3-Substituted-4-methoxy-5-hydroxybenzaldehydes and benzoic acids as inhibitors of catechol-O-methyltransferase

  • Ronald T. Borchardt
  • Joan A. Huber


The extraneuronal inactivation of catecholamines and the detoxification of many xenobiotic catechols are dependent upon the enzyme catechol-O-methyltransferase (COMT, EC COMT is a soluble, magnesium-requiring enzyme which catalyzes the transfer of a methyl group from S-adenosylmethionine (SAM) to a catechol substrate resulting in the formation of the meta and para-O-methylated products (Borchardt, 1980).


Sulfide Dopamine Disulfide Catecholamine Monoamine 


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  1. Borchardt, R. T., Cheng, C. F. and Thakker, D. R. (1975). Purification of Catechol-O-Methyltransferase by Affinity Chromatography. Biochem. Biophys. Res. Commun., 63, 69–77.Google Scholar
  2. Borchardt, R. T. and Thakker, D. R. (1976). Evidence for Sulfhydryl Groups at the Active Site of Catechol-O-Methyltransferase. Biochim. Biophys. Acta, 445, 498–509.Google Scholar
  3. Borchardt, R. T. (1977). Chemical Probes of the Active Site of Catechol-O-Methyltransferase. In Biochemistry and Function of Monoamine Enzymes, (ed., E. Usdin and N. Weiner), Marcel Dekker, New York, p. 707–720.Google Scholar
  4. Borchardt, R. T. (1980). N- and O-Methylation. In Enzymatic Basis of Detoxication, Vol. II, Wiley, New York, p. 43–62.Google Scholar
  5. Borchardt, R. T. (1981). Catechol-O-Methyltransferase: Assay, Purification and Properties. In Methods in Enzymology - Detoxication and Drug Metabolism: Conjugation and Related Systems, (ed., W. B. Jakoby), Academic Press, New York, in press.Google Scholar
  6. Guldberg, H. C. and Marsden, C. A. (1975). Catechol-O-Methyltransferase: Pharmacological Aspects and Physioloqical Role. Pharmacol. Rev., 27, 135–206.Google Scholar
  7. Lutz, W. B., Creveling, C. R., Daly, J. W. and Witkop, B. (1972). Sulfur Analogs of Dopamine and Norepinephrine. Inhibition of Catechol-O-Methyltransferase. J. Med. Chem., 15, 795–802.Google Scholar
  8. Nikodejevic, B., Senoh, S., Daly, J. W. and Creveling, C. R. (1970). Catechol-O-Methyltransferase. II. A New Class of Inhibitors of Catechol-O-Methyltransferase; 3,5-Dihydroxy-4-Methoxybenzoic Acid and Related Compounds. J. Pharmacol. Exptl. Therap., 174, 83–93.Google Scholar

Copyright information

© The Contributors 1981

Authors and Affiliations

  • Ronald T. Borchardt
    • 1
  • Joan A. Huber
    • 1
  1. 1.Department of BiochemistryUniversity of KansasLawrenceUnited Kingdom

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