1. Targeted protein degradation PROTAC (proteolysis targeting chimera)

We developed a novel strategy for small molecule drug discovery, in which, degradation of target proteins is based on the use of small hybrid molecules composed of a ligand for the target protein and another for ubiquitin ligase. These hybrid small molecules direct the ubiquitin ligase towards the target protein, leading to selective degradation by the ubiquitin-proteasome system. In addition, we demonstrated that this strategy could be an effective therapeutic approach for neurodegenerative diseases.
J. Am. Chem Soc. 2010, 132, 5820.　Angew. Chem. Int. Ed. 2017, 56, 11530.

1. Improvement in pharmacokinetics of bioactive molecules 

Aqueous solubility is essential for drug candidates, and improving aqueous solubility of bioactive compounds is a major concern for medicinal chemists. We have proposed strategies for improving aqueous solubility by modifying molecules using certain methods that would decrease intermolecular interaction. Our results indicate that these strategies can increase the aqueous solubility of molecules although their hydrophobicities increase concomitantly.
J. Med. Chem. 2011, 54, 1539.
The Practice of Medicinal Chemistry (Forth Edition)  Elsevier

• Targeted protein degradation PROTAC (proteolysis targeting chimera）

• Improvement in druglikeness of bioactive molecules