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Recent studies on dendrotoxins and potassium ion channels

Harvey, A L (1997) Recent studies on dendrotoxins and potassium ion channels. General pharmacology, 28 (1). pp. 7-12. ISSN 0306-3623

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Dendrotoxins are small proteins isolated from mamba (Dendroaspis) snake venoms. They block some subtypes of voltage-dependent potassium channels in neurons. Dendrotoxins contain 57-60 amino acid residues crosslinked by three disulfide bridges. They are homologous to Kunitz-type serine protease inhibitors, such as aprotinin, although they have little or no antiprotease activity. Dendrotoxins act mainly on neuronal K+ channels. Studies with cloned K+ channels indicate that alpha-dendrotoxin from green mamba Dendroaspis angusticeps blocks Kv1.1 and Kv1.2 channels in the nanomolar range. In native cells, dendrotoxin appears preferentially to block inactivating forms of K+ current. Dendrotoxins can induce repetitive firing in neurons and facilitate transmitter release. On direct injection to the CNS, dendrotoxins can induce epileptiform activity. Radiolabeled dendrotoxins are useful markers of subtypes of K+ channels in vivo, and structural analogs help to define the molecular recognition properties of different types of K+ channels.