Abstract:
:A high-throughput 32D(L858R/T790M) cell-based assay to identify inhibitors of the L858R/T790M mutant epidermal growth factor receptor (EGFR) pathway was established. After screening, ten hits from among 60,000 compounds in our in-house compound library were initially identified. In the secondary assays, one hit, 1-[2-(decyloxy)-2-oxoethyl]-3-methyl-2-[(4-methylphenoxy) methyl]-1H-benzimidazol-3-ium, was confirmed to directly inhibit the kinase activity of recombinant L858R/T790M EGFR and the phosphorylation of EGFR-L858R/T790M in gefitinib-resistant H1975 cells. Thus, this high-throughput assay system may be useful for identifying novel inhibitors which suppress mutant EGFR-T790M signalling and for overcoming T790M-mediated acquired resistance for future anticancer drug discovery.
journal_name
Anticancer Resjournal_title
Anticancer researchauthors
Lin WH,Song JS,Lien TW,Chang CY,Wu SH,Huang YW,Chang TY,Fang MY,Yen KJ,Chen CH,Chu CY,Hsieh HP,Chen YR,Chao YS,Hsu JTsubject
Has Abstractpub_date
2012-01-01 00:00:00pages
147-51issue
1eissn
0250-7005issn
1791-7530pii
32/1/147journal_volume
32pub_type
杂志文章abstract::To elucidate the rates of appearance of hepatocellular carcinoma (HCC) and the prognosis of alcoholic liver cirrhosis upon infection with hepatitis virus, we retrospectively studied 190 consecutive patients. The patients were divided into three groups based on whether they were exposed either to hepatitis B virus (HBV...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2001-07-01 00:00:00
abstract:BACKGROUND:The determination of dihydropyrimidine dehydrogenase (DPD) deficiency is important in avoiding severe 5-fluorouracil (FU) toxicity. The dihydrouracil (UH2)-uracil (Ura) ratio (UH2/Ura) in plasma might be an important indicator of the risk of 5-FU catabolic deficiency. In order to clarify this possibility, th...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2006-09-01 00:00:00
abstract:AIM:To analyze female gender as a possible age-dependent prognostic factor for overall (OS) and cancer-specific survival (CSS) in patients with upper urinary tract urothelial carcinoma (UUTUC) after radical nephroureterectomy (RNU). PATIENTS AND METHODS:A total of 167 men and 101 women with UUTUC treated with RNU with...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2015-07-01 00:00:00
abstract::To determine the changes in biological features of the prostate during the course of local recurrence of prostate cancer after endocrine therapy, histologic grade, proliferating activity and apoptotic indices were examined in prostate specimens obtained before treatment and at recurrence. A total of 16 patients, who h...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2000-03-01 00:00:00
abstract:BACKGROUND:Matrix metalloproteinase 9 (MMP-9) plays an important role in cancer invasion and metastasis. The relationship between serum MMP-9 levels and clinicopathological factors in gastric cancer patients is not clear. MATERIALS AND METHODS:Preoperative serum was obtained from 170 patients who had undergone gastrec...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2000-03-01 00:00:00
abstract:BACKGROUND:Taxane-based chemotherapy is useful for peritoneal dissemination control in advanced/recurrent gastric cancer; however, insufficient relative dose intensity (RDI) may preclude disease control achievement. Nab-paclitaxel, with high tumour permeability, is a promising second- or later-line treatment. PATIENTS...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.11622
更新日期:2017-05-01 00:00:00
abstract::The electrophysiological effects of gallium chloride (Ga ) and its activity on arrhythmias induced by digitalis were investigated in guinea pig papillary muscle. KCl microelectrodes were used to record transmembrane electrical activity from Purkinje cells from the papillary muscle of guinea pig hearts during superfusi...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1996-01-01 00:00:00
abstract::To determine the group of patients for whom a biological response modifier is useful, the efficacy of postoperative adjuvant immunotherapy was investigated with regard to infiltration of dendritic cells (DC) in patients with advanced gastric cancer who underwent absolute curative resection. The infiltration of DC was ...
