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.

Chang, Xiaosa; Sun, Dejuan; Shi, Danfeng; Wang, Guan; Chen, Yanmei; Zhang, Kai; Tan, Huidan; Liu, Jie; Liu, Bo; Ouyang, Liang

Design, synthesis, and biological evaluation of quinazolin-4(3H)-one derivatives co-targeting poly(ADP-ribose) polymerase-1 and bromodomain containing protein 4 for breast cancer therapy.

Chang, Xiaosa; Sun, Dejuan; Shi, Danfeng; Wang, Guan; Chen, Yanmei; Zhang, Kai; Tan, Huidan; Liu, Jie; Liu, Bo; Ouyang, Liang.

Afiliación

Chang X; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu 610041, China.
Sun D; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu 610041, China.
Shi D; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu 610041, China.
Wang G; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu 610041, China.
Chen Y; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu 610041, China.
Zhang K; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu 610041, China.
Tan H; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu 610041, China.
Liu J; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu 610041, China.
Liu B; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu 610041, China.
Ouyang L; State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu 610041, China.

Acta Pharm Sin B ; 11(1): 156-180, 2021 Jan.

Article en En | MEDLINE | ID: mdl-33532187

Palabras clave

BC, breast cancer; BET, bromodomain and extra-terminal domain; BRCA1/2, breast cancer susceptibility gene 1/2; BRD4; BRD4, bromodomain 4; CDK4/6, cyclin-dependent kinase 4/6; DSB, DNA double-strand break; Dual-target inhibitor; EGFR, epidermal growth factor receptor; ELISA, enzyme linked immunosorbent assay; ER, estrogen receptor; ESI-HR-MS, high-resolution mass spectra; FDA, U.S. Food and Drug Administration; FITC, fluorescein isothiocyanate isomer I; HE, hematoxylin-eosin; HPLC, high-performance liquid chromatography; HR, homologous recombination; HRD, homologous recombination deficiency; IHC, immunohistochemistry; NHEJ, nonhomologous end-joining; PARP1; PARP1, poly(ADP-ribose) polymerase-1; PI, propidium iodide; PK, pharmacokinetics; PPI, protein−protein interaction; Quinazolin-4(3H)-one derivatives; SAR, structureactivity relationship; SOP, standard operation process; Synthetic lethality; TCGA, the cancer genome atlas; TGI, tumor growth inhibition; TLC, thin-layer chromatography; TNBC, triple-negative breast cancer; TR-FRET, time-resolved fluorescence resonance energy transfer.; shRNA, short hairpin RNA

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Texto completo: 1 Base de datos: MEDLINE Tipo de estudio: Prognostic_studies Idioma: En Revista: Acta Pharm Sin B Año: 2021 Tipo del documento: Article País de afiliación: China

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