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A. A. Mazurov T. I. Korotenko V. Ya. Gorbatyuk Yu. E. Shapiro A. V. Mazepa A. I. Dyadenko S. A. Andronati 《Russian Chemical Bulletin》1998,47(10):1960-1964
Easy lactamization of Gln(Asn)−Pro−NH2 with the formation of cyclic dipeptides with the diketopiperazine structure (mimetics of the conformational fragments of
linear tripeptides with the X−Protrans-bond) was observed in the synthesis of tripeptide Glp−Gln−Pro−NH2 modified by the replacement of histidine with obligatory similar glutamine in thyroliberin (Glp−His−Pro−NH2, TRH) and in the synthesis of its structural analog [Asn2]TRH. Ion peaks corresponding to the Glp and Pro amino acid residues were revealed in the mass spectra of the peptides synthesized.
The biological properties of the compounds obtained were determined indicating that the obligatory replacement resulted in
an increased physiological specificity of [Gln2]TRH. The enhanced activity of conformationally restricted cyclic peptides compared to linear ones suggests that the biologically
active conformation responsible for the antidepressant activity of linear TRH analogs is the conformation with X−Protrans-bond.
Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 10, pp. 2015–2020, October, 1998. 相似文献
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