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PMID:11522785
| Citation |
Wang, XH, Connor, M, Wilson, D, Wilson, HI, Nicholson, GM, Smith, R, Shaw, D, Mackay, JP, Alewood, PF, Christie, MJ and King, GF (2001) Discovery and structure of a potent and highly specific blocker of insect calcium channels. J. Biol. Chem. 276:40306-12 |
|---|---|
| Abstract |
We have isolated a novel family of insect-selective neurotoxins that appear to be the most potent blockers of insect voltage-gated calcium channels reported to date. These toxins display exceptional phylogenetic specificity, with at least a 10,000-fold preference for insect versus vertebrate calcium channels. The structure of one of the toxins reveals a highly structured, disulfide-rich core and a structurally disordered C-terminal extension that is essential for channel blocking activity. Weak structural/functional homology with omega-agatoxin-IVA/B, the prototypic inhibitor of vertebrate P-type calcium channels, suggests that these two toxin families might share a similar mechanism of action despite their vastly different phylogenetic specificities. |
| Links |
PubMed Online version:10.1074/jbc.M105206200 |
| Keywords |
Amino Acid Sequence; Animals; Bees/cytology; Calcium Channel Blockers/pharmacology; Insect Control/methods; Insecticides/pharmacology; Models, Molecular; Molecular Sequence Data; Neurons/drug effects; Neurotoxins/genetics; Neurotoxins/pharmacology; Nuclear Magnetic Resonance, Biomolecular; Patch-Clamp Techniques; Protein Precursors/chemistry; Recombinant Proteins/chemistry; Recombinant Proteins/pharmacology; Spider Venoms/chemistry; Spider Venoms/genetics; Spider Venoms/pharmacology; Spiders; omega-Agatoxin IVA/chemistry |
| edit table |
Significance
Annotations
| Gene product | Qualifier | GO Term | Evidence Code | with/from | Aspect | Extension | Notes | Status |
|---|---|---|---|---|---|---|---|---|
| GO:0019855: calcium channel inhibitor activity |
ECO:0000314: |
F |
Fig. 2 |
complete | ||||
|
enables |
GO:0019855: calcium channel inhibitor activity |
ECO:0000314: direct assay evidence used in manual assertion |
F |
Seeded From UniProt |
complete | |||
See also
References
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