Targeting KRAS mutant cancers: from druggable therapy to drug resistance

doi:10.1186/s12943-022-01629-2

HFCAS OpenIR

	Targeting KRAS mutant cancers: from druggable therapy to drug resistance
	Zhu, Chunxiao 1,2; Guan, Xiaoqing 1,3; Zhang, Xinuo 1,4; Luan, Xin 5,6; Song, Zhengbo 1; Cheng, Xiangdong 1,3; Zhang, Weidong 5,6,7; Qin, Jiang-Jiang 1,2,3
	2022-08-04
发表期刊	MOLECULAR CANCER
通讯作者	Cheng, Xiangdong(chengxd@zjcc.org.cn) ; Zhang, Weidong(wdzhangy@hotmail.com) ; Qin, Jiang-Jiang(jqin@ucas.ac.cn)
摘要	Kirsten Rat Sarcoma Viral Oncogene Homolog (KRAS) is the most frequently mutated oncogene, occurring in a variety of tumor types. Targeting KRAS mutations with drugs is challenging because KRAS is considered undruggable due to the lack of classic drug binding sites. Over the past 40 years, great efforts have been made to explore routes for indirect targeting of KRAS mutant cancers, including KRAS expression, processing, upstream regulators, or downstream effectors. With the advent of KRAS (G12C) inhibitors, KRAS mutations are now druggable. Despite such inhibitors showing remarkable clinical responses, resistance to monotherapy of KRAS inhibitors is eventually developed. Significant progress has been made in understanding the mechanisms of drug resistance to KRAS-mutant inhibitors. Here we review the most recent advances in therapeutic approaches and resistance mechanisms targeting KRAS mutations and discuss opportunities for combination therapy.
关键词	KRAS mutations Druggable Resistance Combination therapy
DOI	10.1186/s12943-022-01629-2
关键词[WOS]	COLONY-STIMULATING FACTOR ; ACQUIRED-RESISTANCE ; LUNG ADENOCARCINOMA ; PI3K INHIBITORS ; MEK INHIBITION ; PHASE-II ; RAS ; EGFR ; KINASE ; RECEPTOR
收录类别	SCI
语种	英语
资助项目	Key Laboratory of Prevention, Diagnosis and Therapy of Upper Gastrointestinal Cancer of Zhejiang Province[2022E10021] ; Medical Science and Technology Project of Zhejiang Province[WKJ-ZJ-2202] ; Program of Zhejiang Provincial TCM Sci-tech Plan[2020ZZ005] ; National Key R&D Program of China[2021YFA0910100] ; Shanghai Frontiers Science Center of TCM Chemical Biology, and Innovation Team and Talents Cultivation Program of National Administration of Traditional Chinese Medicine[ZYYCXTD-D-202004]
项目资助者	Key Laboratory of Prevention, Diagnosis and Therapy of Upper Gastrointestinal Cancer of Zhejiang Province ; Medical Science and Technology Project of Zhejiang Province ; Program of Zhejiang Provincial TCM Sci-tech Plan ; National Key R&D Program of China ; Shanghai Frontiers Science Center of TCM Chemical Biology, and Innovation Team and Talents Cultivation Program of National Administration of Traditional Chinese Medicine
WOS研究方向	Biochemistry & Molecular Biology ; Oncology
WOS类目	Biochemistry & Molecular Biology ; Oncology
WOS记录号	WOS:000835692300001
出版者	BMC
引用统计	被引频次：62[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	http://ir.hfcas.ac.cn:8080/handle/334002/132193
专题	中国科学院合肥物质科学研究院
通讯作者	Cheng, Xiangdong; Zhang, Weidong; Qin, Jiang-Jiang
作者单位	1.Univ Chinese Acad Sci, Chinese Acad Sci, Zhejiang Canc Hosp, Inst Basic Med & Canc IBMC,Canc Hosp, Hangzhou 310022, Peoples R China 2.UCAS, Hangzhou Inst Adv Study, Sch Mol Med, Hangzhou 310024, Peoples R China 3.Key Lab Prevent Diag & Therapy Upper Gastrointest, Hangzhou 310022, Peoples R China 4.Zhejiang Univ Technol, Coll Pharmaceut Sci, Hangzhou 310032, Peoples R China 5.Shanghai Univ Tradit Chinese Med, Inst Interdisciplinary Integrat Med Res, Shanghai 201203, Peoples R China 6.Shanghai Univ Tradit Chinese Med, Shuguang Hosp, Shanghai 201203, Peoples R China 7.Second Mil Med Univ, Sch Pharm, Shanghai 200433, Peoples R China
推荐引用方式 GB/T 7714	Zhu, Chunxiao,Guan, Xiaoqing,Zhang, Xinuo,et al. Targeting KRAS mutant cancers: from druggable therapy to drug resistance[J]. MOLECULAR CANCER,2022,21.
APA	Zhu, Chunxiao.,Guan, Xiaoqing.,Zhang, Xinuo.,Luan, Xin.,Song, Zhengbo.,...&Qin, Jiang-Jiang.(2022).Targeting KRAS mutant cancers: from druggable therapy to drug resistance.MOLECULAR CANCER,21.
MLA	Zhu, Chunxiao,et al."Targeting KRAS mutant cancers: from druggable therapy to drug resistance".MOLECULAR CANCER 21(2022).