| 摘要 |
<p>This invention relates to derivatives of the conopeptide MII, an α-4/7 conotoxin peptide, in which amino acid residues are substituted as described herein while maintaining the basic activity of MII. The present invention also relates to the discovery of the 3-dimensional structure of MII, and the relationship of its structure to its specificity to the α3β2 subtype of the neuronal nicotinic acetylcholine receptor (nAChR). The present invention also relates to computer based programs for the expression of the three-dimensional structure of MII and peptide analogs, peptide mimetics or non-peptide mimetics thereof. The structural characteristics may be correlated with biological activity to enable the design of α-4/7 conotoxin peptide analogs and peptide mimetics which demonstrate the same specificity to neuronal nAChR. Such analogs and peptide mimetics are useful as cardiovascular agents and for treating or detecting small-cell lung carcinoma (SCLC).</p> |
