title: Synthesis and evaluation of cell-permeable biotinylated PU-H71 derivatives as tumor Hsp90 probes.
abstract: The attachment of biotin to a small molecule provides a powerful tool in biology. Here, we present a systematic approach to identify biotinylated analogues of the Hsp90 inhibitor PU-H71 that are capable of permeating cell membranes so as to enable the investigation of Hsp90 complexes in live cells. The identified derivative 2g can isolate Hsp90 through affinity purification and, as we show, represents a unique and useful tool to probe tumor Hsp90 biology in live cells by affinity capture, flow cytometry and confocal microscopy. To our knowledge, 2g is the only reported biotinylated Hsp90 probe to have such combined characteristics.
authors.affiliation: Molecular Pharmacology and Chemistry Program, Sloan-Kettering Institute, 1275 York Avenue, New York, NY 10065, USA.
authors.forename: Tony
authors.initials: T
authors.lastname: Taldone
authors.affiliation: Molecular Pharmacology and Chemistry Program, Sloan-Kettering Institute, 1275 York Avenue, New York, NY 10065, USA.
authors.forename: Anna
authors.initials: A
authors.lastname: Rodina
authors.affiliation: Molecular Pharmacology and Chemistry Program, Sloan-Kettering Institute, 1275 York Avenue, New York, NY 10065, USA.
authors.forename: Erica M
authors.initials: EM
authors.lastname: DaGama Gomes
authors.affiliation: Molecular Pharmacology and Chemistry Program, Sloan-Kettering Institute, 1275 York Avenue, New York, NY 10065, USA.
authors.forename: Matthew
authors.initials: M
authors.lastname: Riolo
authors.affiliation: Molecular Pharmacology and Chemistry Program, Sloan-Kettering Institute, 1275 York Avenue, New York, NY 10065, USA.
authors.forename: Hardik J
authors.initials: HJ
authors.lastname: Patel
authors.affiliation: Molecular Pharmacology and Chemistry Program, Sloan-Kettering Institute, 1275 York Avenue, New York, NY 10065, USA.
authors.forename: Raul
authors.initials: R
authors.lastname: Alonso-Sabadell
authors.affiliation: Molecular Pharmacology and Chemistry Program, Sloan-Kettering Institute, 1275 York Avenue, New York, NY 10065, USA.
authors.forename: Danuta
authors.initials: D
authors.lastname: Zatorska
authors.affiliation: Molecular Pharmacology and Chemistry Program, Sloan-Kettering Institute, 1275 York Avenue, New York, NY 10065, USA.
authors.forename: Maulik R
authors.initials: MR
authors.lastname: Patel
authors.affiliation: Molecular Pharmacology and Chemistry Program, Sloan-Kettering Institute, 1275 York Avenue, New York, NY 10065, USA.
authors.forename: Sarah
authors.initials: S
authors.lastname: Kishinevsky
authors.affiliation: Molecular Pharmacology and Chemistry Program, Sloan-Kettering Institute, 1275 York Avenue, New York, NY 10065, USA.|Department of Medicine, Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, New York, NY 10065, USA.|Department of Pharmacology, Weill Graduate School of Medical Sciences, 1300 York Avenue, New York, NY 10065, USA.
authors.forename: Gabriela
authors.initials: G
authors.lastname: Chiosis
keywords: PU-H71; affinity capture; biotin; flow cytometry; fluorescence microscopy; tumor Hsp90