Abstract:
:The structural specificity of alpha-PMTX, a novel peptide toxin derived from wasp venom has been studied on the neuromuscular synapse in the walking leg of the lobster. alpha-PMTX is known to induce repetitive action potentials in the presynaptic axon due to sodium channel inactivation. We synthesized 29 analogs of alpha-PMTX by substituting one or two amino acids and compared threshold concentrations of these mutant toxins for inducing repetitive action potentials. In 13 amino acid residues of alpha-PMTX, Arg-1, Lys-3 and Lys-12 regulate the toxic activity because substitution of these basic amino acid residues with other amino acid residues greatly changed the potency. Determining the structure-activity relationships of PMTXs will help clarifying the molecular mechanism of sodium channel inactivation.
journal_name
Neurosci Lettjournal_title
Neuroscience lettersauthors
Konno K,Hisada M,Naoki H,Itagaki Y,Yasuhara T,Nakata Y,Miwa A,Kawai Ndoi
10.1016/s0304-3940(00)01017-xkeywords:
subject
Has Abstractpub_date
2000-05-05 00:00:00pages
29-32issue
1eissn
0304-3940issn
1872-7972pii
S0304-3940(00)01017-Xjournal_volume
285pub_type
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