Synthesis, Bioactivity, and Cloning of the L-Type Calcium Channel Blocker ω-Conotoxin TxVII †
✍ Scribed by Sasaki, Toru; Feng, Zhong-Ping; Scott, Randolph; Grigoriev, Nikita; Syed, Naweed I.; Fainzilber, Michael; Sato, Kazuki
- Book ID
- 127383684
- Publisher
- American Chemical Society
- Year
- 1999
- Tongue
- English
- Weight
- 113 KB
- Volume
- 38
- Category
- Article
- ISSN
- 0006-2960
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We have prepared a series of biotinylated analogs of \(\omega\)-conotoxin ( \(\omega \mathrm{CgTx}\) ) as potent, selective markers for \(\mathrm{N}-\) type calcium channels. At \(\mathbf{p H} 9.5\), reaction of \(\omega \mathrm{CgTx}\) with amidocaproylbiotin succinimidyl ester gives three biotinyl
omega-Agatoxin IVA, isolated from the venom of funnel web spider Agelenopsis aperta, blocks potently and selectively P-type calcium channels. This toxin, composed of 48 amino acids and containing 8 cysteine residues, was synthesized by the solid-phase procedure. The Cys residues were protected by ac