| Autor: |
Kozlowski ES; Department of Central Nervous System Chemistry, Richard L. Gelb Center for Pharmaceutical Research and Development, Bristol-Myers Squibb, Wallingford, Connecticut, USA., Johnson G, Dischino DD, Dworetzky SI, Boissard CG, Gribkoff VK |
| Jazyk: |
angličtina |
| Zdroj: |
International journal of peptide and protein research [Int J Pept Protein Res] 1996 Aug; Vol. 48 (2), pp. 194-9. |
| DOI: |
10.1111/j.1399-3011.1996.tb00831.x |
| Abstrakt: |
The synthesis and iodination of a structural analogue of the specific large-conductance calcium-activated potassium (BK) channel blocker, iberiotoxin (IbTX), a 37-amino acid scorpion neurotoxin, is reported. The synthesis of this analogue, [Tyr5, Phe36]-IbTX, was accomplished using standard solid-phase Fmoc (9-fluorenylmethoxycarbonyl) chemistry protocols. The linear peptide was cyclized via the formation of three intramolecular disulfide bridges and subsequently iodinated at the Tyr5 position. Upon purification, the iodinated analogue, [mono-iodo-Tyr5, Phe36]-IbTX, exhibited comparable biological activity to native IbTX in blocking BK-mediated currents. These findings suggest the synthesis and use of an 125I labelled IbTX analogue for BK channel localization in autoradiography experiments. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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