在各种癌症模型中,MCL1抑制剂S63845是可以容忍和有效的
András Kotschy1, Zoltán Szlavik1, James Murray2
1Servier Research Institute of Medicinal Chemistry, Budapest 1031, Hungary.
Nature
|October 28, 2016
概括
一种新型小分子,S63845,在各种癌症中有效向支持生存的肌肉细胞白血病1 (MCL1). 这项突破为治疗多发性骨髓瘤,白血病,淋巴瘤和固体瘤提供了新的治疗策略.
科学领域:
- 癌症学
- 分子生物学
- 药物发现
背景情况:
- 瘤的生长依赖于逃避亡.
- 在许多癌症中,骨髓细胞白血病1 (MCL1) 的过度表达是常见的.
- 开发针对MCL1的临床可行的小分子是困难的.
研究的目的:
- 介绍一个新的小分子抑制剂S63845.
- 在临床前模型中研究S63845的抗癌效果.
主要方法:
- 对MCL1的BH3结合沟的S63845结合亲和性的表征.
- 对S63845在MCL1依赖癌细胞中诱导亡的能力的评估.
- 在体内和组合治疗中评估S63845的抗瘤活性.
主要成果:
- S63845具有很高的亲和力结合MCL1, 抑制其促生存功能.
- 通过BAX/ BAK通路,S63845有效地杀死MCL1依赖的癌细胞 (多发性骨髓瘤,白血病,淋巴瘤).
- 在组合治疗中,S63845表现出强大的体内抗瘤活性,具有良好的安全性和有效性.
结论:
- 对于广泛的癌症,MCL1已被验证为治疗标.
- S63845是一个有前途的新药候选药物,用于针对MCL1的癌症治疗.
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