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In Situ Inhibitor Synthesis and Screening by Fluorescence Polarization: An Efficient Approach for Accelerating Drug Discovery
Angewandte Chemie International Edition ( IF 16.6 ) Pub Date : 2022-09-16 , DOI: 10.1002/anie.202211510
Zhihong Li 1 , Yue Wu 1 , Shuai Zhen 1 , Kaijun Su 1 , Linjian Zhang 1 , Fulai Yang 1 , Michael A McDonough 2 , Christopher J Schofield 2 , Xiaojin Zhang 1
Affiliation  

In situ inhibitor synthesis and screening (ISISS) links high-throughput bioorthogonal synthesis with screening tor target binding by fluorescence, as exemplified by the efficient identification of in vivo orally active inhibitors of PHD2, a target for anemia treatment.

中文翻译:

原位抑制剂合成和荧光偏振筛选:加速药物发现的有效方法

原位抑制剂合成和筛选 (ISISS) 将高通量生物正交合成与通过荧光筛选靶点结合联系起来,例如有效鉴定 PHD2 的体内口服活性抑制剂,贫血治疗靶点。
更新日期:2022-09-16
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