Drug Discovery Chemistry Platform Unit

The main objective of our unit is to identify small molecule drug candidates suitable for animal safety studies and following human clinical trials. Our dedicated scientists conduct lead compound generation, and multi-dimensional lead compound optimization on potency to target receptor/enzyme, PKPD profiles, and off-target activities through SAR development. Capitalizing on RIKEN's available expertise in X-ray crystal structure analysis, in-silico modeling studies, and HTS, we strive to expedite the drug discovery process by rational drug design. Our unit is also responsible for material support for our biochemistry and pharmacology colleagues for assay development and proof-of-concept experiments.

Research Fields

Chemistry / Biology & Biochemistry / Pharmacology & Toxicology

Research Subjects

• Small molecule drug discovery by medicinal chemistry

Publications

1. * Koyama, H.; Miller, D. J.; Boueres, J. K.;
   (2R)-2-Ethylchromane-2-carboxylic Acids: Discovery of Novel PPARα/γ Dual Agonists as Antihyperglycemic and Antihyperlipidemic Agents
   J. Med. Chem. 2004, 47, 3255-3263
2. * Koyama, H.; Boueres, J. K.; Han, W.;
   5-Aryl thiazolidine-2, 4-dione as Selective PPARγ Agonists
   Bioorg. Med. Chem. Lett. 2003, 13, 1801-1803
3. * Koyama, H.; Boueres, J. K.; Miller, D. J.;
   "(2R)-2-Methylchromane-2-carboxylic Acids: Discovery of Selective PPARαAgonists as Hypolipidemic Agents
   Bioorg. Med. Chem. Lett. 2005, 15(14), 3347-3351