journal_title:Anticancer research
pub_type: 临床试验,杂志文章
doi:
更新日期:1992-05-01 00:00:00
abstract:AIM:To evaluate the role of radiotherapy alone or combined with chemotherapy in the treatment of recurrent vulvar cancer, emphasising the prognostic factors and outcomes. MATERIALS AND METHODS:Twenty women with loco-regional recurrence of vulvar carcinoma were retrospectively reviewed. Eleven patients were managed wit...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2003-05-01 00:00:00
abstract::Interleukin-10 (IL-10) is an immunosuppressive cytokine involved in carcinogenesis via immune escape. The present study aimed at evaluating the contribution of IL-10 promoter A-1082G (rs1800896), T-819C (rs3021097), A-592C (rs1800872) genetic polymorphisms to the risk of lung cancer in Taiwan. Associations of three IL...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2014-12-01 00:00:00
abstract::The role of extracellular amines such as noradrenaline and serotonin and their interaction with cyclic nucleotides and intracellular polyamines in the regulation of intestinal epithelial cell proliferation is reviewed with particular reference to the differences between normal and neoplastic cells. In respect to the n...
journal_title:Anticancer research
pub_type: 杂志文章,评审
doi:
更新日期:1987-01-01 00:00:00
abstract:BACKGROUND:Amrubicin is an active agent for the treatment of small-cell lung cancer (SCLC). However, there have been no reports of long-term amrubicin use. PATIENTS AND METHODS:Twelve patients with SCLC who were treated with eight or more cycles of amrubicin chemotherapy were retrospectively reviewed. RESULTS:The med...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2012-04-01 00:00:00
abstract:BACKGROUND/AIM:High-mobility group box 1 (HMGB1) is a nuclear DNA-binding protein that exerts a range of proinflammatory actions when it is secreted extracellularly. We hypothesized that HMGB1 released from damaged cells in pituitary apoplexy would exacerbate the neurological symptoms due to acute inflammation. PATIEN...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.13624
更新日期:2019-08-01 00:00:00
abstract:BACKGROUND:The genetic basis of sinonasal inverted papilloma (SNIP)-derived squamous cell carcinoma (SCC) has not yet been well characterized. AIM:To characterize the genetic abnormalities of SNIP and SNIP-derived SCC and to uncover their differences. MATERIALS AND METHODS:Mutations of 409 genes were analyzed using a...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.14752
更新日期:2021-01-01 00:00:00
abstract:BACKGROUND:To improve long-term survival by reducing toxicity in intermediate stage Hodgkin's disease patients, we compared the effects of involved field (IF) versus extended field (EF) irradiation administered after four cycles of ABVD regimen. MATERIALS AND METHODS:Two hundred and ten Hodgkin's disease patients, at ...
journal_title:Anticancer research
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:
更新日期:2004-11-01 00:00:00
abstract:BACKGROUND:The purpose of the study was to test the feasibility of laser scanning cytometry (LSC) to simultaneously measure estrogen receptor (ER) and nucleolin (NU) expression in the nuclei of the same individual breast cancer cells. MATERIALS AND METHODS:Cancer cells from 64 breast tumors were labeled with anti-NU a...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2004-03-01 00:00:00
abstract:UNLABELLED:The aim of this study was to evaluate the utility of HER2/neu ECD concentration as a marker of the efficacity of clinical response to Herceptin. PATIENTS AND METHODS:Iterative measurements of HER2/neu ECD (ELISA c-erbB2/c-neu Rapid Format Elisa kit QIA10 Calbiochem) concentrations in 45 patients treated wit...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2009-05-01 00:00:00
abstract:BACKGROUND/AIM:Sarcoma of the oral cavity is rare accounting for around 1% of all malignant oral tumors. The purpose of this study was to find important prognostic factors for patients with oral sarcoma. PATIENTS AND METHODS:The study included 1,643 patients examined from April 1980 to March 2010 at the Departments of...
journal_title:Anticancer research
pub_type: 杂志文章,多中心研究
doi:
更新日期:2015-08-01 00:00:00
abstract::This epidemiological study was performed to evaluate the influence of postoperative complementary treatment with lectin-standardized mistletoe extract (sME) on breast cancer patients. The design (retrolective cohort analysis with parallel groups) and conduct of the study were in agreement with current standards for pr...
