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趋化因子受体 CCR8 的拮抗作用在灵长类哮喘模型中无效。

Antagonism of chemokine receptor CCR8 is ineffective in a primate model of asthma.

机构信息

Department of Cellular Immunology and Pharmacology, Millennium Pharmaceuticals Inc., Cambridge, MA, USA.

出版信息

Thorax. 2013 Jun;68(6):506-12. doi: 10.1136/thoraxjnl-2012-203012. Epub 2013 Mar 1.

Abstract

BACKGROUND

Expression of the T-cell-associated chemokine receptor CCR8 and its ligand CCL1 have been demonstrated to be elevated in patients with asthma. CCR8 deficiency or inhibition in models of allergic airway disease in mice resulted in conflicting data.

OBJECTIVE

To investigate the effects of a selective small molecule CCR8 inhibitor (ML604086) in a primate model of asthma.

METHODS

ML604086 and vehicle were administered by intravenous infusion to 12 cynomolgus monkeys during airway challenge with Ascaris suum. Samples were collected throughout the study to measure pharmacokinetics (PK) and systemic CCR8 inhibition, as well as inflammation, T helper 2 (Th2) cytokines and mucus in bronchoalveolar lavage (BAL). Airway resistance and compliance were measured before and after allergen challenge, and in response to increasing concentrations of methacholine.

RESULTS

ML604086 inhibited CCL1 binding to CCR8 on circulating T-cells>98% throughout the duration of the study. However, CCR8 inhibition had no significant effect on allergen-induced BAL eosinophilia and the induction of the Th2 cytokines IL-4, IL-5, IL-13 and mucus levels in BAL. Changes in airway resistance and compliance induced by allergen provocation and increasing concentrations of methacholine were also not affected by ML604086.

CONCLUSIONS

These results clearly demonstrate a dispensable role for CCR8 in ameliorating allergic airway disease in atopic primates, and suggest that strategies other than CCR8 antagonism should be considered for the treatment of asthma.

摘要

背景

已证实 T 细胞相关趋化因子受体 CCR8 的表达及其配体 CCL1 在哮喘患者中升高。在小鼠变应性气道疾病模型中,CCR8 缺乏或抑制导致了相互矛盾的数据。

目的

研究选择性小分子 CCR8 抑制剂(ML604086)在灵长类哮喘模型中的作用。

方法

在 Ascaris suum 气道挑战期间,通过静脉输注将 ML604086 和载体给予 12 只食蟹猴。在整个研究过程中收集样本,以测量药代动力学(PK)和系统 CCR8 抑制以及炎症、T 辅助 2(Th2)细胞因子和支气管肺泡灌洗液(BAL)中的粘液。在过敏原挑战前后以及对越来越高浓度的乙酰甲胆碱的反应中测量气道阻力和顺应性。

结果

ML604086 在整个研究期间抑制循环 T 细胞上 CCL1 与 CCR8 的结合>98%。然而,CCR8 抑制对过敏原诱导的 BAL 嗜酸性粒细胞增多和 Th2 细胞因子 IL-4、IL-5、IL-13 和 BAL 中粘液水平的诱导没有显著影响。过敏原刺激和乙酰甲胆碱浓度增加引起的气道阻力和顺应性变化也不受 ML604086 的影响。

结论

这些结果清楚地表明 CCR8 在改善特应性灵长类动物的过敏性气道疾病中起着可有可无的作用,并表明除 CCR8 拮抗作用之外,还应考虑其他策略来治疗哮喘。

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