Research topics

A research group led by Associate Professor Shuntaro Takahashi and Director Naoki Sugimoto of the FIBER at Konan University has developed a design technique for molecules that bind strongly to the G-quadruplex structure at the ends of human chromosomal DNA and successfully developed new compounds for use as cancer drugs. The research results were published in Journal of the American Chemical Society. This article was also selected as a cover story. This research was conducted in international collaboration with Kyushu Institute of Technology, National NMR Center of Slovenia, University of Kolkata, India, and Academia Sinica, Taiwan.

In cancer cells, the telomere region at the end of chromosomal DNA, which controls life span, is abnormally elongated, resulting in immortalization. Therefore, the development of compounds that suppress telomere elongation is attracting attention as a cancer drug development. In this study, we focused on the fact that telomere DNA forms a G-quadruplex structure and developed a method to design molecules that bind strongly to different windings of the G-quadruplex. As a result, they succeeded in developing a compound that inhibits telomere DNA replication more than 100 times more efficiently than the telomere-binding compound (TMPyP4) that was developed earlier. By developing compounds that bind strongly to the G-quadruplex structure in a rational manner, it is expected that new drugs that eradicate cancer cells and treat cancer can be developed.

Publication of research results
The link to the Journal of the American Chemical Society is here.

The article published in the journal is
“Chemical Modulation of DNA Replication along G-Quadruplex Based on Topology-Dependent Ligand Binding”
S. Takahashi, A. Kotar, H. Tateishi-Karimata, S. Bhowmik, Z.-F. Wang, T.-C. Chang, S. Sato, S. Takenaka, J. Plavec, N. Sugimoto, J. Am. Chem. Soc., 143, 16458-16469（2021）[Selected as supplemental cover]

The Frontier Institute for Biomolecular Engineering Research (FIBER) will continue to contribute to the advancement of science and technology and to the benefit of society through research and development in the field of biochemistry.