Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 220, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.113539
Keywords
Bfl-1; BCL2A1; Anti-cancer; Apoptosis; SAR
Categories
Funding
- National Natural Science Foundation of China [81773581, 81773639, 81930100]
- National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China [2018ZX09711002]
- Priority Academic Program Development of Jiangsu Higher Education Institutions
- State Key Laboratory of Natural Medicines, China Pharmaceutical University [SKLNMZZ202003]
- Qing Lan Project of Jiangsu Province
- Young Elite Scientists Sponsorship Program by CAST
- Double First Class Innovation Team of China Pharmaceutical University [CPU2018GY02]
Ask authors/readers for more resources
Bfl-1, an important anti-apoptotic protein, lacks developed inhibitors with ideal activity and selectivity, and its therapeutic potential is yet to be fully explored.
The Bcl-2 family members rigorously regulate cell endogenous apoptosis, and targeting anti-apoptotic members is a hot topic in design of anti-cancer drugs. At present, FDA and EMA have approved Bcl-2 inhibitor Venetoclax (ABT-199) for treating chronic lymphocytic leukemia (CLL). However, inhibitors of anti-apoptotic protein BCL2A1/Bfl-1 have not been vigorously developed, and no molecule with ideal activity and selectivity has been found yet. Here we review the biological function and protein structure of Bfl-1, discuss the therapeutic potential and list the currently reported inhibitory peptides and small molecules. This will provide a reference for Bfl-1 targeting drug discovery in the future. (C) 2021 Elsevier Masson SAS. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available
Share Paper
