ABSTRACT Biosynthesis, utilizing highly evolved enzymes, achieves exceptional efficiency and precise stereo‐control under mild conditions. In contrast, chemical synthesis provides stability, flexibility, and broad applicability, enabling numerous transformations beyond natural metabolism. Although these two systems have complementary strengths and appear to operate under different synthetic philosophies, recent decades have revealed the exciting opportunities of integration strategy in molecular synthesis. Considering the fact that catalysis is the key of synthesis, this perspective highlights some representative examples in catalysis where chemistry and biology mutually inspire and extend one another. For chemical synthesis, biomimetic catalysis has evolved from coenzyme‐inspired small‐molecule systems to peptide frameworks and sophisticated metal complexes that replicate enzymatic logic, achieving efficiency and selectivity rivaling or surpassing natural enzymes. Conversely, chemical inspiration has reshaped biosynthesis through artificial metalloenzymes, enzyme repurposing, photoenzymatic catalysis, and dual chemo‐biocatalysis, thereby greatly expanding enzymat
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