Method for Identifying Novel Telomerase Inhibitors with Utility in Cancer Treatment
Life Sciences : Materials and Compounds
Available for licensing
- Sean Kerwin, Ph.D. , College of Pharmacy
- Oleg Fedoroff, Ph.D. , College of Pharmacy
- Miguel Salazar, Ph.D. , College of Pharmacy
- Laurence Hurley, Ph.D. , University of Arizona
Certain sequences of DNA are able to form unique, G-quadruplex structures. These structures are implicated in a variety of biological processes. One example of such a process is the cancer-cell specific elongation of chromosome telomeres by the enzyme telomerase. G-quadruplex structures have also been implicated in the transcriptional control of specific genes, and in inherited diseases such as fragile X syndrome.
These compounds are inhibitors of the cancer-cell specific telomerase and have potential as anticancer agents.
Lack of toxicity: due to the high level of G-quadruplex DNA binding selectivity, these compounds are non-cytotoxic in acute cell toxicity studies, and in mice in vivo.
Novel mode of action: In addition to inhibiting the cancer cell specific enzyme telomerase, these compounds may have more immediate effects on disrupting telomere function in cancer cells.Selectivity: This class of compounds is the most selective G-quadruplex interactive agents known, with G-quadruplex DNA to double-stranded DNA binding selectivity of up to one-thousand-fold.
Proof of concept
- 3 foreign patents application filed