Acta Scientific Pharmaceutical Sciences (ASPS)(ISSN: 2581-5423)

Perspective Volume 6 Issue 2

Perspective on Targeted Protein Degradation strategy by PROTAC Technology

Raghu Vannam*

Sr. Scientist, Intellia Therapeutics, USA

*Corresponding Author: Raghu Vannam, Sr. Scientist, Intellia Therapeutics, USA.

Received: June 28, 2021; Published: January 31, 2022

The targeted protein degradation- proteolysis targeting chimeras (PROTAC) technology is an attractive strategy to evaluate the fast biology and changes in a target protein, and its degradation [1]. The PROTAC- a hetero bi functional small molecule, one end contains a ligand of protein of interest (POI) and other end E3 ligase ligand attached through a linker, there by formation of a ternary complex resulted in ubiquitination of E3 ligase and ultimately tagging target proteins (POI) that then are recognized by the proteasome for degradation [2]. PROTAC technology uses event driven process and catalytic mode of action, which is different than traditionally occupancy driven pathway and attracting from academia to industry.

References

  1. Burslem GM and Crews CM. “Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery”. Cell 1 (2020): 102-114.
  2. Lai AC and Crews CM. “Induced protein degradation: an emerging drug discovery paradigm”. Nature Reviews. Drug Discovery 2 (2017): 101-114.
  3. Gechijian LN., et al. “Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands”. Nature Chemical Biology 4 (2018): 405-412.
  4. Burslem GM., et al. “Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-Mediated Targeted Protein Degradation”. Cancer Research 18 (2019): 4744-4753.
  5. Remillard D., et al. “Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands”. Angewandte Chemie 21 (2017): 5738-5743.
  6. Vannam R., et al. “Targeted degradation of the enhancer lysine acetyltransferases CBP and p300”. Cell Chemical Biology 4 (2021): 503-514.

Citation

Citation: Raghu Vannam. “Perspective on Targeted Protein Degradation strategy by PROTAC Technology". Acta Scientific Pharmaceutical Sciences 6.2 (2022): 18-19.

Copyright

Copyright: © 2022 Raghu Vannam. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.




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