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Drug Discovery at the Enzyme Level

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Drug Discovery and Development

Abstract

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.

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Authors
  1. Ray W. Fuller
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  2. Larry R. Steranka
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Editor information

Editors and Affiliations

  1. Drug Discovery Administration, Pharmaceuticals Division, Ciba-Geigy Corporation, Summit, New Jersey, USA

    Michael Williams

  2. Biomedical Research Department, Stuart Pharmaceuticals, ICI Americas Inc., Wilmington, Delaware, USA

    Jeffrey B. Malick

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© 1987 The Humana Press Inc.

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Fuller, R.W., Steranka, L.R. (1987). Drug Discovery at the Enzyme Level. In: Williams, M., Malick, J.B. (eds) Drug Discovery and Development. Humana Press. https://doi.org/10.1007/978-1-4612-4828-6_7

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  • DOI: https://doi.org/10.1007/978-1-4612-4828-6_7

  • Publisher Name: Humana Press

  • Print ISBN: 978-1-4612-9180-0

  • Online ISBN: 978-1-4612-4828-6

  • eBook Packages: Springer Book Archive

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