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      PROTAC: A Novel Drug Delivery Technology for Targeting Proteins in Cancer Cells.

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          Abstract

          The treatment measures of malignant carcinomas are most important for human health. In recent years the use of targeted therapy based on small molecule compounds and identical immunoglobulin has been the most frequently used tool to combat cancerous cells. But there are still several limitations in their clinical development and applications, including their ability to bind multiple molecular target sites, both cell surface receptors and intracellular proteins, promoting a greater risk of toxicity. PROTAC is a novel technology that maintains a balance between protein synthesis and degradation and uses molecules instead of conventional enzyme inhibitors, containing two active domains and a linker to destroy unwanted selective protein (like kinase, skeleton protein and regulatory protein). PROTACs are heterobifunctional nano molecules with a size range of about 10 nanometres that eliminate the protein complexes formed by protein-protein interaction through large and flat surfaces generally defined as "undruggable" in conventional drug delivery systems, which include around 85% of proteins present in humans, suggesting their wide application in the field of drug development. Such peptide-based PROTACs have successfully shown targets' destruction in cultured cells (e.g., MetAP-2, and FKBP12F36V, receptors for estrogens and androgen). However, some obstacles prevent this technology from transferring from the laboratory to its actual clinical utility, such as delivery system and bioavailability. The scope of the presented review is to give an overview of novel PROTAC technology with its limitations, advantages, mechanism of action, and development of photocontrolled PROTACs and to summarize its futuristic approach to targeting proteins in cancer cells.

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          Author and article information

          Journal
          Curr Drug Discov Technol
          Current drug discovery technologies
          Bentham Science Publishers Ltd.
          1875-6220
          1570-1638
          2023
          : 20
          : 2
          Affiliations
          [1 ] Chitkara College of Pharmacy, Chitkara University, Punjab, India.
          [2 ] School of Pharmacy, Sharda University, Greater Noida, Gautam Buddha Nagar 201306, Uttar Pradesh, India.
          Article
          CDDT-EPUB-127297
          10.2174/1570163820666221031124612
          36321238
          1e3c09ae-37cd-4b53-86a6-882977f23c65
          History

          PROTACs,Carcinoma,undruggable,small molecules,proteins,bioavailability

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