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Enzyme Inhibitors: Comparison
Please note this is a comparison between Version 1 by Yu Peng and Version 2 by Yu Peng.

Enzyme inhibitors are substances that reduce enzyme activity by interacting with an enzyme or a state of its catalytic cycle. Reversible binding can obstruct substrate association or alter the ability of a substrate-bound enzyme to complete turnover. The relationship between inhibitor binding and the reaction sequence produces characteristic inhibition kinetics [1][2]. Covalent inhibitors possess chemical groups capable of forming a bond with a residue in the target protein [3]. Their selectivity can be assessed across multiple enzymes by measuring competition with activity-based probes, which report accessible, reactive enzyme sites [4]. Recognition interactions position the inhibitor near a susceptible residue, while the inhibitor's reactive group participates in bond formation. Together, these features determine the target engagement and persistence of covalent inhibition [5].

  • inhibitor binding
  • enzyme kinetics
  • partial inhibition
  • enzyme inactivation

Enzyme function and inhibition·Molecular Biology·Biochemistry, Genetics and Molecular Biology·Life Sciences

References

  1. Rona R. Ramsay; Keith F. Tipton; Assessment of Enzyme Inhibition: A Review with Examples from the Development of Monoamine Oxidase and Cholinesterase Inhibitory Drugs. Molecules 2017, 22, 1192. [CrossRef]
  2. 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]
  3. Juswinder Singh; Russell C. Petter; Thomas A. Baillie; Adrian Whitty; The Resurgence of Covalent Drugs. Nat. Rev. Drug Discov. 2011, 10, 307-317. [CrossRef]
  4. Micah J. Niphakis; Benjamin F. Cravatt; Enzyme Inhibitor Discovery by Activity-Based Protein Profiling. Annu. Rev. Biochem. 2014, 83, 341-377. [CrossRef]
  5. 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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