Bioactivation to an aldehyde metabolite—Possible role in the onset of toxicity induced by the anti-HIV drug abacavir |
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Authors: | Ná dia M. Grilo,Catarina Charneira,Sofia A. Pereira,Emí lia C. Monteiro,M. Matilde Marques,Alexandra M.M. Antunes |
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Affiliation: | 1. Centro de Estudos de Doenças Crónicas (CEDOC), NOVA Medical School, Universidade NOVA, 1169-056 Lisboa, Portugal;2. Centro de Química Estrutural, Instituto Superior Técnico, Universidade de Lisboa, 1049-001 Lisboa, Portugal |
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Abstract: | Aldehydes are highly reactive molecules, which can be generated during numerous physiological processes, including the biotransformation of drugs. Several non-P450 enzymes participate in their metabolism albeit alcohol dehydrogenase and aldehyde dehydrogenase are the ones most frequently involved in this process. Endogenous and exogenous aldehydes have been strongly implicated in multiple human pathologies. Their ability to react with biomacromolecules (e.g. proteins) yielding covalent adducts is suggested to be the common primary mechanism underlying the toxicity of these reactive species. |
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Keywords: | Abacavir Aldehyde metabolite Drug bioactivation Protein adducts Cardiotoxicity Hypersensitivity reactions |
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