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Peng, Y. Enzyme Inhibition. Encyclopedia. Available online: https://encyclopedia.pub/entry/61052 (accessed on 02 November 2026).
Peng Y. Enzyme Inhibition. Encyclopedia. Available at: https://encyclopedia.pub/entry/61052. Accessed November 02, 2026.
Peng, Yu. "Enzyme Inhibition" Encyclopedia, https://encyclopedia.pub/entry/61052 (accessed November 02, 2026).
Peng, Y. (2026, October 17). Enzyme Inhibition. In Encyclopedia. https://encyclopedia.pub/entry/61052
Peng, Yu. "Enzyme Inhibition." Encyclopedia. Web. 17 October, 2026.
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Enzyme Inhibition
EditEnzyme inhibition is the reduction of an enzyme-catalyzed reaction rate through an interaction that restricts substrate binding, catalytic turnover, or the availability of active enzyme. Reversible inhibitors associate with particular states of the catalytic cycle, producing kinetic patterns related to their binding relationships with enzyme and substrate [1]. Covalent inhibitors form a chemical bond with the target protein and can produce persistent inhibition after free inhibitor has been removed [2]. Inhibition can be examined by measuring product formation or by testing competition with a probe that labels an active enzyme. Such competition measurements also reveal inhibition across enzyme populations in a biological sample [3][4]. The chemical reactivity and recognition properties of a covalent inhibitor govern which residues and target proteins it modifies [5].
enzyme kinetics
reversible inhibition
irreversible inhibition
enzyme–inhibitor complex
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References
- Geoffrey A. Holdgate; Thomas D. Meek; Rachel L. Grimley; Mechanistic Enzymology in Drug Discovery: A Fresh Perspective. Nat. Rev. Drug Discov. 2017, 17, 115-132. [CrossRef]
- Juswinder Singh; Russell C. Petter; Thomas A. Baillie; Adrian Whitty; The Resurgence of Covalent Drugs. Nat. Rev. Drug Discov. 2011, 10, 307-317. [CrossRef]
- Benjamin F. Cravatt; Aaron T. Wright; John W. Kozarich; Activity-Based Protein Profiling: From Enzyme Chemistry to Proteomic Chemistry. Annu. Rev. Biochem. 2008, 77, 383-414. [CrossRef]
- Micah J. Niphakis; Benjamin F. Cravatt; Enzyme Inhibitor Discovery by Activity-Based Protein Profiling. Annu. Rev. Biochem. 2014, 83, 341-377. [CrossRef]
- Keriann M. Backus; Bruno E. Correia; Kenneth M. Lum; Stefano Forli; Benjamin D. Horning; Gonzalo E. González-Páez; Sandip Chatterjee; Bryan R. Lanning; John R. Teijaro; Arthur J. Olson; Dennis W. Wolan; Benjamin F. Cravatt; Proteome-wide Covalent Ligand Discovery in Native Biological Systems. Nature 2016, 534, 570-574. [CrossRef]
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Biochemistry & Molecular Biology
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