换一批Design, synthesis, and biological evaluation of quinazolin-4(3<i>H</i>)-one derivatives co-targeting poly(ADP-ribose) polymerase-1 and bromodomain containing protein 4 for breast cancer therapy.
第一作者：
Xiaosa,Chang
第一单位：
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu 610041, China.
作者：
关键词
BC, breast cancerBET, bromodomain and extra-terminal domainBRCA1/2, breast cancer susceptibility gene 1/2BRD4BRD4, bromodomain 4CDK4/6, cyclin-dependent kinase 4/6DSB, DNA double-strand breakDual-target inhibitorEGFR, epidermal growth factor receptorELISA, enzyme linked immunosorbent assayER, estrogen receptorESI-HR-MS, high-resolution mass spectraFDA, U.S. Food and Drug AdministrationFITC, fluorescein isothiocyanate isomer IHE, hematoxylin-eosinHPLC, high-performance liquid chromatographyHR, homologous recombinationHRD, homologous recombination deficiencyIHC, immunohistochemistryNHEJ, nonhomologous end-joiningPARP1PARP1, poly(ADP-ribose) polymerase-1PI, propidium iodidePK, pharmacokineticsPPI, protein?protein interactionQuinazolin-4(3H)-one derivativesSAR, structure–activity relationshipSOP, standard operation processSynthetic lethalityTCGA, the cancer genome atlasTGI, tumor growth inhibitionTLC, thin-layer chromatographyTNBC, triple-negative breast cancerTR-FRET, time-resolved fluorescence resonance energy transfer.shRNA, short hairpin RNA
DOI
10.1016/j.apsb.2020.06.003
PMID
33532187
发布时间
2021-02-06
- 浏览1
Acta pharmaceutica Sinica. B
2021年11卷1期
156-180页
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