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抗体蛋白酶抑制剂的合理设计

Tao Liu¹, Guangsen Fu², Xiaozhou Luo¹

¹†Department of Chemistry and the Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, California 92037, United States.

Journal of the American Chemical Society

|March 17, 2015

概括

研究人员设计了一种新的牛抗体支架,以创建强大的蛋白酶抑制剂. 这种新策略产生了高度选择性的抗体,向涉及人类疾病的酶.

科学领域:

免疫学和生物化学
蛋白质工程是指蛋白质工程.
药物发现药物发现药物发现

背景情况:

抗体具有独特的结构特征,例如牛抗体BLV1H12中的超长CDR3H,这为新的功能工程提供了潜力.
细胞外蛋白酶在各种人类疾病中起着重要的作用,使它们成为有吸引力的治疗点.

研究的目的:

使用BLV1H12支架设计基于抗体的新型蛋白酶抑制剂.
开发针对目标蛋白酶的强效和选择性抑制剂,如牛素和人类中性粒细胞弹性酶 (HNE).

主要方法:

用蛋白酶抑制剂序列修改BLV1H12抗体的β链茎.
工程抗体的生成和表征,包括人性化的变体.
对针对蛋白酶的产生的抗体的亲和性和选择性评估.

主要成果:

工程抗体表明牛素和人类中性粒细胞弹性酶 (HNE) 的低纳米分子抑制.
成功生成了一种与BLV1H12具有高度同质性的人性化变体.
进一步的优化导致了具有亚纳米系亲和力的高度选择性人性化抗HNE抗体.

结论:

BLV1H12抗体支架是一个多功能平台,用于设计强效和选择性蛋白酶抑制剂.
这种新的策略为开发抗体治疗方法提供了有前途的方法,用于对抗涉及人类疾病的细胞外蛋白酶.

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