Korabeynikova, V.N.; Toporova, V.A.; Yakimov, S.A.; Kirpichnikov, M.P.; Nekrasova, O.V.; Feofanov, A.V.

Авторы: Efremenko A.V., Kryukova E.V., Kazakov O.V., Ignatova A.A., Shmatin I.I., Korabeynikova V.N., Toporova V.A., Yakimov S.A., Kirpichnikov M.P., Nekrasova O.V., Feofanov A.V.
Журнал: Cells
Том: 14
Год издания: 2025
Издательство: MDPI
Местоположение издательства: Basel, Switzerland
Номер статьи: 1364
DOI: 10.3390/cells14171364
Аннотация: Heterotetramerization of Kv1.1 and Kv1.2 α-subunits expands the functional diversity ofvoltage-gated potassium Kv1 channels in the central nervous system (CNS), thus necessitating the study of the properties of these heterochannels, including their interactions withligands. We report on the expression, electrophysiological, and ligand-binding propertiesof human heterochannels Kv(1.1-1.2)2 formed by dimeric concatemers Kv1.1-Kv1.2 fusedwith fluorescent protein mKate2 in Neuro-2a cells. Kv(1.1-1.2)2 is a low-voltage-activated,highly active, non-inactivating channel with a fast activation rate. Its activation rate andhalf-maximum activation voltage are similar to that of the Kv1.1 channel, but differ from that of Kv1.2. This suggests that the membrane expression of Kv(1.1-1.2)2 may functionally compensate for the absence of membrane presentation of homotetrameric Kv1.1 channelsin CNS. Hongotoxin 1 fused with fluorescent protein GFP (HgTx-G) is shown to be apore-blocking ligand of Kv(1.1-1.2)2 with a dissociation constant of 100 pM. Using confocalmicroscopy and competitive binding assay, HgTx-G and cells expressing Kv(1.1-1.2)2, the apparent dissociation constants of the complexes between Kv(1.1-1.2)2 and peptides Ce1,Ce4, hongotoxin 1, MeKTx11-1, agitoxin 2, charybdotoxin, and scyllatoxin were evaluated to be 14, 33, 40, 250, 800, and >>3300 pM, respectively. Heterotetramerization ofα-subunits has a different effect on the affinity of ligands compared to those for Kv1.1 andKv1.2 channels.
Добавил в систему: Феофанов Алексей Валерьевич

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