Kumar Sakshi, Sharma Vikram, Yadav Shikha
Department of Pharmacy, Galgotias College, Greater Noida, Uttar Pradesh, 201310, India.
School of Medical and Allied Sciences, Galgotias University, Greater Noida, Uttar Pradesh, 201310, India.
Curr Protein Pept Sci. 2025;26(4):241-258. doi: 10.2174/0113892037324425241018061548.
TLR4 stands at the forefront of innate immune responses, recognizing various pathogen- associated molecular patterns and endogenous ligands, thus serving as a pivotal mediator in the immune system's defense against infections and tissue damage. Beyond its canonical role in infection, emerging evidence highlights TLR4's involvement in numerous non-infectious human diseases, ranging from metabolic disorders to neurodegenerative conditions and cancer. Targeting TLR4 signaling pathways presents a promising therapeutic approach with broad applicability across these diverse pathological states. In metabolic disorders such as obesity and diabetes, dysregulated TLR4 activation contributes to chronic low-grade inflammation and insulin resistance, driving disease progression. In cardiovascular diseases, TLR4 signaling promotes vascular inflammation and atherogenesis, implicating its potential as a therapeutic target to mitigate cardiovascular risk. Neurodegenerative disorders, including Alzheimer's and Parkinson's diseases, exhibit aberrant TLR4 activation linked to neuroinflammation and neuronal damage, suggesting TLR4 modulation as a strategy to attenuate neurodegeneration. Additionally, in cancer, TLR4 signaling within the tumor microenvironment promotes tumor progression, metastasis, and immune evasion, underscoring its relevance as a target for anticancer therapy. Advances in understanding TLR4 signaling cascades and their contributions to disease pathogenesis have spurred the development of various pharmacological agents targeting TLR4. These agents range from small molecule inhibitors to monoclonal antibodies, with some undergoing preclinical and clinical evaluations. Furthermore, strategies involving TLR4 modulation through dietary interventions and microbiota manipulation offer additional avenues for therapeutic exploration. Hence, targeting TLR4 holds significant promise as a therapeutic strategy across a spectrum of human diseases, offering the potential to modulate inflammation, restore immune homeostasis, and impede disease progression.
Toll样受体4(TLR4)处于固有免疫反应的前沿,识别各种病原体相关分子模式和内源性配体,因此在免疫系统抵御感染和组织损伤中起着关键介导作用。除了其在感染中的经典作用外,新出现的证据突显了TLR4参与众多非感染性人类疾病,从代谢紊乱到神经退行性疾病和癌症。靶向TLR4信号通路是一种有前景的治疗方法,在这些不同的病理状态中具有广泛的适用性。在肥胖和糖尿病等代谢紊乱中,TLR4激活失调会导致慢性低度炎症和胰岛素抵抗,推动疾病进展。在心血管疾病中,TLR4信号促进血管炎症和动脉粥样硬化形成,暗示其作为减轻心血管风险治疗靶点的潜力。包括阿尔茨海默病和帕金森病在内的神经退行性疾病表现出与神经炎症和神经元损伤相关的异常TLR4激活,表明调节TLR4是减轻神经退行性变的一种策略。此外,在癌症中,肿瘤微环境中的TLR4信号促进肿瘤进展、转移和免疫逃逸,强调其作为抗癌治疗靶点的相关性。对TLR4信号级联及其对疾病发病机制贡献的理解进展,推动了各种靶向TLR4的药理制剂的开发。这些制剂从小分子抑制剂到单克隆抗体不等,有些正在进行临床前和临床评估。此外,通过饮食干预和微生物群操纵调节TLR4的策略为治疗探索提供了额外途径。因此,靶向TLR4作为一种治疗策略在一系列人类疾病中具有重大前景,有可能调节炎症、恢复免疫稳态并阻碍疾病进展。