Assays for screening activity of modulators of members of the hydroxy steroid (17-beta) dehydrogenase (HSD17B) family
申请人:Regeneron Pharmaceuticals, Inc.
公开号:US11479802B2
公开(公告)日:2022-10-25
Screening methods as well as kits for identifying modulators of hydroxysteroid (17-beta) dehydrogenase (HSD17B) family member proteins, such as HSD17B13, are provided. The methods comprise screening molecules for their capacity to modulate the HSD17B family member protein, including inhibiting the HSD17B family member protein, as measured by substrate depletion, product concentration from the HSD17B family member protein substrate conversion or NADH concentration, levels of labeled substrate, luciferin light emission, or combinations thereof. Inhibitors of HSD17B family member proteins identified through the screening methods may be used to treat liver diseases, disorders, or conditions in which the HSD17B family member protein plays a role.
本发明提供了用于鉴定羟基类固醇(17-beta)脱氢酶(HSD17B)家族成员蛋白(如 HSD17B13)调节剂的筛选方法和试剂盒。这些方法包括筛选分子,以确定其调节 HSD17B 家族成员蛋白的能力,包括抑制 HSD17B 家族成员蛋白的能力,通过底物耗竭、HSD17B 家族成员蛋白底物转化产物浓度或 NADH 浓度、标记底物水平、荧光素发光或其组合来测量。通过筛选方法鉴定的 HSD17B 家族成员蛋白的抑制剂可用于治疗 HSD17B 家族成员蛋白起作用的肝脏疾病、失调或病症。