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针对三阴性乳腺癌的关键激酶通路的小分子抑制剂的最新研究进展。

Recent advancement in developing small molecular inhibitors targeting key kinase pathways against triple-negative breast cancer.

机构信息

School of Pharmacy, Monash University Malaysia, Jalan Lagoon Selatan, Bandar Sunway, Selangor Darul Ehsan 47500, Malaysia.

Faculty of Pharmacy and Health Sciences, Universiti Kuala Lumpur, Royal College of Medicine Perak, 30450 Ipoh, Perak, Malaysia.

出版信息

Bioorg Med Chem. 2024 Oct 1;112:117877. doi: 10.1016/j.bmc.2024.117877. Epub 2024 Aug 18.

DOI:10.1016/j.bmc.2024.117877
PMID:39159528
Abstract

Triple-negative breast cancer (TNBC) stands out as the most formidable variant of breast cancer, predominantly affecting younger women and characterized by a bleak outlook and a high likelihood of spreading. The absence of safe and effective targeted treatments leaves standard cytotoxic chemotherapy as the primary option. The role of protein kinases, frequently altered in many cancers, is significant in the advancement and drug resistance of TNBC, making them a logical target for creating new, potent therapies against TNBC. Recently, an array of promising small molecules aimed at various kinases have been developed specifically for TNBC, with combination studies showing a synergistic improvement in combatting this condition. This review underscores the effectiveness of small molecule kinase inhibitors in battling the most lethal form of breast cancer and sheds light on prospective pathways for crafting novel treatments.

摘要

三阴性乳腺癌(TNBC)是乳腺癌中最具侵袭性的一种亚型,主要影响年轻女性,预后较差且容易转移。由于缺乏安全有效的靶向治疗药物,标准细胞毒性化疗仍然是主要治疗手段。在 TNBC 的发展和耐药过程中,蛋白激酶经常发生改变,其作用至关重要,因此它们成为开发针对 TNBC 的新型有效治疗方法的合理靶点。最近,专门针对 TNBC 开发了一系列针对多种激酶的有前途的小分子药物,联合研究显示这些药物在治疗这种疾病方面具有协同增效作用。本综述强调了小分子激酶抑制剂在治疗最致命形式的乳腺癌方面的有效性,并为开发新的治疗方法提供了潜在途径。

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