Affinity Labelling

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Affinity Labelling

A method for studying an enzyme’s active site, by using a ligand (a so-called affinity label or Trojan horse inhibitor), which is an analogue of the normal substrate; the more label that covalently binds to the enzyme’s active site, the less active the enzyme.
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Among their topics are the role of reactive metabolites in genotoxicity, the bioactivation and inactivation of cytochrome P450 and other drug-metabolizing enzymes, intrinsically electrophilic compounds as a liability in drug discovery, the retrospective analysis of structure-toxicity relationships of drugs, experimental approaches to detecting reactive metabolites, structural alert and reactive metabolite analysis for the top 200 drugs in the US market by prescription, and mitigating toxicity risks with affinity labeling drug candidates.
By affinity labeling in vivo, the lifetime of physiologically active entities can be greatly enhanced by becoming bound to long-lived blood components.
1:00 Laura Parnas (UND): DOPAMINE TRANSPORTER LIGAND BINDING DOMAINS ANALYZED THROUGH PHOTO AFFINITY LABELING