Antibody–drug conjugates (ADCs) are a novel modality that allows targeted delivery of potent therapeutic agents to the desired site. Herein we report our discovery of NAMPT inhibitors as a novel nonantimitotic payload for ADCs. The resulting anti-c-Kit conjugates (ADC-3 and ADC-4) demonstrated in vivo efficacy in the c-Kit positive gastrointestinal stromal tumor GIST-T1 xenograft model in a target-dependent manner.

中文翻译：

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烟酰胺磷酸核糖基转移酶抑制剂作为抗体-药物缀合物的新型有效负载

抗体-药物偶联物（ADC）是一种新型药物，可将有效的治疗药物靶向递送至所需部位。在这里，我们报告我们发现NAMPT抑制剂作为ADC的新型非抗有丝分裂有效负载。所得的抗c-Kit缀合物（ADC-3和ADC-4）在c-Kit阳性胃肠道间质瘤GIST-T1异种移植模型中以靶标依赖性方式表现出体内功效。