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在P2X3中的第二个药物结合点

Trung Thach1, KanagaVijayan Dhanabalan1, Prajwal Prabhakarrao Nandekar2

  • 1Department of Biological Sciences, Purdue University, West Lafayette, IN-47907, USA.

bioRxiv : the preprint server for biology
|June 25, 2024
PubMed
概括

研究人员阐明了与camlipixant结合的P2X3受体的结构,揭示了一个新的全抑制机制. 这一发现促进了对慢性咳治疗方法和P2X3受体对抗性的理解.

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科学领域:

  • 结构生物学 结构生物学
  • 药理学 药理学是指药理学的学科.
  • 分子神经科学 分子神经科学

背景情况:

  • 纯能P2X3受体对慢性咳至关重要,影响超过10%的人口.
  • 开发选择性P2X3抗剂是具有挑战性的,因为保留了受体结构.
  • 坎利皮克桑在临床试验的后期阶段是一个有前途的P2X3抗剂,但其精确的结合和抑制机制是未知的.

研究的目的:

  • 为了确定与camlipixant复合的P2X3受体的高分辨率结构.
  • 为了阐明P2X3受体对抗性和camlipixant的全抑制的分子机制.
  • 了解卡姆利皮克桑特对其他P2X受体家族成员的选择性的结构基础.

主要方法:

  • 建立了一个表达同位三元P2X3受体的稳定细胞系.
  • 使用基架净化了P2X3-camlipixant复合体.
  • 通过冷电子显微镜 (cryo-EM) 确定了复合物的结构.
  • 进行结构-活动关系研究,分子建模和模拟.

主要成果:

  • 揭示了camlipixant的P2X3受体上一个以前未知的药物结合部位.
  • 证明卡姆利皮克桑作为P2X3.3的全抑制剂起作用.
  • 确定了负责卡姆利皮克桑特选择性P2X3对抗性的关键结构特征.

结论:

  • 这项研究为camlipixant的P2X3受体对抗提供了第一个结构性见解.
  • 卡姆利皮克桑的全抑制机制和选择性结合部位为P2X3向提供了新的理解.
  • 这些发现为改善慢性咳和相关疾病的药物设计铺平了道路.