journal_title:Anticancer research
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:
更新日期:2003-11-01 00:00:00
abstract::Chk1 (checkpoint kinase 1) is a serine-threonine kinase that is critical for G2/M arrest in response to DNA damage. Chk1 phosphorylates Cdc25C at serine-216, a major regulatory site, in response to DNA damage. Furthermore, Chk1 also phosphorylates Cdc25A on serine 123 which accelerates its degradation through the ubiq...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2004-11-01 00:00:00
abstract:BACKGROUND:Primary small cell carcinoma of the ovary (SCCO) is rare, making prognosis and outcomes largely undefined. PATIENTS AND METHODS:Using case listing session of SEER 18 (1973-2010), we examined outcomes for patients with SCCO. Analyses were conducted with SEER(*)Stat 8.1.2, Microsoft Excel 2007 and GraphPad Pr...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2015-05-01 00:00:00
abstract:BACKGROUND:Metastatic breast cancer remains a major clinical issue despite progress achieved in recent years. Three randomised trials have demonstrated the benefit of combining bevacizumab with various taxane schedules. Herein, this study sought to investigate an alternative bevacizumab-taxane regimen as first-line tre...
journal_title:Anticancer research
pub_type: 临床试验,杂志文章
doi:
更新日期:2010-07-01 00:00:00
abstract::We carried out a systematic review of new drugs active in non-small cell lung carcinoma (NSCLC). Fifty five phase II and III trials were reviewed (vinorelbine (19 trials), paclitaxel (15), gemcitabine (11), docetaxel (6), topotecan (2) or irinotecan (2)). The first four ones could be considered as active drugs when gi...
journal_title:Anticancer research
pub_type: 杂志文章,评审
doi:
更新日期:1999-09-01 00:00:00
abstract::During intercellular induction of apoptosis, transformed fibroblasts are eliminated through the action of neighbouring nontransformed cells. TGF-beta thereby plays three distinct and central roles. a) TGF-beta released by transformed cells or added exogenously to the assay system triggers nontransformed cells to relea...
journal_title:Anticancer research
pub_type: 杂志文章,评审
doi:
更新日期:1999-01-01 00:00:00
abstract::Cell proliferation measurements using bromodeoxyuridine administration to patients and flow cytometry to measure Tpot in head and neck cancer are discussed. Several hundred patients have now been assessed and the majority of studies suggest that this group of tumours represent a relatively fast proliferating site with...
journal_title:Anticancer research
pub_type: 杂志文章,评审
doi:
更新日期:1998-11-01 00:00:00
abstract:BACKGROUND:C-reactive protein (CRP) is the prototypical biomarker of inflammation. Genetic variations within the CRP gene have been shown to be associated with alterations of CRP expression and prognosis in cancer patients. The purpose of this study was to evaluate the association between four polymorphisms of the CRP ...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2011-06-01 00:00:00
abstract::Clinical and hematological parameters, and three derived major staging systems were compared with DNA-cytometric parameters in 73 patients with newly diagnosed multiple myeloma (MM) and correlated in univariate analysis with survival to assess their predictive value. Regarding diagnostic validity, a multi-parameter sy...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1994-09-01 00:00:00
abstract::Within the brain, dissemination of glioma cells follows myelinated fiber tracts and extracellular matrix containing structures such as the basement membranes of blood vessels. These patterns represent the two major routes of invasion frequently observed in clinical disease. Previously, we have characterized the substr...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1998-07-01 00:00:00
abstract:BACKGROUND:The mammalian target of rapamycin (mTOR) controls cell growth through protein synthesis regulation. It can be activated by protein kinase B (AKT) or through ribosomal S6 kinase (S6K1). In malignant glioma, mTOR inhibitors have antiproliferative and proapoptotic effects and mTOR has been suggested as a target...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2009-08-01 00:00:00
abstract:BACKGROUND/AIM:γδ T cells mediate cytotoxicity against prostate cancer (PCa) cells in vitro; however, the clinical efficacy of γδ T cell-targeted immunotherapy for recurrent and metastatic PCa is unsatisfactory. We hypothesized that the resistance of recurrent and metastatic PCa to γδ T cells is related to the presence...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.14559
更新日期:2020-10-01 00:00:00