LDV peptidomimetics equipped with biotinylated spacer-arms: Synthesis and biological evaluation on CCRF-CEM cell line

…, A Meulle, O Feron, J Marchand-Brynaert

Index: Gerard, Estelle; Meulle, Aline; Feron, Olivier; Marchand-Brynaert, Jacqueline Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 1 p. 586 - 590

Full Text: HTML

Citation Number: 6

Abstract

The tripeptide Leu-Asp-Val (LDV) is known to bind α4β1 integrin in leukemia cells. Here we have synthesized a LDV peptidomimetic equipped with a biotin-conjugated spacer-arm. Compound 9 acts as an inhibitor of the α4β1 integrin in an adhesion assay using fluorescently labeled, α4β1 integrin-expressing leukemia CCRF-CEM cells. Furthermore, when bound to neutravidin-coated plates, compound 9 could capture CCRF-CEM cells. ...