This project focuses on the research and development of small molecule drugs. With the support of the National Major New Drug Creation, Key R&D Program, and the Macau Science and Technology Development Fund, after more than 20 years, it has established a two-way research model for small molecule drugs of “effective monomer establishment → new target discovery and new target discovery → new molecule innovative drugs”, and has achieved the transformation of 2 first-in-class innovative drugs, creating a new model for new drug research and development. The main technical content of this project includes the discovery, design, synthesis, screening, delivery and evaluation of small molecule drug targets, as well as related production and quality control technologies, and will realize industrial production. Technique 1): Discovery of effective small molecule leonurine from leonurus, target confirmation and drug development Technique 2): Discovery of key targets for the production of hydrogen sulfide (H₂S) in vivo and development of new small molecule drug SPRC. Technique 3): Discovery of epigenetic key target SMYD3 and targeted drug development.

Fig 1 Effective monomer establishment → new target discovery and new target discovery → new molecule innovative drugs

Fig 2 Target-based drug screening and activity studies