New compound tested as treatment for rheumatoid arthritis using human cell lines and patients cells
2017
Duke University, Durham, USA(1)
University of Texas, Dallas, USA(2)
University of Texas, Dallas, USA(2)
TNF-α is a major contributor to tissue inflammation and inhibition of its signalling cascade has been proven to reduce disease burden for rheumatoid arthritis (RA), ankylosing spondylitis, and inflammatory bowel disease. TAK1 acts as a key mediator in TNF-α-mediated signalling. In the present study, the researchers aimed at describing the newly synthesized compound Takinib, a potent and selective TAK1 inhibitor. The compound was studied using a variety of human cell lines and cells isolated from RA patients. At the molecular level, biochemical assays and crystallography showed the mechanisms of action of Takinib on TAK1. Overall, Takinib is an attractive starting point for the development of inhibitors that sensitize cells to TNF-α-induced cell death, with general implications for cancer and autoimmune disease treatment.
Takinib, a selective TAK1 inhibitor, broadens the therapeutic efficacy of TNFα inhibition for cancer and autoimmune disease
Timothy A. J. Haystead(1), Emily R. Derbyshire(1), Kenneth D. Westover(2)
Added on: 10-30-2021
[1] https://www.cell.com/cell-chemical-biology/fulltext/S2451-9456(17)30269-6?_returnURL=https%3A%2F%2Flinkinghub.elsevier.com%2Fretrieve%2Fpii%2FS2451945617302696%3Fshowall%3Dtrue[2] https://data.jrc.ec.europa.eu/dataset/700397b2-edd7-4ed6-86f7-fc1b164ed432
