Drug Discovery at the Enzyme Level

  • Ray W. Fuller
  • Larry R. Steranka


This chapter deals with enzymes as targets of drug action. The focus is on inhibition of enzyme activity by drugs, although other actions of drugs on enzymes are possible, such as activation or allosteric modification of enzyme function. This chapter will not deal with enzymes themselves as drugs, e. g., L-asparaginase in the treatment of acute lymphocytic leukemia, papain used for proteolysis in wound debridement, and urokinase used in thrombolytic therapy. Metabolism of drugs by enzymes and inhibition or induction of drug-metabolizing enzymes are other drug-enzyme interactions that can be important considerations in drug development, but our focus will be entirely on drug inhibition of enzymes as a primary mechanism to which drugs owe their efficacy. We will consider how enzyme activity is assayed, how inhibitors are found (or made) and characterized, how enzyme inhibition is demonstrated in vivo, and some specific examples of enzyme inhibitors that are used as drugs.


Enzyme Inhibitor Drug Discovery Xanthine Oxidase Monoamine Oxidase Competitive Inhibitor 
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© The Humana Press Inc. 1987

Authors and Affiliations

  • Ray W. Fuller
  • Larry R. Steranka

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