The 3UTR of human MAVS mRNA contains multiple regulatory elements for the control of protein expression and subcellular localization
- Author:
- Journal:
- Volumes and pages:
- Ling Xu et al.
- Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms
- Volume 1862, Issue 1 January 2019 Pages 47-57
![2 Biological Activity
TW-37 is a Bcl-2 protein family inhibitor with a Ki of 0.29 μM. TW-37 binds to the BH3 binding groove in Bcl-2 protein competing with BH3 peptides derived from Bid, Bim, and Bad proteins. TW-37 binds to Bcl-2 with a Ki value of 290 nM and also to Bcl-xL and Mcl-1 with high affinities. TW-37 potently inhibits cell growth in PC-3 prostate cancer cells with an IC50 value of 200 nM and effectively induces apoptosis in a dose-dependent manner. TW-37 has an IC50 of 1.1 μM for primary human endothelial cells and averaged 0.3 μM for head and neck cancer cells (OSCC3, UM-SCC-1, and UMSCC-74A). The combination of TW-37 and cisplatin showed enhanced cytotoxic effects for endothelial cells and HNSCC in vitro, compared with single agent treatment. [1][2]
3 References:
Antiangiogenic Effect of TW37, a Small-Molecule Inhibitor of Bcl-2 Esther Joo, Zhihong Dong, et al. Cancer Res 2006;66:8698-8706
TW-37, a small-molecule inhibitor of Bcl-2, mediates S-phase cell cycle arrest and suppresses head and neck tumor angiogenesis Benjamin D. Zeitlin, Zhaocheng Zhang, et al. Mol Cancer Ther 2009;8:893-903
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