PPI-targeted drug discovery strategy is intriguing field. Target identification and functional modulation are crucial for new drug discovery and development. Assay development, technological improvements of structural biology and bioinformatics allowed us to rapidly identify the target so far, even though there are still challenges. Target-based drug discovery is a current standard, and a project often...

How do you think about PPI? It’s of interest by many pharmaceutical companies as well as scientists for long but few drugs have developed so far. PPI field is still a chaos and needs more intensive research. We are trying to establish a confirmed PPI drug discovery & development methodology as a leading company. Protein-protein...

Transition from a macrocyclic peptide to a small molecule with the desired activity is still a huge challenge in drug discovery and development. Here is an interesting strategy “Peptide-to-Small Molecule” developed by Shionogi Pharma Co., Ltd., where small molecules are generated by pharmacophore-guided de novo design from macrocyclic peptides.1 Macrocyclic peptides are goldmines for drug...

Science has solved numerous issues relating to disease treatment through the discovery of new drugs. Small synthetic molecules, natural products, antibodies, and nucleic acids have been developed into candidates through the aid of SBDD (structure-based drug design) and HTS (high-throughput screening) approaches. Tremendous efforts have been thrown into molecular target drugs, but about 85% of...