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Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 147))

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Abstract

Voltage-gated potassium (Kv) channels play an important role in many cellular functions correlated with changes in excitability. Their functions range from the setting of basal levels of membrane potential to shaping action potentials in excitable cells (PAPAZIAN et al. 1987). About a decade ago, the first Kv channel cDNAs were cloned from Drosophila (KAMS et al. 1987; PONGS et al. 1988; TEMPEL et al. 1988) and mammals (STÜHMER et al. 1988, 1989). The cDNAs encoded -in comparison to the then known Ca-and Na-channel a-subunits-considerably smaller protein sequences. Their analysis showed that Kv a-subunits contain a membrane-spanning core region with six hydrophobic transmembrane segments (S1—S6) flanked by hydrophilic amino-and carboxyterminal sequences. They are exposed to the cytoplasmic side of the plasma membrane. Subsequently, it was shown that four Kva-subunits make up a functional Kv channel (see Fig.1) (MACKINNroN 1991). Assembly of the four subunits may occur in the form of oligo-or heteromultimers (IsACOFF et al. 1990; RUPPERSBERG et al. 1990; CHRISTIE et al. 1990). In fact, assembly of Kva-subunits to heteromultimers appears to be a wide spread phenomenon in eukaryotic cells, making it difficult to correlate native potassium outward-currents with cloned Kv channel subunits. Nevertheless, heterologous expression studies with cloned Kv channel subunits have shown that the various homo-and heteromultimeric Kv channel assemblies may mediate the whole spectrum of rapidly-to non-inactivating outward currents observed in physiological studies.

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Pongs, O., Legros, C. (2000). Pharmacology of Voltage-Gated Potassium Channels. In: Endo, M., Kurachi, Y., Mishina, M. (eds) Pharmacology of Ionic Channel Function: Activators and Inhibitors. Handbook of Experimental Pharmacology, vol 147. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-57083-4_7

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