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.
Keywords: PROTACs, cancer, ubiquitin, anticancer, proteins, target.
Mini-Reviews in Medicinal Chemistry
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.
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Cite this article as:
Arora Poonam , Singh Manjinder , Singh Varinder , Bhatia Shiveena and Arora Sandeep *, PROTACs in Treatment of Cancer: A Review, Mini-Reviews in Medicinal Chemistry 2021; 21 (16) . https://dx.doi.org/10.2174/1389557521666210226150740
DOI https://dx.doi.org/10.2174/1389557521666210226150740 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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