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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Review Article

PROTACs in Treatment of Cancer: A Review

Author(s): Poonam Arora, Manjinder Singh, Varinder Singh, Shiveena Bhatia and Sandeep Arora*

Volume 21, Issue 16, 2021

Published on: 26 February, 2021

Page: [2347 - 2360] Pages: 14

DOI: 10.2174/1389557521666210226150740

Price: $65

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.

Graphical Abstract

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