Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Agonists as Potential Small Molecule Therapeutics for Cancer Immunotherapy,Journal of Medicinal Chemistry

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Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Agonists as Potential Small Molecule Therapeutics for Cancer Immunotherapy
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2018-02-07 00:00:00 , DOI: 10.1021/acs.jmedchem.7b01314
Ruomeng Qiu ₁ , Yonghui Wang ₁

Affiliation

The recent success of PD-1/PD-L1 antibodies for advanced cancer treatment has led to the conclusion that activating the immune system can be employed to fight cancer. These results also encourage the development of small molecule immunomodulators for cancer immunotherapy. RORγt is a key transcription factor mediating Th17 cell differentiation and IL-17 production, which is able to activate CD8⁺ T cells and elicit antitumor efficacy. Since RORγt agonists have been shown to increase basal activity of RORγt and promote Th17 cell differentiation, development of RORγt agonists could provide a unique approach to cancer immunotherapy. In this review, we summarize RORγt sterol and synthetic agonists, analyze the common ground of their mode of actions, and discuss the potential role of RORγt agonists as small molecule therapeutics for cancer immunotherapy.

中文翻译：

维甲酸受体孤儿γt（RORγt）激动剂可作为潜在的小分子疗法用于癌症免疫治疗

PD-1 / PD-L1抗体在晚期癌症治疗中的最新成功已得出结论，可以激活免疫系统来对抗癌症。这些结果也鼓励开发用于癌症免疫疗法的小分子免疫调节剂。RORγt是介导Th17细胞分化和IL-17产生的关键转录因子，能够激活CD8 ⁺T细胞并引发抗肿瘤功效。由于已显示RORγt激动剂可增加RORγt的基础活性并促进Th17细胞分化，因此RORγt激动剂的开发可为癌症免疫治疗提供独特的方法。在这篇综述中，我们总结了RORγt甾醇和合成激动剂，分析了它们的作用方式的共同点，并讨论了RORγt激动剂作为癌症免疫疗法的小分子疗法的潜在作用。

更新日期：2018-02-07

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