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Synthesis of a Biologically Active Triazole‐Containing Analogue of Cystatin A Through Successive Peptidomimetic Alkyne–Azide Ligations
Author(s) -
Valverde Ibai E.,
Lecaille Fabien,
Lalmanach Gilles,
Aucagne Vincent,
Delmas Agnès F.
Publication year - 2012
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201107222
Subject(s) - peptidomimetic , click chemistry , cycloaddition , azide , combinatorial chemistry , triazole , alkyne , chemistry , peptide , stereochemistry , organic chemistry , catalysis , biochemistry
“Click” protein : Cu I ‐catalyzed cycloaddition of azides and terminal alkynes has been applied to the successive ligations of three unprotected peptide fragments. Peptidomimetic triazole ligation (PTL, see scheme) as a new method for the chemical production of bioactive proteins is applied for the synthesis of a triazole‐containing analogue of the 97 amino acid protein cystatin A.