drug discovery编辑历史

**Drug discovery** is the process by which new therapeutic molecules are identified, designed, and developed to treat or prevent diseases. It integrates multiple scientific disciplines—including medicinal chemistry, pharmacology, molecular biology, and computational modeling—to transform a biological target or disease hypothesis into a safe and effective drug candidate. The journey from initial concept to approved medication typically takes 10–15 years and involves iterative cycles of hypothesis testing, lead optimization, and preclinical validation before entering human clinical trials.

## 1 Historical background

### 1.1 Traditional approaches (serendipity and natural products)
Before the 20th century, most medicines were discovered by chance or derived from folklore remedies. Plant extracts, minerals, and animal products were used empirically. For example, digitalis from foxglove was used for heart conditions, and quinine from cinchona bark treated malaria. Early pharmacology relied on whole-organism effects, and active principles were rarely isolated.

### 1.2 Emergence of rational drug design
In the late 19th and early 20th centuries, advances in organic chemistry and physiology enabled a more systematic approach. Paul Ehrlich’s concept of the “magic bullet” led to the first synthetic drugs, such as arsphenamine for syphilis. Structure–activity relationships began to be explored, and by the mid-20th century, drug discovery incorporated receptor theory and enzyme inhibition.

### 1.3 Modern era: high-throughput screening and genomics
The 1980s and 1990s saw automation and miniaturization of assays, allowing millions of compounds to be tested rapidly against a target. The Human Genome Project (completed 2003) identified thousands of potential new drug targets. Combinatorial chemistry and later DNA-encoded libraries expanded chemical space. Today, genomics, proteomics, and systems biology inform target selection.

## 2 Core stages of drug discovery