Synthesis and evaluation of cell-permeable biotinylated PU-H71 derivatives as tumor Hsp90 probes Journal Article


Authors: Taldone, T.; Rodina, A.; DaGama Gomes, E. M.; Riolo, M.; Patel, H. J.; Alonso Sabadell, R.; Zatorska, D.; Patel, M. R.; Kishinevsky, S.; Chiosis, G.
Article 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. © 2013 Taldone et al.
Keywords: flow cytometry; fluorescence microscopy; biotin; pu-h71; tumor hsp90; affinity capture
Journal Title: Beilstein Journal of Organic Chemistry
Volume: 9
ISSN: 1860-5397
Publisher: Beilstein Institute  
Date Published: 2013-03-15
Start Page: 544
End Page: 556
Language: English
PROVIDER: scopus
PMCID: PMC3628991
PUBMED: 23616796
DOI: 10.3762/bjoc.9.60
DOI/URL:
Notes: --- - "Export Date: 1 May 2013" - "CODEN: BJOCB" - ":doi 10.3762/bjoc.9.60" - "Source: Scopus"
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