Discovery of Pyrimidinediamine Derivatives as Potent Methuosis Inducers for the Treatment of Triple-Negative Breast Cancer

KIZ OpenIR > 科研部门 > 肿瘤生物学（陈策实）

	Discovery of Pyrimidinediamine Derivatives as Potent Methuosis Inducers for the Treatment of Triple-Negative Breast Cancer
	He, J; Wang, LZ; Mi, DZ; Guan, T; Liu, WJ; He, P; Gu, HJ; Li, YZ; Peng, YR; Jia, AQ; Chen, CS; Chen, YH
	2023
发表期刊	JOURNAL OF MEDICINAL CHEMISTRY
ISSN	0022-2623
卷号	66 期号:11 页码:7421-7437
摘要	Triple-negativebreast cancer (TNBC) is a leading malignancyamongwomen that currently lack effective targeted therapeutic agents, andthe limitations of treatment have prompted the emergence of new strategies.Methuosis is a novel vacuole-presenting cell death modality that promotestumor cell death. Hence, a series of pyrimidinediamine derivativeswere designed and synthesized through evaluation of their abilitiesthat inhibit proliferation as well as induce methuosis against TNBCcells. Among them, JH530 showed excellent anti-proliferativeactivities and vacuolization capacity in TNBC. The mechanism researchindicated that JH530 caused cell death through inducingmethuosis of cancer cells. Furthermore, JH530 inhibitedtumor growth remarkably in the HCC1806 xenograft model without anapparent decrease in body weight. Overall, JH530 is amethuosis inducer that displayed remarkable suppression of TNBC growth in vitro and in vivo, which provides abasis for the future progress of more small molecules for TNBC treatment.
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/152453/14183
专题	科研部门_肿瘤生物学（陈策实）
推荐引用方式 GB/T 7714	He, J,Wang, LZ,Mi, DZ,et al. Discovery of Pyrimidinediamine Derivatives as Potent Methuosis Inducers for the Treatment of Triple-Negative Breast Cancer[J]. JOURNAL OF MEDICINAL CHEMISTRY,2023,66(11):7421-7437.
APA	He, J.,Wang, LZ.,Mi, DZ.,Guan, T.,Liu, WJ.,...&Chen, YH.(2023).Discovery of Pyrimidinediamine Derivatives as Potent Methuosis Inducers for the Treatment of Triple-Negative Breast Cancer.JOURNAL OF MEDICINAL CHEMISTRY,66(11),7421-7437.
MLA	He, J,et al."Discovery of Pyrimidinediamine Derivatives as Potent Methuosis Inducers for the Treatment of Triple-Negative Breast Cancer".JOURNAL OF MEDICINAL CHEMISTRY 66.11(2023):7421-7437.

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