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• W2032037185 abstract "The cloning of KCa2 channels revealed three subtypes, with each displaying distinct but partially overlapping expression distributions in the mammalian CNS and periphery. Activation of KCa2 channels leads to membrane hyperpolarization and inhibition of action potential firing. Block of KCa2 channels has been suggested as a novel target for cognitive enhancement, depression, myotonic muscular dystrophy and heart arrhythmias. It is clear however, that blockers selective for individual KCa2 channel subtypes would be required to be therapeutically useful. KCa2 channel current is blocked by apamin, with the bee venom toxin being unusual in displaying some selectivity between KCa2 channel subtypes. This suboptimal selectivity is not sufficient to be therapeutically useful and the toxin has been shown in vivo to have a very narrow therapeutic window. Mutational and molecular modelling studies of the KCa2 channels are beginning to determine how selective block might be achieved. Mutagenesis has indicated the importance of the outer pore region and the extracellular loop between transmembrane domains S3 and S4 for block of KCa2 current by apamin. Mapping the sequence of transmembrane domains S5, pore helix and S6 onto the crystal structures of KcsA, MthK and Kv1.2 has provided an approximation of the pore structure. This approach has allowed structural modelling of the interactions between toxins and channel, demonstrating that the toxins that show little discrimination between KCa2 channel subtypes interact with the outer pore and around the K+ selectivity filter. We present the structural modelling of the interaction of apamin and KCa2.2, which is superimposed onto the crystal structure of Kv1.2. This has shown that apamin interacts only with the outer pore and does not come into contact with channel's selectivity filter. It is clear that by comparing how different toxins interact with each KCa2 channel subtype, a detailed picture will be generated that will aid the development of more specific KCa2 channel blockers." @default.
• W2032037185 created "2016-06-24" @default.
• W2032037185 creator A5002091267 @default.
• W2032037185 creator A5029781869 @default.
• W2032037185 creator A5030969256 @default.
• W2032037185 creator A5083648229 @default.
• W2032037185 date "2010-07-01" @default.
• W2032037185 modified "2023-10-15" @default.
• W2032037185 title "Small conductance calcium-activated potassium channels: From structure to function" @default.
• W2032037185 cites W132626488 @default.
• W2032037185 cites W1490915066 @default.
• W2032037185 cites W1512465642 @default.
• W2032037185 cites W1523536119 @default.
• W2032037185 cites W1525085839 @default.
• W2032037185 cites W1542049838 @default.
• W2032037185 cites W1643706501 @default.
• W2032037185 cites W1812802776 @default.
• W2032037185 cites W1953088445 @default.
• W2032037185 cites W1963624422 @default.
• W2032037185 cites W1964991820 @default.
• W2032037185 cites W1969992726 @default.
• W2032037185 cites W1970196869 @default.
• W2032037185 cites W1970277917 @default.
• W2032037185 cites W1972090163 @default.
• W2032037185 cites W1973383177 @default.
• W2032037185 cites W1974260774 @default.
• W2032037185 cites W1979530856 @default.
• W2032037185 cites W1980205307 @default.
• W2032037185 cites W1982593576 @default.
• W2032037185 cites W1983519301 @default.
• W2032037185 cites W1984417726 @default.
• W2032037185 cites W1985095190 @default.
• W2032037185 cites W1985108182 @default.
• W2032037185 cites W1987369275 @default.
• W2032037185 cites W1988049420 @default.
• W2032037185 cites W1990571474 @default.
• W2032037185 cites W1990705961 @default.
• W2032037185 cites W1990798621 @default.
• W2032037185 cites W1993938009 @default.
• W2032037185 cites W1995888798 @default.
• W2032037185 cites W1997867282 @default.
• W2032037185 cites W1998469634 @default.
• W2032037185 cites W1998719957 @default.
• W2032037185 cites W2000629783 @default.
• W2032037185 cites W2005317840 @default.
• W2032037185 cites W2005927608 @default.
• W2032037185 cites W2006710293 @default.
• W2032037185 cites W2006839087 @default.
• W2032037185 cites W2006957979 @default.
• W2032037185 cites W2007310802 @default.
• W2032037185 cites W2008320401 @default.
• W2032037185 cites W2011944068 @default.
• W2032037185 cites W2014968048 @default.
• W2032037185 cites W2020405692 @default.
• W2032037185 cites W2020551068 @default.
• W2032037185 cites W2020626643 @default.
• W2032037185 cites W2021801605 @default.
• W2032037185 cites W2022062323 @default.
• W2032037185 cites W2026065951 @default.
• W2032037185 cites W2027864023 @default.
• W2032037185 cites W2033908484 @default.
• W2032037185 cites W2033948669 @default.
• W2032037185 cites W2034611255 @default.
• W2032037185 cites W2035845442 @default.
• W2032037185 cites W2036686141 @default.
• W2032037185 cites W2037132191 @default.
• W2032037185 cites W2038251790 @default.
• W2032037185 cites W2039793331 @default.
• W2032037185 cites W2041315703 @default.
• W2032037185 cites W2042216906 @default.
• W2032037185 cites W2042670053 @default.
• W2032037185 cites W2042685214 @default.
• W2032037185 cites W2043822158 @default.
• W2032037185 cites W2046771994 @default.
• W2032037185 cites W2047353734 @default.
• W2032037185 cites W2049100140 @default.
• W2032037185 cites W2050216084 @default.
• W2032037185 cites W2051642210 @default.
• W2032037185 cites W2055025881 @default.
• W2032037185 cites W2056581537 @default.
• W2032037185 cites W2059680732 @default.
• W2032037185 cites W2061260058 @default.
• W2032037185 cites W2061784042 @default.
• W2032037185 cites W2065693649 @default.
• W2032037185 cites W2066070661 @default.
• W2032037185 cites W2071052205 @default.
• W2032037185 cites W2073049800 @default.
• W2032037185 cites W2076074044 @default.
• W2032037185 cites W2082309756 @default.
• W2032037185 cites W2084303869 @default.
• W2032037185 cites W2085169889 @default.
• W2032037185 cites W2091417303 @default.
• W2032037185 cites W2091499426 @default.
• W2032037185 cites W2094587000 @default.
• W2032037185 cites W2095952083 @default.
• W2032037185 cites W2097151900 @default.
• W2032037185 cites W2099587101 @default.
• W2032037185 cites W2101692831 @default.

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