Protacs: a novel approach to targeted protein degradation
Author
Parikshit Shirure, Pankaj Itamale, Sneha Jadhav, Nandini Bajaj
Abstract
Targeted protein degradation utilizing PROTACs technology is a possible therapeutic technique for treating disorders caused by abnormal synthesis of a disease-causing protein. Few currently used drugs are small, component-based and employ occupancy-driven MOA to impede protein activity for a short period of time to temporarily modify it. The proteolysis-targeting chimeras (PROTACs) technology is introducing a breakthrough technique by using an event-driven MOA. Heterobifunctional PROTACs based on small molecules hijack the ubiquitin–proteasome system to induce the destruction of the target protein. The key problem in the development of PROTACs presently is to discover powerful, tissue- and cell-specific PROTAC molecules with good drug-likeness and conventional safety procedures. This review focuses on approaches to enhance the effectiveness and selectivity of PROTACs. In the present review, we have emphasized the most relevant findings on the degradation of proteins by PROTACs, innovative targeted techniques to enhance the efficacy and development of proteolysis, and potential future avenues in medicine.
Keywords
PROTACs, proteolysis, developing medicine, degradation, druggable technologies
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