title: Picazoplatin, an azide-containing platinum(II) derivative for target analysis by click chemistry.
abstract: Despite the broad use of platinum-based chemotherapeutics, identification of their full range of cellular targets remains a significant challenge. In order to identify, visualize, and isolate cellular targets of Pt(II) complexes, we have modified the chemotherapeutic drug picoplatin with an azide moiety for subsequent click reactivity. The new compound picazoplatin readily binds DNA and RNA oligonucleotides and undergoes facile post-labeling click reactions to alkyne-fluorophore conjugates. Pt-fluorophore click reactions in rRNA purified from drug-treated Saccharomyces cerevisiae demonstrate its potential for future in vivo efforts.
authors.affiliation: Department of Chemistry and Biochemistry and Institute of Molecular Biology, University of Oregon, Eugene, Oregon 97403-1253, USA.
authors.forename: Jonathan D
authors.initials: JD
authors.lastname: White
authors.forename: Maire F
authors.initials: MF
authors.lastname: Osborn
authors.forename: Alan D
authors.initials: AD
authors.lastname: Moghaddam
authors.forename: Lindsay E
authors.initials: LE
authors.lastname: Guzman
authors.forename: Michael M
authors.initials: MM
authors.lastname: Haley
authors.forename: Victoria J
authors.initials: VJ
authors.lastname: DeRose
mesh_terms: D000480:Alkynes / Q000737:chemistry; D001386:Azides / Q000737:chemistry* / Q000494:pharmacology; D057930:Click Chemistry; D055808:Drug Discovery; D005456:Fluorescent Dyes / Q000737:chemistry; D008958:Models, Molecular; D009841:Oligonucleotides / Q000378:metabolism; D009944:Organoplatinum Compounds / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000480:Alkynes; D001386:Azides; D005456:Fluorescent Dyes; D009841:Oligonucleotides; D009944:Organoplatinum Compounds; C110525:amminedichloro(2-methylpyridine)platinum(II)