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使用菌体显示,和突变发生和计算建模的方法,发现和药理性地表征化学激素网络抑制剂

Serena Vales¹, Jhanna Kryukova¹, Soumyanetra Chandra¹

¹Wellcome Centre for Human Genetics and RDM Cardiovascular Medicine, University of Oxford, Roosevelt Drive, Oxford, OX3 7BN, UK.

Nature communications

|September 16, 2023

概括

科学家们发现了来自的短,它们广泛向炎症化学因子 (CC和CXC). 这些可以通过阻断化基因网络,克服药物耐药性来显示治疗潜力.

科学领域:

免疫学和分子生物学
药物发现和药理学

背景情况:

化基因 (CC和CXC) 是炎症和免疫细胞迁移的关键调节者.
化基因网络的冗余性对开发有效的抗炎药物提出了挑战.
众所周知,脱素与CC和CXC化学激素结合,这表明一种潜在的治疗策略.

研究的目的:

为了识别具有广泛的抗化基因活性的小.
描述这些的功能动机和结合相互作用.
为了评估这些的治疗潜力,阻断化学激素驱动的炎症.

主要方法:

用多个CC和CXC化学基因并行进行菌体显示查,以识别逃避性.
和突变发生因子的菌体显示和化学毒素测试以确定必需氨基酸残留物和基因.
AlphaFold2-Multimer建模用于预测-化学结合相互作用和作用机制.

主要成果:

识别来自的短,这些短可以随意结合CC和CXC化学因子.
在这些中发现了两种保存的基因,对阴离子补丁和疏水/芳香/半氨酸残留物有特定的功能要求.
计算建模表明,可以通过离子和疏水相互作用来遮CC和CXC化学因子上的不同的受体结合部位.

结论:

滴虫可以作为识别广谱抗化学类的来源.
这种特征的药理为设计针对炎症性化学因子网络的新疗法提供了基础.
这些发现突出了在炎症性疾病的药理干预中克服化学激素冗余性的有希望的策略.

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