title: Reversible Michael additions: covalent inhibitors and prodrugs.
abstract: Covalent inhibition is an efficient molecular mechanism for inhibiting enzymes or modulating the function of proteins and is found in the action of many drugs and biologically active natural products. However, it is has been less appreciated that the formation of covalent bonds can be reversible or irreversible. This review focuses on biologically active compounds that are Michael acceptors and how the reversible nature of the Michael addition reaction influences biological activity and how this can be exploited in designing prodrugs.
authors.affiliation: Center for Molecular Pathology, Lund University, University Hospital MAS, Entrance 78, S-205 02 Malmö, Sweden. martin_h.johansson@med.lu.se
authors.forename: Martin H
authors.initials: MH
authors.lastname: Johansson
mesh_terms: D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D011355:Prodrugs / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D011355:Prodrugs