Synthesis, Purification, and Characterization of Precursors for Pt-HDACi Adducts as Bifunctional Anticancer Agents
Faculty Mentor Name
Qinliang Zhao
Research or Creativity Area
Natural Sciences
Abstract
Cancer can be characterized by disordered cell activity. Its dynamic characteristics allows cancer cells to reprogram themselves to sustain proliferation and adapt to therapeutic stress, which creates major challenges for treatment. Therefore, modern anticancer strategies focus more on the underlying molecular mechanisms that regulate gene expression and cellular behavior. Histone deacetylases (HDACs) are zinc-dependent enzymes involved in gene regulation, and their overexpression is associated with cancer progression through transcriptional repression of tumor suppressor genes. Because HDAC inhibitors (HDACi) can promote a more transcriptionally active chromatin state and induce anticancer effects, they have emerged as promising therapeutic agents.
Cisplatin is a widely used platinum-based chemotherapeutic drug that exerts its cytotoxic effects by forming DNA crosslinks, thereby disrupting DNA replication and inducing programmed cell death. However, its clinical application is often limited by drug resistance and poor selectivity toward cancer cells. Incorporating HDAC inhibitors as ligands onto a platinum (Pt) center creates a dual-function system that may increase DNA accessibility, enhance cisplatin activity, and produce stronger anticancer effects. Overall, HDAC inhibitor–platinum combinations appear to be more effective than either agent alone, showing enhanced anticancer activity and more precise targeting of cancer cells.
Synthesis, Purification, and Characterization of Precursors for Pt-HDACi Adducts as Bifunctional Anticancer Agents
Cancer can be characterized by disordered cell activity. Its dynamic characteristics allows cancer cells to reprogram themselves to sustain proliferation and adapt to therapeutic stress, which creates major challenges for treatment. Therefore, modern anticancer strategies focus more on the underlying molecular mechanisms that regulate gene expression and cellular behavior. Histone deacetylases (HDACs) are zinc-dependent enzymes involved in gene regulation, and their overexpression is associated with cancer progression through transcriptional repression of tumor suppressor genes. Because HDAC inhibitors (HDACi) can promote a more transcriptionally active chromatin state and induce anticancer effects, they have emerged as promising therapeutic agents.
Cisplatin is a widely used platinum-based chemotherapeutic drug that exerts its cytotoxic effects by forming DNA crosslinks, thereby disrupting DNA replication and inducing programmed cell death. However, its clinical application is often limited by drug resistance and poor selectivity toward cancer cells. Incorporating HDAC inhibitors as ligands onto a platinum (Pt) center creates a dual-function system that may increase DNA accessibility, enhance cisplatin activity, and produce stronger anticancer effects. Overall, HDAC inhibitor–platinum combinations appear to be more effective than either agent alone, showing enhanced anticancer activity and more precise targeting of cancer cells.
