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Highly potentside‐chain toside‐chain cyclizedenkephalin analoguescontaining a carbonylbridge: synthesis,biology andconformation Danuta PawlakMarta OleszczukJacek Wójcik2001 год

Highly potent side‐chain to side‐chain cyclized enkephalin analogues containing a carbonyl bridge: synthesis, biology and conformation
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Аннотация: Abstract Six novel cyclic enkephalin analogues have been synthesized. Cyclization of the linear peptides containing basic amino acid residues in position 2 and 5 was achieved by treatment with bis(4‐nitrophenyl)carbonate. It was found that some of the compounds exibit unusually high µ ‐opioid activity in the guinea pig ileum (GPI) assay. The 18‐membered analogue cyclo( N ε , N β ′ ‐carbonyl‐𝒹‐Lys 2 ,Dap 5 )enkephalinamide turned out to be one of the most potent µ‐agonists reported so far. NMR spectra of the peptides were recorded and structural parameters were determined. The conformational space was exhaustively examined for each of them using the electrostatically driven Monte Carlo method. Each peptide was finally described as an ensemble of conformations. A model of the bioactive conformation of this class of opioid peptides was proposed. Copyright © 2001 European Peptide Society and John Wiley & Sons, Ltd.
Год издания: 2001
Авторы: Danuta Pawlak, Marta Oleszczuk, Jacek Wójcik, Maria Pachulska, Nga N. Chung, Peter W. Schiller, Jan Izdebski
Издательство: Wiley
Источник: Journal of Peptide Science
Ключевые слова: Neuropeptides and Animal Physiology, Chemical Synthesis and Analysis, Antimicrobial Peptides and Activities
Другие ссылки: Journal of Peptide Science (HTML)
PubMed (HTML)