BH3-mimetic drugs: blazing the trail for new cancer medicines
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
WEHI Research Division(s)
Cancer And Haematology; Molecular Genetics Of Cancer; Chemical Biology
PubMed ID
30537511
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
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