Abstract: Traditional genetics, based on the central dogma, has established the fundamental framework of protein function. However, numerous complex regulatory processes in living systems cannot be fully explained by genetic sequences alone, as the central dogma has limitations in elucidating their underlying mechanisms. Chemical biology provides a transformative research paradigm by employing small molecules to directly interact with and modulate biomacromolecules, thereby decoding intricate life processes. Using Chapter 14 (“Chemical Regulation of Life Processes”) from the “101 Plan” Chemical Biology textbook as an example, this study proposes an instructional framework structured along a spatial hierarchy from the extracellular to intracellular level (“cell membrane → cytoplasm → nucleus”). Through representative case studies, the framework systematically demonstrates how chemical biology deciphers complex biological processes following the logical progression of “phenomenon → mechanism → translation”. Case analyses and extended discussions enable students to not only consolidate core knowledge but also develop chemical biology thinking that spans target identification, mechanistic investigation, functional modulation, and therapeutic intervention.

Key words: Chemistry “101 Plan”, Chemical biology, Course design