title: LDV peptidomimetics equipped with biotinylated spacer-arms: synthesis and biological evaluation on CCRF-CEM cell line.
abstract: The tripeptide Leu-Asp-Val (LDV) is known to bind α(4)β(1) 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 α(4)β(1) integrin in an adhesion assay using fluorescently labeled, α(4)β(1) integrin-expressing leukemia CCRF-CEM cells. Furthermore, when bound to neutravidin-coated plates, compound 9 could capture CCRF-CEM cells. Such biotin-conjugated LDV peptidomimetic may thus represent a novel tool for biotechnological applications using avidin interaction for leukapheresis or leukemia cell targeting.
authors.affiliation: Université catholique de Louvain (UCL), Institut de la Matière Condensée et des Nanosciences, Bâtiment Lavoisier, Place L. Pasteur, L4.01.02, B-1348 Louvain-la-Neuve, Belgium.
authors.forename: Estelle
authors.initials: E
authors.lastname: Gérard
authors.forename: Aline
authors.initials: A
authors.lastname: Meulle
authors.forename: Olivier
authors.initials: O
authors.lastname: Feron
authors.forename: Jacqueline
authors.initials: J
authors.lastname: Marchand-Brynaert
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology; D001710:Biotin / Q000737:chemistry; D002448:Cell Adhesion; D002460:Cell Line; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D015973:Gene Expression Regulation, Leukemic; D006801:Humans; D020128:Inhibitory Concentration 50; D039041:Integrin alpha4beta1 / Q000378:metabolism; D007700:Kinetics; D007938:Leukemia / Q000378:metabolism; D008956:Models, Chemical; D009842:Oligopeptides / Q000737:chemistry*; D010455:Peptides / Q000737:chemistry; D057786:Peptidomimetics / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D039041:Integrin alpha4beta1; D009842:Oligopeptides; D010455:Peptides; D057786:Peptidomimetics; C090763:leucyl-aspartyl-valine; D001710:Biotin