Magnetic particles for enzyme immobilization: A versatile support for ligand screening

Enzyme inhibitors represent a substantial fraction of all small molecules currently in clinical use. Therefore, the early stage of drug-discovery process and development efforts are focused on the identification of new enzyme inhibitors through screening assays. The use of immobilized enzymes on solid supports to probe ligand-enzyme interactions have been employed with success not only to identify and characterize but also to isolate new ligands from complex mixtures. Between the available solid supports, magnetic particles have emerged as a promising support for enzyme immobilization due to the high superficial area, easy separation from the reaction medium and versatility. Particularly, the ligand fishing assay has been employed as a very useful tool to rapidly isolate bioactive compounds from complex mixtures, and hence the use of magnetic particles for enzyme immobilization has been widespread. Thus, this review provides a critical overview of the screening assays using immobilized enzymes on magnetic particles between 2006 and 2021.