Laboratory of Drug Discovery Science

We have the expertise and motivation necessary for basic medical science and advanced drug discovery science, yielding collaborative and successful R&D projects, under the supports of a series of external fundings, including Japan Agency for Medical Research and Development (AMED), Japan Science and Technology Agency (JST), Japan Society for the Promotion of Science (JSPS) etc.
We have a broad background in molecular biology, biochemistry and expertise in structural biology, especially X-ray crystallography using synchrotron radiation (SPring-8) and NMR. Our current research is focused on the tertiary structure analysis of cancer-driver gene products by using the conventional technics of structural biology as described above and also X-ray free electron laser (XFEL/SACLA) which visualizes time-resolved structural changes in the drug-target protein crystals (Fig.1).

Further, the structural data collected these fifteen years are effectively utilized for the development of anti-cancer drugs targeting the oncogene products including Ras. Kobe compounds which are small molecule Ras inhibitors developed by us are published in PNAS (2013), and one of them, called Kobe0065, is currently sold by Sigma-Aldrich and TOCRIS (movies1).

In addition, the patent of another type of Ras inhibitors developed by the collaborative R&D with the domestic pharmaceutical companies are filed in USA as US9056862 (2016).
Moreover, in silico screening of Ras inhibitors as described above brought an unexpected but fruitful outgrowth i.e., the discovery of novel Ras/MAPK signaling inhibitors （PCT/JP2022/29379）whose R&D is now on going in our lab (Fig.2).