Key result
Noxiustoxin chimeras with altered alpha-carbon backbones inhibited maxi-K channels (Kd 0.4-6 microM) unlike wild-type NxTX, suggesting the backbone controls its specificity for Kv1.3 channels.
The specificity of Noxiustoxin for Kv1.3 over maxi-K channels is controlled in part by the toxin's alpha-carbon backbone.
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Provides basis for selective Kv1.3 modulators; leaves open in vivo validation and clinical translation.
Mullmann et al. (2001) studied this question. Noxiustoxin (NxTX) mutants and chimeras vs. Wild-type NxTX was evaluated on Channel inhibition (Kd values). Noxiustoxin chimeras with altered alpha-carbon backbones inhibited maxi-K channels (Kd 0.4-6 microM) unlike wild-type NxTX, suggesting the backbone controls its specificity for Kv1.3 channels.
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