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A gene called MYC has become one of the most sought after targets of cancer researchers in the world. MYC is known to stimulate tumor growth in almost all types of cancer – but successful targeting of the gene has proven to be a challenge. A project that has baffled researchers for more than three decades.
Purdue University researchers have discovered a new set of MYC G-quadruplex promoter stabilizers that have demonstrated anticancer activity in human cancer cell cultures. The discovery is published in the July 8 edition of the Journal of the American Chemical Society.
We strive to discover effective anticancer agents. The ability to incorporate the stabilizing activity of the MYC G-quadruplex promoter into existing topoisomerase I inhibitors has shown promise to make them more potent as anticancer agents and to render cancer cells less likely to become resistant to these. "
Mark Cushman, Distinguished Professor of Medicinal Chemistry at Purdue College of Pharmacy, Principal Investigator
The Purdue team has discovered potential anti-cancer agents that target the MYC G-quadruplex promoter and downregulate the expression of the MYC oncogene, overexpressed in cancer and badociated with almost every aspect of development. cancer. The work was supported by the National Cancer Institute and the National Institutes of Health.
Cushman, whose cancer research contributed to his election to the National Academy of Inventors, said he discovered a new clbad of G-quadruplex stabilizers from the MYC indenoisoquinoline promoter in collaboration with Danzhou Yang. Some of them also inhibit topoisomerase I, an enzyme that facilitates the replication of DNA and that is produced in greater amounts in cancer cells.
"The targeting of G-quadruplex promoters offers a relatively new and exciting strategy for inhibiting the critical expression of the oncogene in cancer cells," said Yang, Martha and Fred Borch Chair in Cancer Therapy. Purdue's College of Pharmacy, who led the research with Cushman. "We hope to combine the power of drugs targeting DNA and the selectivity of molecular targeted approaches for new cancer treatments."
Yang and Cushman, both members of the Purdue University Cancer Research Center, said the discovered agents could be used to help treat almost all types of cancer. Some of the technology derived from their work has been licensed to Gibson Oncology LLC by the Technology Marketing Office of the Purdue Research Foundation.
Some of the work previously developed by Cushman and his team led to the development of three anti-cancer agents undergoing clinical trials. The MYC innovation will greatly increase the interest of the scientific community for these anticancer agents and will also contribute to the understanding of their functioning.
The work aligns with the celebration of Purdue's giant leaps, recognizing the university's global advances in health as part of Purdue's 150th anniversary. This is one of the four themes of the Festival of Ideas for the year-long celebration and aims to introduce Purdue as an intellectual center for solving real problems.
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