Laboratory of Lymphocyte Signalling and Development, Babraham Institute, Cambridge, United Kingdom.
Blood. 2010 Mar 18;115(11):2203-13. doi: 10.1182/blood-2009-07-232330. Epub 2010 Jan 15.
We have previously described critical and nonredundant roles for the phosphoinositide 3-kinase p110delta during the activation and differentiation of naive T cells, and p110delta inhibitors are currently being developed for clinical use. However, to effectively treat established inflammatory or autoimmune diseases, it is important to be able to inhibit previously activated or memory T cells. In this study, using the isoform-selective inhibitor IC87114, we show that sustained p110delta activity is required for interferon-gamma production. Moreover, acute inhibition of p110delta inhibits cytokine production and reduces hypersensitivity responses in mice. Whether p110delta played a similar role in human T cells was unknown. Here we show that IC87114 potently blocked T-cell receptor-induced phosphoinositide 3-kinase signaling by both naive and effector/memory human T cells. Importantly, IC87114 reduced cytokine production by memory T cells from healthy and allergic donors and from inflammatory arthritis patients. These studies establish that previously activated memory T cells are at least as sensitive to p110delta inhibition as naive T cells and show that mouse models accurately predict p110delta function in human T cells. There is therefore a strong rationale for p110delta inhibitors to be considered for therapeutic use in T-cell-mediated autoimmune and inflammatory diseases.
我们之前描述了磷酸肌醇 3-激酶 p110δ在初始 T 细胞激活和分化过程中的关键且非冗余作用,目前正在开发 p110δ抑制剂用于临床应用。然而,要有效地治疗已建立的炎症或自身免疫性疾病,能够抑制先前激活或记忆 T 细胞是很重要的。在这项研究中,我们使用了同工酶选择性抑制剂 IC87114,表明持续的 p110δ活性对于干扰素-γ的产生是必需的。此外,p110δ的急性抑制可抑制细胞因子的产生并减少小鼠的过敏反应。p110δ 是否在人类 T 细胞中发挥类似作用尚不清楚。在这里,我们表明 IC87114 可有效阻断幼稚和效应/记忆人 T 细胞的 T 细胞受体诱导的磷酸肌醇 3-激酶信号。重要的是,IC87114 减少了来自健康和过敏供体以及炎症性关节炎患者的记忆 T 细胞的细胞因子产生。这些研究确立了先前激活的记忆 T 细胞对 p110δ抑制的敏感性至少与幼稚 T 细胞一样高,并表明小鼠模型准确预测了 p110δ 在人类 T 细胞中的功能。因此,有充分的理由考虑使用 p110δ 抑制剂来治疗 T 细胞介导的自身免疫和炎症性疾病。