PROTACs: A Hope for Breast Cancer Patients?

(E-pub Ahead of Print)

Author(s): Rajwinder Kaur, Gaurav Chaudhary, Amritpal Kaur, Pargat Singh, Gagan Deep Longowal, Gayatri P. Sapkale, Sandeep Arora*

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

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Background: Breast Cancer (BC) is the most widely recognized disease in women. A massive number of women are diagnosed with breast cancer and many lost their lives every year. Cancer is the subsequent driving reason for dying, giving rise to it one of the current medication's most prominent difficulties.

Objectives: The main objective of the study is to examine and explore novel therapy (PROTAC) and its effectiveness against breast cancer.

Methods: The literature search was done across Medline, Cochrane, ScienceDirect, Wiley Online, Google Scholar, PubMed, Bentham Sciences from 2001 to 2020. The articles were collected; screened, segregated, and selected papers were included for writing the review article.

Results and Conclusion: A novel innovation emerged around two decades ago that has great potential to not only overcome the limitations but also can provide future direction for the treatment of many diseases which has presently not many therapeutic options available and regarded as incurable with traditional techniques; that innovation is called PROTAC (Proteolysis Targeting Chimera) and able to efficaciously ubiquitinate and debase cancer encouraging proteins by noncovalent interaction. PROTACs are constituted of two active regions isolated by a linker and equipped for eliminating explicit undesirable protein. It is empowering greater sensitivity to "drug-resistant targets" as well as a more prominent opportunity to influence non-enzymatic function. PROTACs have been demonstrated to show better target selectivity contrasted with traditional small-molecule inhibitors. So far, the most investigation into PROTACs possesses particularly concentrated on applications to cancer treatment including breast cancer, the treatment of different ailments may profit from this blossoming innovation.

Keywords: Breast cancer, novel therapy, protein degradation, PROTACs, ER-PROTAC, BET-PROTAC, BRD4-degrader.

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Article Details

(E-pub Ahead of Print)
DOI: 10.2174/1871520621666210308100327
Price: $95

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