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Can I read Design and Characterization of a Pyridone-Containing EZH2 Inhibitor Phosphate Prodrug on EtoBox?
Design and Characterization of a Pyridone-Containing EZH2 Inhibitor Phosphate Prodrug by Pei-Pei Kung; Connie Fan; Hovhannes J. Gukasyan; Buwen Huang; Susan Kephart; Manfred Kraus; Joseph H. Lee; Scott C. Sutton; Shinji Yamazaki; Luke Zehnder is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Design and Characterization of a Pyridone-Containing EZH2 Inhibitor Phosphate Prodrug about?
A pyridone-derived phosphate prodrug of an enhancer of zeste homolog 2 (EZH2) inhibitor was designed and synthesized to improve the inhibitor's aqueous solubility. This prodrug (compound ) was profiled in pharmacokinetic experiments to assess its ability to deliver the corresponding parent compound (compound ) to animals following oral administration. Results from these studies showed that the prodrug was efficiently converted to its parent compound . In separate experiments, the prodrug demonstrated impressive tumor growth inhibition in a diffuse large B-cell lymphoma Karpas-422 cell line-derived xenograft model. The described prodrug strategy is expected to be generally applicable to poorly soluble pyridone-containing EZH2 inhibitors and provides a new option to enable such compounds to achieve sufficiently high exposures .
Who reads Design and Characterization of a Pyridone-Containing EZH2 Inhibitor Phosphate Prodrug?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Pei-Pei Kung; Connie Fan; Hovhannes J. Gukasyan; Buwen Huang; Susan Kephart; Manfred Kraus; Joseph H. Lee; Scott C. Sutton; Shinji Yamazaki; Luke Zehnder
- Publisher
- American Chemical Society (ACS)
- Published
- 2021
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)