Journal article
Control of NF-kB activity in human melanoma by bromodomain and extra-terminal protein inhibitor I-BET151
SJ Gallagher, B Mijatov, D Gunatilake, K Gowrishankar, J Tiffen, W James, L Jin, G Pupo, C Cullinane, GA Mcarthur, PJ Tummino, H Rizos, P Hersey
Pigment Cell and Melanoma Research | WILEY | Published : 2014
DOI: 10.1111/pcmr.12282
Abstract
The transcription factor NF-kappaB (NF-kB) is a key regulator of cytokine and chemokine production in melanoma and is responsible for symptoms such as anorexia, fatigue, and weight loss. In addition, NF-kB is believed to contribute to progression of the disease by upregulation of cell cycle and anti-apoptotic genes and to contribute to resistance against targeted therapies and immunotherapy. In this study, we have examined the ability of the bromodomain and extra-terminal (BET) protein inhibitor I-BET151 to inhibit NF-kB in melanoma cells. We show that I-BET151 is a potent, selective inhibitor of a number of NF-kB target genes involved in induction of inflammation and cell cycle regulation a..
View full abstractGrants
Awarded by Australian National Health and Medical Research Council (NHMRC)
Funding Acknowledgements
We would like to thank Dr. Warren Kaplan (Garvin Institute of Medical Research) and Dr. Anthony Ashton (Kolling Institute of Medical Research) for their assistance in planning experiments and Prof. T. D. Gilmore (www.nf-kb.org) for the NF-kB target list. This work was supported by program grant 633004 from the Australian National Health and Medical Research Council (NHMRC).