Synthesis, structure-activity relationships and preliminary mechanism study of N-benzylideneaniline derivatives as potential TLR2 inhibitors

Cai, Shaoyi; Zhu, Gengzheng; Cen, Xiaohong; Bi, Jingjie; Zhang, Jingru; Tang, Xiaoshan; Chen, Kun; Cheng, Kui

doi:10.1016/j.bmc.2018.03.001

Cited by 12 publications

(5 citation statements)

References 28 publications

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“…Additionally, further evaluation of the TLR2/NF-ĸB signaling pathway constituents, including MyD88, IRAK-4, IRAK-1, and TRAF6, amongst others, will provide a better understanding of the downstream effects following TLR2 activation. The use of TLR2/NF-ĸB antagonists, such as pyrrogallol or Nbenzylideneaniline derivatives, applied to in vitro and in vivo models may provide future potential therapies for investigation in human clinical trials (35,36).…”

Section: Discussionmentioning

confidence: 99%

Activation of Toll-Like Receptor 2 Promotes Proliferation of Human Lung Adenocarcinoma Cells

et al. 2020

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Background/Aim: The aim of this study was to evaluate the role of toll-like receptor 2 (TLR2) in the proliferation of human lung cancer cells and identify the signaling pathway that mediates this effect. Materials and Methods: Adenocarcinoma (A549 and H1650) and adenosquamous (H125) cells were treated with increasing doses of Pam3CSK4, a TLR2 agonist. Cell proliferation and NF-ĸB activation were evaluated. NF-ĸB was inhibited prior to treatment with Pam3CSK4 and proliferation was assessed. Results: TLR2 expression was significantly higher in A549 and H1650 cells compared to H125 cells (p<0.001). TLR2 stimulation induced proliferation in adenocarcinoma cells only and led to a corresponding increase in NF-ĸB activity (p<0.05). Inhibition of NF-ĸB prior to treatment with Pam3CSK4 attenuated this proliferative response. Conclusion: TLR2 activation induced proliferation of lung adenocarcinoma cells through activation of NF-ĸB. Thus, the TLR2 signaling pathway may be a potential therapeutic target in lung adenocarcinoma.

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Section: Discussionmentioning

confidence: 99%

Activation of Toll-Like Receptor 2 Promotes Proliferation of Human Lung Adenocarcinoma Cells

et al. 2020

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“…Another study reported structure-activity relationship of related N-benzylideneaniline derivatives. 40 However, readers should note that most TLR2 antagonists in literature contain alert structures for assay interference and stability. [41][42][43] TLR4.…”

Section: Rsc Chemical Biology Reviewmentioning

confidence: 99%

Small molecule modulators of immune pattern recognition receptors

Tsukidate,

Hespen,

Hang

2023

RSC Chem. Biol.

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“…Under normal circumstances, activation of TLR2-Toll/interleukin-1 receptor (TIR) on macrophages can trigger the production of chemokines dependent on the NF-κB signaling pathway, and recruit immune cells in the bladder ( 115 , 116 ). However, E.faecalis has a TIR domain-containing protein structure, which is similar to the TIR domain of TLR2 on macrophages ( 113 , 117 ).…”

Section: The Bladder Immune Responses To the Main Nine Uropathogensmentioning

confidence: 99%

The immune responses to different Uropathogens call individual interventions for bladder infection

Yang

et al. 2022

Front. Immunol.

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Urinary tract infection (UTI) caused by uropathogens is the most common infectious disease and significantly affects all aspects of the quality of life of the patients. However, uropathogens are increasingly becoming antibiotic-resistant, which threatens the only effective treatment option available-antibiotic, resulting in higher medical costs, prolonged hospital stays, and increased mortality. Currently, people are turning their attention to the immune responses, hoping to find effective immunotherapeutic interventions which can be alternatives to the overuse of antibiotic drugs. Bladder infections are caused by the main nine uropathogens and the bladder executes different immune responses depending on the type of uropathogens. It is essential to understand the immune responses to diverse uropathogens in bladder infection for guiding the design and development of immunotherapeutic interventions. This review firstly sorts out and comparatively analyzes the immune responses to the main nine uropathogens in bladder infection, and summarizes their similarities and differences. Based on these immune responses, we innovatively propose that different microbial bladder infections should adopt corresponding immunomodulatory interventions, and the same immunomodulatory intervention can also be applied to diverse microbial infections if they share the same effective therapeutic targets.

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Synthesis, structure-activity relationships and preliminary mechanism study of N-benzylideneaniline derivatives as potential TLR2 inhibitors

Cited by 12 publications

References 28 publications

Activation of Toll-Like Receptor 2 Promotes Proliferation of Human Lung Adenocarcinoma Cells

Activation of Toll-Like Receptor 2 Promotes Proliferation of Human Lung Adenocarcinoma Cells

Small molecule modulators of immune pattern recognition receptors

The immune responses to different Uropathogens call individual interventions for bladder infection

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