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设计,合成和T细胞检查点组合的潜力,第一类DGKα/ζ抑制剂BMS-986408的组合潜力.

Denise C Grünenfelder1, Upender Velaparthi2, Jayakumar S Warrier3

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基酶α (DGKα) 和zeta (DGKζ) 是T细胞的检查点. 用BMS-408抑制DGKα/ζ可增强T细胞功能和瘤免疫力,为下一代癌症免疫疗法显示出前途.

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科学领域:

  • 免疫学 免疫学 免疫学
  • 药理学 药理学是指药理学的学科.
  • 在瘤学瘤学.

背景情况:

  • 糖醇激酶α (DGKα) 和DGKζ是细胞内检查点,抑制T细胞信号,激活和抗瘤免疫力.
  • 抑制DGKα/ζ是下一代癌症免疫疗法的有希望的策略.
  • 这种方法有可能增强对抗PD-1和抗CTLA-4等现有治疗方法的反应.

研究的目的:

  • 优化一个分子 (BMS-502) 成为一流的双DGKα/ζ抑制剂,用于潜在的癌症免疫疗法.
  • 确定一种具有改善细胞功率,药理动力学和物理化学性质的开发候选物.
  • 评估优化抑制剂 (BMS-408) 的临床前疗效和安全性.

主要方法:

  • 基于结构的药物设计和药物化学,用于分子优化.
  • 在体外测试以评估细胞效能和酶抑制.
  • 在小鼠模型中进行体内药理动力学和药理动力学研究.
  • 在MC-38和1956瘤模型中使用组合治疗的临床前疗效研究.

主要成果:

  • 开发候选BMS-408,一个双重DGKα/ζ抑制剂,通过优化BMS-502.2来确定.
  • BMS-408在体外和体内表现出良好的药理学特征.
  • 临床前研究表明小鼠的剂量相对应的药理动力学和药理动力学.
  • 在相关瘤模型中,BMS-408与抗PD-1和/或抗CTLA-4结合时表现出强大的疗效.

结论:

  • BMS-408是一种强效的,一流的双重DGKα/ζ抑制剂,具有前临床抗瘤活性.
  • 良好的体外和体内特征支持BMS-408进入临床开发.
  • 通过BMS-408抑制DGKα/ζ具有增强癌症免疫疗法的潜力.