Article
Segmental exchanges define 4-aminopyridine binding and the inner mouth of K+ pores.
Neuron - 1 Sept 1993
Kirsch G E, Shieh C C, Drewe J A, Vener D F, Brown A M
Abstract excerpt
4-Aminopyridine (4AP) blocks the intracellular mouth of voltage-gated K+ channels. We identified critical regions for 4AP binding with chimeric channels in which segments of a low affinity clone (Kv2.1, IC50 = 18 mM) were replaced with those of a high affinity clone (Kv3.1, IC50 = 0.1 mM). 4AP sensitivity was not transferred with the S5-S6 linker (pore or P region). Instead, a chimera of the cytoplasmic half of...
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