title: Synthesis and application of fluorescein- and biotin-labeled molecular probes for the chemokine receptor CXCR4.
abstract: The design, synthesis, and bioevaluation of fluorescence- and biotin-labeled CXCR4 antagonists are described. The modification of D-Lys8 at an epsilon-amino group in the peptide antagonist Ac-TZ14011 derived from polyphemusin II had no significant influence on the potent binding of the peptide to the CXCR4 receptor. The application of the labeled peptides in flow cytometry and confocal microscopy studies demonstrated the selectivity of their binding to the CXCR4 receptor, but not to CXCR7, which was recently reported to be another receptor for stromal cell-derived factor 1 (SDF-1)/CXCL12.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan. soishi@pharm.kyoto-u.ac.jp
authors.forename: Shinya
authors.initials: S
authors.lastname: Oishi
authors.forename: Ryo
authors.initials: R
authors.lastname: Masuda
authors.forename: Barry
authors.initials: B
authors.lastname: Evans
authors.forename: Satoshi
authors.initials: S
authors.lastname: Ueda
authors.forename: Yukiko
authors.initials: Y
authors.lastname: Goto
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Ohno
authors.forename: Akira
authors.initials: A
authors.lastname: Hirasawa
authors.forename: Gozoh
authors.initials: G
authors.lastname: Tsujimoto
authors.forename: Zixuan
authors.initials: Z
authors.lastname: Wang
authors.forename: Stephen C
authors.initials: SC
authors.lastname: Peiper
authors.forename: Takeshi
authors.initials: T
authors.lastname: Naito
authors.forename: Eiichi
authors.initials: E
authors.lastname: Kodama
authors.forename: Masao
authors.initials: M
authors.lastname: Matsuoka
authors.forename: Nobutaka
authors.initials: N
authors.lastname: Fujii
mesh_terms: D000595:Amino Acid Sequence; D001710:Biotin / Q000737:chemistry*; D002460:Cell Line; D005434:Flow Cytometry; D019793:Fluorescein / Q000737:chemistry*; D005453:Fluorescence; D005456:Fluorescent Dyes / Q000032:analysis* / Q000138:chemical synthesis* / Q000737:chemistry; D020128:Inhibitory Concentration 50; D018613:Microscopy, Confocal; D010455:Peptides / Q000032:analysis* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D019718:Receptors, CXCR4 / Q000032:analysis* / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013379:Substrate Specificity
chemical_list: D005456:Fluorescent Dyes; D010455:Peptides; D019718:Receptors, CXCR4; D001710:Biotin; D019793:Fluorescein