CDK9 targeting PROTAC L055 inhibits ERα-positive breast cancer

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	CDK9 targeting PROTAC L055 inhibits ERα-positive breast cancer
	Chen, WM; Wu, Y; Yang, CY; Ren, WL; Hou, L; Liang, HC; Wu, TY; Kong, YJ; Wu, J; Rao, Y; Chen, CS
	2024
发表期刊	BIOMEDICINE & PHARMACOTHERAPY
ISSN	0753-3322
卷号	177
摘要	Breast cancer is one of the most prevalent malignancies affecting women worldwide, underscoring the urgent need for more effective and specific treatments. Proteolysis-targeting chimeras (PROTACs) have emerged as a promising strategy to develop new lead compounds by selectively targeting oncoproteins for degradation. In this study, we designed, synthesized and evaluated a CRBN-based PROTAC, L055, which targets CDK9. Our findings demonstrate that L055 effectively inhibits the proliferation, induces cell cycle arrest, and decreases the survival of ER alpha-positive breast cancer cells in vitro. L055 specifically binds to CDK9, facilitating its degradation via the CRBN-dependent proteasomal pathway. Additionally, L055 suppressed the growth of organoids and tumors derived from T47D and MCF7 cells in nude mice. Thus, L055 represents a potential novel therapeutic agent for ER alpha-positive breast cancer and potentially other malignancies.
收录类别	SCI
语种	英语
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/14560
专题	科研部门_肿瘤生物学（陈策实）
推荐引用方式 GB/T 7714	Chen, WM,Wu, Y,Yang, CY,et al. CDK9 targeting PROTAC L055 inhibits ERα-positive breast cancer[J]. BIOMEDICINE & PHARMACOTHERAPY,2024,177.
APA	Chen, WM.,Wu, Y.,Yang, CY.,Ren, WL.,Hou, L.,...&Chen, CS.(2024).CDK9 targeting PROTAC L055 inhibits ERα-positive breast cancer.BIOMEDICINE & PHARMACOTHERAPY,177.
MLA	Chen, WM,et al."CDK9 targeting PROTAC L055 inhibits ERα-positive breast cancer".BIOMEDICINE & PHARMACOTHERAPY 177(2024).

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CCS2025040703.pdf（10252KB）	期刊论文	出版稿	开放获取	CC BY-NC-SA	请求全文