In drug discovery, different methods exist to create new inhibitors possessing satisfactory biological activity. The multisubstrate adduct inhibitor (MAI) approach is one of these methods, which consists of a covalent combination between analogs of the substrate and the cofactor or of the multiple substrates used by the target enzyme. Adopted as the first line of investigation for many enzymes, this method has brought insights into the enzymatic mechanism, structure, and inhibitory requirements. In this review, the MAI approach, applied to different classes of enzyme, is reported from the point of view of biological activity.
|Number of pages||28|
|Journal||Journal of Enzyme Inhibition and Medicinal Chemistry|
|Publication status||Published - Dec 2009|
Le Calvez, P. B., Scott, C., & Migaud, M. (2009). Multisubstrate adduct inhibitors: Drug design and biological tools. Journal of Enzyme Inhibition and Medicinal Chemistry , 24(6), 1291-1318. https://doi.org/10.3109/14756360902843809