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活性位点(英语:Active site),又称激活位置,是指一个酵素中具有催化能力与结合的部位。其结构与化学性质可供底物辨识,并与底物结合。激活位置通常是酵素表面上一个类似口袋的区域,内部含有可与特定底物发生反应的残基





由Emil Fischer提出的,他的假设是说酵素的活性位点和底物可以很完美的结合,当两者结合,底物的修饰就开始了。


由Daniel Koshland提出的,它是锁钥理论的延伸,但它主张活性位点和底物不会完美结合,且活性位点是可以形状改变到和底物完美结合的状态;当底物接上后,诱导形状改变,当底物离开后,酵素回到它原本的样子。







例子 和活性位点结合? 降低反应速率?
竞争可逆型 HIV蛋白酶抑制剂
非竞争可逆型 重金属 不会
不可逆型 氰化物


辨认活性位点,在药学上很重要;借由辨认出活性位点,设计出底物(药物),可以阻断它和底物结合;其中一个重要的因子在药物设计,是抑制剂和酵素结合的强度。 例如AIDS





  1. ^ Alberts, B (2010). Essential Cell Biology. Garland Science. p. 91.
  2. ^ Campbell, P (2006). Biochemistry Illustrated. Elsevier. pp. 83–85.
  3. ^ Kool ET (1984). "Active site tightness and substrate fit in DNA replication". Annual Review of Biochemistry 71: 191–219. doi:10.1146/annurev.biochem.71.110601.135453.
  4. ^ a b Sullivan SM (2008). "Enzymes with lid-gated active sites must operate by an induced fit mechanism instead of conformational selection". Proceedings of the National Academy of Sciences of the United States of America 105: 13829–13834. doi:10.1073/pnas.0805364105.
  5. ^ a b Schechter I (2005). "Mapping of the active site of proteases in the 1960s and rational design of inhibitors/drugs in the 1990s". Current Protein and Peptide Science 6: 501–512. doi:10.2174/138920305774933286.
  6. ^ a b c DeDecker BS (2000). "Allosteric drugs: thinking outside the active-site box". Chemistry and Biology 7: 103–107. doi:10.1016/S1074-5521(00)00115-0.
  7. ^ Zuercher M (2008). "Structure-Based Drug Design: Exploring the Proper Filling of Apolar Pockets at Enzyme Active Sites". Journal of Organic Chemistry 73: 4345–4361. doi:10.1021/jo800527n.
  8. ^ Powers R (2006). "Comparison of protein active site structures for functional annotation of proteins and drug design". Proteins - Structure, Function and Bioinformatics 65: 124–135. doi:10.1002/prot.21092.
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