- Chemoenzymatic routes to enantiomerically pure 2-azatyrosine and 2-, 3- and 4-pyridylalanine derivatives
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Enantiomerically pure 2-, 3- or 4-pyridylalanine (pya) and 2-azatyrosine (azatyr) are known to present various biological activities. After incorporation into appropriate peptide sequences, these heterocyclic non natural α-amino acids could behave as new substrates or inhibitors of elastase from Pseudomonas aeruginosa. This enzyme is known to be involved in nosocomial infections and infections related to the cystic fibrosis disease. New efficient chemoenzymatic preparations of those compounds using α-chymotrypsin (α-CT) are presented. Springer-Verlag 2011.
- Moussa, Amer,Meffre, Patrick,Martinez, Jean,Rolland, Valerie
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p. 1339 - 1348
(2012/09/07)
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- Potential mechanism-based tyrosine kinase inhibitors. Part 2. Design and synthesis of peptides containing heterocyclic tyrosine analogues
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The Fmoc derivatives of two homochiral tyrosine analogues, a pyridine N-oxide and a pyridone, have been prepared in high stereochemical purity.Solid-phase synthesis has been used to prepare a decapeptide substrate for the tyrosine kinase domain of epidermal growth factor.Two decapeptides, which incorporate the tyrosine analogues in place of tyrosine, and thereby have the potential to act as mechanism-based inhibitors of epidermal growth factor tyrosine kinase, have been synthesised and found to inhibit the aforementioned kinase.
- Andrews, David M.,Gregoriou, Mary,Page, Timothy C. M.,Peach, Josephine M.,Pratt, Andrew J.
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p. 1335 - 1340
(2007/10/02)
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