Top1/TDP1/TDP2 Triple Inhibitor Anticancer Agents

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In 2016, the American Cancer Society estimated 1,685,210 new cancer cases diagnosed and 595,690 cancer deaths in the U.S. There is a great need for the development of new therapies for cancer treatment. Currently, topoisomerase 1 (Top1) inhibitors are used as anticancer agents. DNA damage caused by topoisomerase 1 inhibitors needs to be repaired in order to prevent the death of tumor cells. Tyrosyl-DNA phosphodiesterase 1 and 2 (TDP1 and TDP2) can repair damaged DNA resulting from Top1 inhibitors and a variety of other DNA-damaging agents. Triple inhibitors of Top1, TDP1, and TDP2 are therefore able to damage the DNA of cancer cells and also prevent its repair, thereby causing cancer cell death.

Purdue University researchers have developed a series of azaindenoisoquinoline compounds that act as inhibitors of Top1, TDP1, and TDP2. Molecular modeling of selected target compounds bound to Top1, TDP1, and TDP2 was used to design the inhibitors and facilitate the structure-activity relationship analysis. The resulting compounds act as triple inhibitors of Top1, TDP1, and TDP2, which increases anticancer activity.

-Triple inhibitors
-Increases anticancer activity

Potential Applications:
-Cancer treatment
-Antiviral therapies
Dec 19, 2017

Dec 22, 2016
United States
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