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双硫化物受约束的基架使得一个强大的治疗发现平台成为可能

Lijuan Zhou¹, Fei Cai¹, Yanjie Li²

¹Departments of Biological Chemistry, Genentech, Inc., South San Francisco, California, United States of America.

|March 28, 2024

概括

双硫化物受约束 (DCPs) 为治疗开发提供了一个稳定的,类似药物的支架. 这项研究提供了一个强大的平台,使用DCP和菌体显示来发现和优化类疗法,展示了成功的HtrA1蛋白酶抑制剂和高亲和度Notch2配体.

科学领域:

生物化学生物化学
分子生物学分子生物学
药物发现药物发现药物发现

背景情况:

类是有前途的治疗剂,但往往缺乏稳定性.
双硫化物受约束 (DCPs) 提供增强的化学和物理稳定性.
DCPs提供类似于毒品的架构,易于工程设计.

研究的目的:

建立一个强大的平台,用于发现使用DCP支架的疗法.
评估平台对功能性命中发现的有效性.
为了证明治疗候选人的击中到领先的进展.

主要方法:

使用七种不同的DCP支架 (2 x 10^11多样性) 构建多种菌体显示库.
从DCP库中选择和合成.
对已识别的结合剂应用的亲和度成熟策略.

主要成果:

功能性发现的高成功率,与合成抗体库相提并论.
产生功能性的HtrA1蛋白酶抑制剂.
优化弱的Notch2结合剂从微分子到纳米分子的亲和力.

结论:

开发的平台是有效的发现和优化疗法.
DCP 作为创造稳定和强大的类药物的有价值的支架.
该平台为药物开发提供了可行的从成功到成功的进展.

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