Here is a review of 50 approved drugs in the US.¹⁾ In 2021, 29 small-molecule drugs appeared in the fields of oncologic, CNS, anti-infective etc.. This review is significantly stimulating for chemistry folks because the synthetic routes of small-molecule drugs are summarized in a simple fashion. Scientists would enjoy the art of synthetic schemes, which...

Visual analysis of proteins and molecule structures is a powerful methodology for better understanding and prediction of potential interactions and drug designs. In the field of PPIs, structural information of peptidomimetics is crucial for rapid drug discovery through designing a precise mimic of a protein or a peptide of interest. We developed two distinctive and...

Novel technologies and strategies bring up beautiful sprouts of innovation. In our recent paper1, a two-step strategy for designing a small molecule was demonstrated by collaboration with GeneFrontier through the integration of respective technologies. This is a fantastic example of synergy creation, leveraging each strength to develop a new and practical strategy. GeneFrontier has unique...

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...