IMPROVEMENT OF HEAD-TO-TAIL RGD PEPTIDE CYCLIZATION EFFICIENCY COMBINING LOW TEMPERATURE AND LITHIUM CHLORIDE

Adriana Gauna, Fredys Sanchez-Hoyos, Maycol Huerta, Marcelo J. Kogan, Eyleen Araya

Producción científica: Contribución a una revistaArtículorevisión exhaustiva

Resumen

RGD-containing peptides (linear and cyclic) have been developed to target some types of cancer cells through interaction with the αvβ3 Integrin. Due to their reduced conformational freedom, cyclic peptides exhibit improved metabolic stability and binding affinity/specificity to their molecular targets. However, macrocyclization is considered a significant synthetic challenge that is affected by the ring size, peptide sequence, and reaction conditions, making tetra- and pentapeptides more difficult to cyclize. In this work, we report some optimized cyclization conditions for the obtention of a cyclic RGDfK peptide that combine the use of low reaction temperature and the addition of LiCl, a combination not yet reported that resulted in a reduction of the formation of oligomers and an improvement of the cyclization efficiency.

Idioma originalInglés
Páginas (desde-hasta)6038-6041
Número de páginas4
PublicaciónJournal of the Chilean Chemical Society
Volumen69
N.º1
DOI
EstadoPublicada - 2024

Áreas temáticas de ASJC Scopus

  • Química General

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