Inhibition of TLR1/2 dimerization by enantiomers of metal complexes. Issue 83 (9th September 2016)

• Record Type: Journal Article
• Authors: Liu, Li-Juan; Wang, Wanhe; Zhong, Zhangfeng; Lin, Sheng; Lu, Lihua; Wang, Yi-Tao; Ma, Dik-Lung; Leung, Chung-Hang
• Is Part Of: Chemical communications. Volume 52:Issue 83(2016)
• Page Start: 12278
• Page End: 12281
• Publication Date: 2016-09-09
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/c6cc06155a
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : Complex1 and its enantiomerΛ-1 are reported for the first time to inhibit NF-κB transduction via the modulation of Pam3 CSK4 -induced TLR1/2 heterodimerization. Abstract : We report herein the identification of an immunomodulatory metal-based complex1 as a direct inhibitor of TLR1/2 heterodimerization. Both enantiomers of complex1 selectively suppressed TNF-α and TLR1/2 heterodimerization in Pam3 CSK4 -induced macrophages, withΛ-1 being more potent thanΔ-1 . Moreover, the complexes inhibited NF-κB transduction via the modulation of TLR1/2 signaling. To our knowledge, complex1 is the first metal-based inhibitor of TLR1/2 heterodimerization reported to date.