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A new class of HDAC inhibitors with a new metal-binding group

详细技术说明

Project ID:  D2018-08 Background Cancer is group of diseases characterized by uncontrolled growth of abnormal cells. Selectivity towards cancer cells has been challenging, resulting in treatment options with severe side effects. Histone deacetylases (HDAC) are highly expressed in cancer cells and have been investigated for cancer drug development. Out of the four anticancer drugs approved by the US FDA, three compounds consist of a hydroxamate as the metal-binding group. They are not selective and bind to many different metallo-proteins causing side effects, such as lymphopenia, neutropenia, thrombocytopenia, prolonged QT, nausea, and diarrhea. Therefore, there is a need for anticancer agents with improved selective activity.  Invention DescriptionResearchers at the University of Toledo have developed a new class of HDAC inhibitors incorporating a new metal-binding group. The compounds were tested at the National Cancer Institute for anti-proliferative activity in the 60 human tumor line assay and at the University of Toledo. Results were positive, and some analogues showed promising cell growth inhibitory activity and specific analogues performed exceptionally, indicating potential for a new drug candidate in the treatment of cancer. Further, the compounds caused mitotic arrest of cancer cells and also produced a unique phenotype when co-treated with an aurora B inhibitor.   Applications•       Drug candidate for cancer treatment•       HDAC inhibitor Advantages•       High specificity to cancer cells•       Fewer anticipated side effects IP Status:       Provisional Patent filed

*Abstract

*Principal Investigation

Name: Liyanaaratchige Tillekeratne, Research Professor

Department: Medicinal & Biological Chemistry

国家/地区

美国