BH3-mimetic drugs: blazing the trail for new cancer medicines
- Author(s)
- Merino, D; Kelly, GL; Lessene, G; Wei, AH; Roberts, AW; Strasser, A;
- Details
- Publication Year 2018-12-10,Volume 34,Issue #6,Page 879-891
- Journal Title
- Cancer Cell
- Publication Type
- Journal Article
- Abstract
- Defects in apoptotic cell death can promote cancer and impair responses of malignant cells to anti-cancer therapy. Pro-survival BCL-2 proteins prevent apoptosis by keeping the cell death effectors, BAX and BAK, in check. The BH3-only proteins initiate apoptosis by neutralizing the pro-survival BCL-2 proteins. Structural analysis and medicinal chemistry led to the development of small-molecule drugs that mimic the function of the BH3-only proteins to kill cancer cells. The BCL-2 inhibitor venetoclax has been approved for treatment of refractory chronic lymphocytic leukemia and this drug and inhibitors of pro-survival MCL-1 and BCL-XL are being tested in diverse malignancies.
- Publisher
- Cell Press
- Research Division(s)
- Cancer And Haematology; Molecular Genetics Of Cancer; Chemical Biology
- PubMed ID
- 30537511
- Publisher's Version
- https://doi.org/10.1016/j.ccell.2018.11.004
- NHMRC Grants
- NHMRC/1101378, NHMRC/1086291, NHMRC/1116937, NHMRC/1113133, NHMRC/1143105, NHMRC/1126843, NHMRC/1113133, NHMRC/1117089,
- Terms of Use/Rights Notice
- Refer to copyright notice on published article.
Creation Date: 2018-12-18 02:54:30
Last Modified: 2018-12-18 04:16:50