Poster abstracts

Poster number 7 submitted by Xun Bao

Synthesis, characterization, and reactivity of cisplatin analogues

Xun Bao (Wayne State University, Department of Chemistry, Detroit, MI 48202, USA), Keshab Rijal (National Institutes of Health, Eunice Kennedy Shriver National Institute of Child Health and Human Development, Bethesda, MD 20892, USA), Jun Jiang (Wayne State University, Department of Chemistry, Detroit, MI 48202, USA), M. T. Rodgers (Wayne State University, Department of Chemistry, Detroit, MI 48202, USA), Christine S. Chow (Wayne State University, Department of Chemistry, Detroit, MI 48202, USA)

Abstract:
As well established in the central dogma, RNA functions as a key component in the middle of the genetic information transformation chain. With its extensive functional roles and accessible location in the cytoplasm, RNA has been considered as an ideal drug target. Among the variable RNAs, ribosomal RNA (rRNA) has drawn the most attention. Compared to other RNAs, it has a relatively large size with a high level of structural diversity, and its activity directly affects cell survival.
The first FDA-approved, platinum-based anticancer drug, cisplatin, has been widely used in clinical antitumor treatment. Its anticancer activity and mechanism have been throughly studied, and genomic DNA is identified as its primary target; however, recent studies have shown that cisplatin can coordinate and accumulate more rapidly on the RNA than DNA, especially within the ribosome. Without protection of the nucleus or repair mechanisms, RNA has better accessibility as well as sustained adducts compared to DNA. It has been hypothesized that if platinum-based drugs can be modified to target and knock down RNA activity, dose-related side effects can be greatly eliminated. In a previous study, cisplatin was used as a probe to detect the accessible sites in structured RNA. These probing results provided valuable information about the overall

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Keywords: ribosome, cisplatin analogue, mass spectrometry