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Challenges for the Discovery of Non-Covalent WRN Helicase Inhibitors
ChemMedChem ( IF 3.4 ) Pub Date : 2024-02-09 , DOI: 10.1002/cmdc.202300613
Alisa Heuser 1 , Wassim Abdul Rahman 1 , Elisabeth Bechter 1 , Jutta Blank 2 , Sylvia Buhr 3 , Dirk Erdmann 4 , Patrizia Fontana 4 , Fanny Mermet-Meillon 4 , Marco Meyerhofer 4 , Ross Strang 5 , Maxime Schrapp 4 , Catherine Zimmermann 4 , Marta Cortes-Cros 4 , Henrik Möbitz 5 , Jacques Hamon 1
Affiliation  

One of the major hurdles in targeting WRN helicase is to overcome the challenge of false positives in screening due to the high propensity of WRN to protein interferences. Biochemical and biophysical fingerprints of hits allow to triage the hits and highlight the artefacts, including compounds (ML216 and NSC617145) wrongly considered as specific WRN probes.

中文翻译:

发现非共价 WRN 解旋酶抑制剂面临的挑战

靶向 WRN 解旋酶的主要障碍之一是克服由于 WRN 极易受到蛋白质干扰而导致的筛选假阳性的挑战。命中的生化和生物物理指纹可以对命中进行分类并突出显示人工制品,包括被错误地视为特定 WRN 探针的化合物(ML216 和 NSC617145)。
更新日期:2024-02-09
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