Title : Mechanism of IRK1 channel block by intracellular polyamines.

Pub. Date : 2000 Jun

PMID : 10828252






6 Functional Relationships(s)
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1 Mechanism of IRK1 channel block by intracellular polyamines. Polyamines potassium inwardly rectifying channel subfamily J member 2 Homo sapiens
2 Intracellular polyamines inhibit the strongly rectifying IRK1 potassium channel by a mechanism different from that of a typical ionic pore blocker such as tetraethylammonium. Polyamines potassium inwardly rectifying channel subfamily J member 2 Homo sapiens
3 Furthermore, contrary to the expectation for a nonpermeant ionic pore blocker, a significant residual IRK1 current persists at very positive membrane voltages; the amplitude of the residual current decreases with increasing polyamine concentration. Polyamines potassium inwardly rectifying channel subfamily J member 2 Homo sapiens
4 This complex blocking behavior of polyamines can be accounted for by a minimal model whereby intracellular polyamines inhibit the IRK1 channel by inducing two blocked channel states. Polyamines potassium inwardly rectifying channel subfamily J member 2 Homo sapiens
5 This complex blocking behavior of polyamines can be accounted for by a minimal model whereby intracellular polyamines inhibit the IRK1 channel by inducing two blocked channel states. Polyamines potassium inwardly rectifying channel subfamily J member 2 Homo sapiens
6 The proposal that polyamines traverse the pore at finite rates is supported by the observation that philanthotoxin-343 (spermine with a bulky chemical group attached to one end) acts as a nonpermeant ionic blocker in the IRK1 channel. Polyamines potassium inwardly rectifying channel subfamily J member 2 Homo sapiens