Computational design, chemical synthesis, and biological evaluation of a novel ERK inhibitor (BL-EI001) with apoptosis-inducing mechanisms in breast cancer

Oncotarget

Volumn 6, Issue 9, 2015, Pages 6762-6775

  Liu, Bo ^a   Fu, Leilei ^a   Zhang, Cui ^b   Zhang, Lan ^b   Zhang, Yonghui ^a,c   Ouyang, Liang ^a   He, Gu ^a   Huang, Jian ^b  

^a SICHUAN UNIVERSITY   (China)

^b SHENYANG PHARMACEUTICAL UNIVERSITY   (China)

^c Tsinghua University   (China)

Author keywords

Apoptosis; Breast cancer; ERK inhibitor (bl ei001); Extracellular signal regulated kinase 1 2 (ERK1 2); Mitochondrial pathway

Indexed keywords

ANTINEOPLASTIC AGENT; BL EI 001; CASPASE 3; CASPASE 9; HIGH MOBILITY GROUP B1 PROTEIN; KI 67 ANTIGEN; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 3; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE KINASE 2; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE 1; PROTEIN BAX; PROTEIN BCL 2; RAF PROTEIN; RAS PROTEIN; SMALL INTERFERING RNA; UNCLASSIFIED DRUG; BENZOTHIAZOLE DERIVATIVE; BL-EI001; IMIDAZOLE DERIVATIVE; MITOGEN ACTIVATED PROTEIN KINASE; PROTEIN KINASE INHIBITOR;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; APOPTOSIS; ARTICLE; BREAST CANCER; BREAST CANCER CELL LINE; CELL SURVIVAL; COMPUTER MODEL; CONCENTRATION RESPONSE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DOWN REGULATION; DRUG DESIGN; DRUG EFFICACY; DRUG MECHANISM; DRUG MEGADOSE; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; ENZYME ACTIVATION; ENZYME ACTIVE SITE; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; FEMALE; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; LOW DRUG DOSE; MCF 7 CELL LINE; MDA MB231 CELL LINE; MDA MB468 CELL LINE; MOLECULAR DOCKING; MOLECULAR DYNAMICS; MOUSE; NONHUMAN; PROTEIN EXPRESSION; PROTEOMICS; STRUCTURE ACTIVITY RELATION; TUMOR VOLUME; UPREGULATION; VALIDATION PROCESS; ANIMAL; ANTAGONISTS AND INHIBITORS; BAGG ALBINO MOUSE; BREAST NEOPLASMS; CELL PROLIFERATION; CHEMICAL STRUCTURE; COMPUTER AIDED DESIGN; DOSE RESPONSE; DRUG EFFECTS; ENZYMOLOGY; GENETIC TRANSFECTION; GENETICS; MCF-7 CELL LINE; METABOLISM; MITOCHONDRION; MOLECULARLY TARGETED THERAPY; NUDE MOUSE; PATHOLOGY; PHOSPHORYLATION; PROTEIN PROTEIN INTERACTION; RNA INTERFERENCE; SIGNAL TRANSDUCTION; SYNTHESIS; TIME FACTOR;

ANIMALS; ANTINEOPLASTIC AGENTS; APOPTOSIS; BENZOTHIAZOLES; BREAST NEOPLASMS; CELL PROLIFERATION; COMPUTER-AIDED DESIGN; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; EXTRACELLULAR SIGNAL-REGULATED MAP KINASES; FEMALE; HUMANS; IMIDAZOLES; MCF-7 CELLS; MICE, INBRED BALB C; MICE, NUDE; MITOCHONDRIA; MOLECULAR DOCKING SIMULATION; MOLECULAR STRUCTURE; MOLECULAR TARGETED THERAPY; PHOSPHORYLATION; PROTEIN INTERACTION MAPS; PROTEIN KINASE INHIBITORS; PROTEOMICS; RNA INTERFERENCE; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP; TIME FACTORS; TRANSFECTION; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84927144395     PISSN: None     EISSN: 19492553     Source Type: Journal    
DOI: 10.18632/oncotarget.3105     Document Type: Article

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