Md Habibur Rahaman, Sara J Thygesen, Michael J Maxwell, Hyoyoung Kim, Prerna Mudai, Jeffrey D Nanson, Xinying Jia, Parimala R Vajjhala, Andrew Hedger, Irina Vetter, Thomas Haselhorst, Avril A B Robertson, Brian Dymock, Thomas Ve, Mehdi Mobli, Katryn J Stacey, Bostjan Kobe
Toll-like receptor (TLR) innate immunity signalling protects against pathogens, but excessive or prolonged signalling contributes to a range of inflammatory conditions. Structural information on the TLR cytoplasmic TIR (Toll/interleukin-1 receptor) domains and the downstream adaptor proteins can help us develop inhibitors targeting this pathway. The small molecule o-vanillin has previously been reported as an inhibitor of TLR2 signalling. To study its mechanism of action, we tested its binding to the TIR domain of the TLR adaptor MAL/TIRAP (MALTIR )...
December 2024: Journal of Enzyme Inhibition and Medicinal Chemistry