1,2,3-Triazoles as Amide Bond Mimics: Triazole Scan Yields Protease-Resistant Peptidomimetics for Tumor Targeting

1,2,3-Triazoles as Amide Bond Mimics: Triazole Scan Yields Protease-Resistant Peptidomimetics for Tumor Targeting

The triazole makes the difference: Replacement of amide bonds in the backbone of peptides by 1,4‐disubstituted 1,2,3‐triazole isosteres affords peptidomimetics with retained receptor affinity and cell‐internalization properties, enhanced proteolytic stability, and improved tumor‐targeting capabiliti...

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Veröffentlicht in:Angewandte Chemie International Edition 2013-08, Vol.52 (34), p.8957-8960
Hauptverfasser: Valverde, Ibai E., Bauman, Andreas, Kluba, Christiane A., Vomstein, Sandra, Walter, Martin A., Mindt, Thomas L.
Format: Artikel
Sprache:eng
Schlagworte:
Affinity
Amides
Backbone
Bonding
click chemistry
drug delivery
Humans
metabolic stabilization
Neoplasms - chemistry
Neoplasms - immunology
peptidomimetics
Peptidomimetics - chemistry
radiopharmaceuticals
Receptors
Stability
Triazoles
Triazoles - chemistry
Tumors
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Beschreibung
Zusammenfassung:The triazole makes the difference: Replacement of amide bonds in the backbone of peptides by 1,4‐disubstituted 1,2,3‐triazole isosteres affords peptidomimetics with retained receptor affinity and cell‐internalization properties, enhanced proteolytic stability, and improved tumor‐targeting capabilities.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201303108