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使用酶激活光探针对抗GLP-1降解的DPPIV抑制剂的高通量查

Ming Zhang^1,2, Shengui He¹, Chaoyan Han³

¹State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024, China.

Analytical chemistry

|December 29, 2024

概括

研究人员开发了一种新的光探针DBX-AP,用于实时监测二二酶IV (DPPIV) 活性. 该工具有助于发现新的DPPIV抑制剂用于治疗糖尿病.

科学领域:

生物化学生化学
酶学是一种酶学.
药理学药理学是指药理学的学科.

背景情况:

双基酶IV (DPPIV) 是一种在各种生理过程中至关重要的外酶.
DPPIV 抑制剂是已知的糖尿病 (DM) 治疗方法.
需要有效的方法来选和识别新型DPPIV抑制剂.

研究的目的:

设计和验证远红色光探头DBX-AP,用于实时监测DPPIV活动.
开发使用DBX-AP的DPPIV抑制剂的视觉高通量查 (HTS) 方法.
从化合物库中识别新型DPPIV抑制剂.

主要方法:

分子对接模拟和DPPIV的功能特征被用来设计DBX-AP探头.
使用DBX-AP来建立DPPIV抑制剂的视觉HTS测定.
进行了体外和体内研究,以评估DPPIV活性和抑制剂在小鼠和肠道微生物群中的有效性.

主要成果:

该DBX-AP探测器使得DPPIV活动的快速,选择性和实时监控成为可能.
一个HTS运动确定了三个强大的DPPIV抑制剂 (K784-2660,6484-0066,E699-0153).
已识别的抑制剂抑制了小鼠皮质中的DPPIV活性,减少GLP-1降解,以及肠道微生物群.

结论:

DBX-AP是评估DPPIV活性和发现新型DPPIV抑制剂的宝贵工具.
开发的HTS方法为发现糖尿病新疗法提供了一个有前途的方法.
针对宿主和肠道微生物群中的DPPIV是一种潜在的DM治疗策略.

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