Bay 11-7085 at the ACR 2015 Meeting in San Francisco

There has been one publication on Bay 11-7085 at the ACR 2015 Annual Meeting in San Francisco. NF-κB and other transcription factors seem to play major roles in the regulation of inflammatory genes. NF-κB is a pivotal regulator of inflammation etc. in rheumatoid arthritis. “BAY 11-7085 is an inhibitor of IκBα phosphorylation that leads to NF-κB inactivation and downregulation of inflammation in mouse model of asthma, in articular chondrocytes as well as in synovial fibroblasts.” BAY 11-7085 has also shown to block TLR4 (Toll-like receptor 4) and ERK expression. So NF-κB is a feasible target in rheumatoid arthritis. If you want to get deeper into this topic, please read the article by Paul Tak and Gary S. Firestein (see link below)

Biserka Relic and colleagues presented: „ Bay 11-7085 Induces Glucocorticoid Receptor Activation and Autophagy to Initiate Human Synovial Fibroblast Cell Death”. Conclusion: “BAY 11-7085 induced human synovial fibroblast autophagy that acts as an agonist to promote BAY 11-7085-induced apoptosis. Furthermore, our results suggest that BAY 11-7085-induced autophagy in synovial fibroblasts is mediated through GR activation and PPAR-γ inactivation.”

Do we get something out of this research right away? Yes, knowledge. But if you wanted a new drug, that’s another story. I think I’ve heard enough talks that mentioned NF-κB, so I think, we eventually will see NF-κB targeted in a therapeutical approach. I don’t think that this will be Bay 11-7085.

References:

Paul P. Tak and Gary S. Firestein: NF-κB: a key role in inflammatory diseases. J Clin Invest. 2001 Jan 1; 107(1): 7–11. doi: 10.1172/JCI11830 PMC198552. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC198552/.

Relic B, Charlier E, Deroyer C, Malaise O, Neuville S, Desoroux A, Gillet P, Malaise MG, de Seny D. Bay 11-7085 Induces Glucocorticoid Receptor Activation and Autophagy to Initiate Human Synovial Fibroblast Cell Death [abstract]. Arthritis Rheumatol. 2015; 67 (suppl 10). http://acrabstracts.org/abstract/bay-11-7085-induces-glucocorticoid-receptor-activation-and-autophagy-to-initiate-human-synovial-fibroblast-cell-death/. Accessed December 8, 2015.