Abstract:
:The scorpion toxin peptide BeKm-1 was synthesised by fluorenylmethoxycarbonyl solid phase chemistry and folded by air oxidation. The peptide's effects on heterologous human ether-a-go-go-related gene potassium current (I(HERG)) in HEK293 cells were assessed using 'whole-cell' patch clamp. Blockade of I(HERG) by BeKm-1 was concentration-dependent, temperature-dependent, and rapid in onset and reversibility. Blockade also exhibited inverse voltage dependence, inverse dependence on duration of depolarisation, and reverse use- and frequency-dependence. Blockade by BeKm-1 and recombinant ergtoxin, another scorpion toxin known to block HERG, differed in their recovery from HERG current inactivation elicited by strong depolarisation and in their ability to block HERG when the channels were already activated. We conclude that synthetic BeKm-1 toxin blocks HERG preferentially through a closed (resting) state channel blockade mechanism, although some open channel blockade also occurs.
journal_name
FEBS Lettjournal_title
FEBS lettersauthors
Milnes JT,Dempsey CE,Ridley JM,Crociani O,Arcangeli A,Hancox JC,Witchel HJdoi
10.1016/s0014-5793(03)00662-8keywords:
subject
Has Abstractpub_date
2003-07-17 00:00:00pages
20-6issue
1-3eissn
0014-5793issn
1873-3468pii
S0014579303006628journal_volume
547pub_type
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