Title:PROTACs in Treatment of Cancer: A Review
Volume: 21
Issue: 16
Author(s): Poonam Arora, Manjinder Singh, Varinder Singh, Shiveena Bhatia and Sandeep Arora*
Affiliation:
- Chitkara College of Pharmacy, Chitkara University, Rajpura, Patiala, Punjab,India
Keywords:
PROTACs, cancer, ubiquitin, anticancer, proteins, target.
Abstract: Cancer treatment has become a major challenge amidst the resistance and relapse caused by
the various treatments available. The PROteolysis TAargeting Chimera (PROTAC) technology involves
the degradation of target protein against the inhibition by small drug molecules. The
PROTACs with high potency and activity have been frequently reported; however, no PROTAC acting
against cancer has reached the clinical trials. The concept of PROTACs involves the reduction in
the disease-causing protein by its degradation through the ubiquitin-proteasomal enzyme system. This
concept has attracted a lot of attention from both industry and academia due to its potential in drug
discovery (in the form of PROTACs), which can conquer the resistance associated with current treatments
of cancer. Thus, it is the need of the hour to identify and synthesize more PROTACs for a viable
treatment of cancer. This article reviews the design, activity and effects produced in cancer by
some recently developed PROTACs.
