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Acetylating, Deacetylating and Amino Acid Conjugating Enzymes

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Concepts in Biochemical Pharmacology

Abstract

Foreign compounds, including many different amines and carboxylic acids, undergo acylation in mammalian species and, in the process, are converted to amide conjugates prior to excretion. Acylation reactions are catalyzed by enzymes (acyltransferases) which are specific for the foreign compound and involve co-enzyme A (CoA-SH) derivatives. These reactions are of two general types. In the first type, foreign amines are acylated by acetyl-S-CoA to form acetylated derivatives: \( C{H_3}CO - S - CoA\,\, + \,\,R - N{H_2}\,\frac{{N - acetyltransferase}}{{}} \to \,CoA - SH\,\, + \,\,R - NH - COC{H_3} \) In the second type, foreign carboxylic acids are converted in the presence of ATP and CoA to acyl-S-CoA derivatives which acylate glycine or another endogenous amino acid: \( CoA - SH\,\, + \,\,R - COOH\,\frac{{\mathop {Activating}\limits_{enzyme} }}{{ATP}} \to \,\,R - CO - S - CoA\,\, + \,{H_2}O \) \( R - CO - S - CoA\,\, + \,\,{H_2}NC{H_2}COOH\,\frac{{Acyltransferase}}{{}} \to \,CoA - SH\,\, + \,\,R - CO - HNC{H_2}COOH \) The properties of the acyltransferases which catalyze these reactions in mammalian tissues and the factors which modify their activity will be discussed in this chapter. Enzymes which catalyze the acetylation of drugs and other foreign compounds will be considered first, and discussion of deacetylating enzymes will be included with them.

Career Scientist of the Health Research Council of the City of New York, Contract 1-441.

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  1. Wendell W. Weber
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  1. Department of Health, Education and Welfare, National Institutes of Health, Bethesda, MD, 20014, USA

    Bernard B. Brodie  & James R. Gillette  & 

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Weber, W.W. (1971). Acetylating, Deacetylating and Amino Acid Conjugating Enzymes. In: Brodie, B.B., Gillette, J.R., Ackerman, H.S. (eds) Concepts in Biochemical Pharmacology. Handbook of Experimental Pharmacology / Handbuch der experimentellen Pharmakologie, vol 28 / 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-65177-9_33

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