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Characterization of novel small-molecule NRF2 activators: Structural and biochemical validation of stereospecific KEAP1 binding.
TLDR
This work demonstrates that reversible cyanoenone Michael acceptors, such as the tpAIMs and sA IMs, can be specifically tuned to regulate redox sensitive cysteine residues on key signaling molecules, an approach with significant promise for innovative drug development. Expand
Synthesis and Evaluation of a Series of Novel Asymmetrical Curcumin Analogs for the Treatment of Inflammation
TLDR
Among the analogs of the potent anti-inflammatory activity of curcumin, compounds 3b8 and 3b9 exhibited significant protection and possess enhanced anti- inflammatory activity thereby attenuated the LPS-induced septic death in mice. Expand
Dihydroceramide-desaturase-1-mediated caspase 9 activation through ceramide plays a pivotal role in palmitic acid-induced HepG2 cell apoptosis
TLDR
Results showed that the inhibition of PA-induced HepG2 cell growth takes place in a time- and concentration-dependent manner, and that palmitoleic acid (POA), an omega-7 monounsaturated fatty acid, reversesPA-induced apoptosis through DES1 → Ceramide →-Caspase 9 →–Caspases 3 signaling. Expand
Discovery and evaluation of novel anti-inflammatory derivatives of natural bioactive curcumin
TLDR
Heterocyclic monocarbonyl curcumin analogs have potential therapeutic effects in acute inflammatory diseases and display the strongest inhibition of lipopolysaccharide (LPS)-stimulated expression of pro-inflammatory cytokines in macrophages. Expand
A novel series of cysteine-dependent, allosteric inverse agonists of the nuclear receptor RORγt.
TLDR
Site-directed mutagenesis and molecular dynamics simulations are supportive of a mechanism of action through specific binding to Cys476 on alpha helix 11 of the ligand binding domain (LBD) of RORγt, supportive of the development of compound 13 in autoimmune diseases. Expand
Lipopolysaccharide and palmitic acid synergistically induced MCP-1 production via MAPK-meditated TLR4 signaling pathway in RAW264.7 cells
TLDR
Combination of LPS and PA synergistically induced MCP-1 secretion in RAW264.7 cells mimics the situation of diabetes with obesity that has higher level of PA and LPS, MAPK/TLR4/ M CP-1 might be potential therapeutic targets for diabetes with Obesity. Expand
Design, synthesis, and evaluation of semi-conservative mono-carbonyl analogs of curcumin as anti-inflammatory agents against lipopolysaccharide-induced acute lung injury
Correction for ‘Design, synthesis, and evaluation of semi-conservative mono-carbonyl analogs of curcumin as anti-inflammatory agents against lipopolysaccharide-induced acute lung injury’ by Lili DongExpand
Synthesis and Broad Antiviral Activity of Novel 2-aryl-isoindolin-1-ones towards Diverse Enterovirus A71 Clinical Isolates
TLDR
This study led to the discovery of 2-aryl-isoindolin-1-ones as a promising scaffold with potent anti-EV-A71 activities, which deserves further in-depth studies. Expand
RTA 1701 is an orally-bioavailable, potent, and selective RORγt inhibitor that suppresses Th17 differentiation in vitro and is efficacious in mouse models of autoimmune disease.
TLDR
RTA 1701 is a potent and selective RORγt inhibitor in preclinical development for autoimmune disorders and is efficacious in animal models of autoimmune disease, suggesting it may have therapeutic potential in Th17-associated autoimmune disorders. Expand
Pyrazolyl- and tricyclic pyrimidinyl enones as antioxidant modulators of inflammation
A compound of the formula: ** Formula ** wherein: atoms marked 1 and 2 are connected by an epoxidized double bond or double bond; n is 1 or 2; m is 0 or 1; X is -CN, -CF3, or -C (O) Ra, where Ra isExpand
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