Philbin V J, Levy O
Department of Medicine, Division of Infectious Diseases, Children's Hospital Boston, Harvard Medical School, 300 Longwood Avenue, Boston, MA 02115, USA.
Biochem Soc Trans. 2007 Dec;35(Pt 6):1485-91. doi: 10.1042/BST0351485.
TLR8 (Toll-like receptor 8) is activated by ssRNAs (single-stranded RNAs) and synthetic imidazoquinoline compounds that resemble purines and have immunostimulatory activity. TLR8 agonists are particularly effective at inducing Th1-polarizing responses from human monocytes and myeloid dendritic cells, with the magnitude of response substantially exceeding that induced by agonists of other TLRs. Mechanisms underlying the remarkable efficacy of TLR8 agonists may include: (i) particularly robust activation of intracellular signalling cascades culminating in nuclear translocation of NF-kappaB (nuclear factor kappaB), (ii) activation of BTK (Bruton's tyrosine kinase), and (iii) the ability of some imidazoquinolines to induce TLR-independent effects via antagonism of adenosine receptors. The strong agonist activities of TLR8 agonists also extend to human neonatal leucocytes, which usually display impaired Th1-polarizing responses to many diverse stimuli including agonists of other TLRs. Their strong Th1-polarizing properties render TLR8 agonists attractive targets of biopharmaceutical development as agents that may induce protective immune responses in diverse populations, including newborns.
Toll样受体8(TLR8)可被单链RNA(ssRNA)和类似嘌呤且具有免疫刺激活性的合成咪唑喹啉化合物激活。TLR8激动剂在诱导人单核细胞和髓样树突状细胞产生Th1极化反应方面特别有效,其反应强度大大超过其他TLR激动剂所诱导的反应。TLR8激动剂显著疗效的潜在机制可能包括:(i)细胞内信号级联的特别强烈激活,最终导致核因子κB(NF-κB)的核转位;(ii)布鲁顿酪氨酸激酶(BTK)的激活;(iii)一些咪唑喹啉通过拮抗腺苷受体诱导非TLR依赖性效应的能力。TLR8激动剂的强激动剂活性还扩展到人类新生儿白细胞,这些白细胞通常对包括其他TLR激动剂在内的多种刺激表现出受损的Th1极化反应。它们强大的Th1极化特性使TLR8激动剂成为生物制药开发的有吸引力的靶点,作为可能在包括新生儿在内的不同人群中诱导保护性免疫反应的药物。
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