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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.

SUBMITTER: White JD

PROVIDER: S-EPMC4130293 | biostudies-literature | 2013 Aug

REPOSITORIES: biostudies-literature

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Picazoplatin, an azide-containing platinum(II) derivative for target analysis by click chemistry.

White Jonathan D JD Osborn Maire F MF Moghaddam Alan D AD Guzman Lindsay E LE Haley Michael M MM DeRose Victoria J VJ

Journal of the American Chemical Society 20130806 32

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-f ...[more]

PMID: 23879391

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