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PURPOSE Melanomas harbor aberrations in the c-Kit gene. We tested the efficiency of the tyrosine kinase inhibitor imatinib in selected patients with metastatic melanoma harboring c-Kit mutations or amplifications. PATIENTS AND METHODS Forty-three patients with metastatic melanoma harboring c-Kit aberrations were enrolled on this phase II trial. Each(More)
For patients with locally advanced non-small-cell lung cancer (LA-NSCLC), the role of consolidation chemotherapy (CCT) following concurrent chemoradiotherapy (CRT) is partially defined. The aim of this study was to evaluate the efficacy and toxicity of CCT. The characteristics of LA-NSCLC patients treated with curative concurrent CRT from 2001 to 2010 were(More)
The role of the individual histone deacetylases (HDACs) in the regulation of cancer cell proliferation was investigated using siRNA-mediated protein knockdown. The siRNA for HDAC3 and HDAC1 demonstrated significant morphological changes in HeLa S3 consistent with those observed with HDAC inhibitors. SiRNA for HDAC 4 or 7 produced no morphological changes in(More)
ABT-869 is a structurally novel, receptor tyrosine kinase (RTK) inhibitor that is a potent inhibitor of members of the vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptor families (e.g., KDR IC50 = 4 nmol/L) but has much less activity (IC50s > 1 micromol/L) against unrelated RTKs, soluble tyrosine kinases, or(More)
Sulfur dioxide (SO(2)) is a common gaseous pollutant. It is also, however, endogenously generated from sulfur-containing amino acids. Recent studies have demonstrated that rat blood pressure can be lowered by SO(2)-exposure in vivo and that vasodilation caused by SO(2) at low concentrations (<450 microM) is endothelium-dependent in rat aorta. However,(More)
To explore the physiological role of endogenous gaseous sulfur dioxide (SO(2)) on vascular contractility and its underlying cellular and molecular mechanisms, vasodilation experiment of isolated rat thoracic aortic rings by gaseous SO(2) was carried out and the signal transduction pathways involved in the vascular effects of SO(2) were investigated. In the(More)
The enantioselective degradation and chiral conversion of theta-cypermethrin (TCYM) in rats have been studied via intravenous (i.v.) injection. The degradation kinetics and the enantiomer fraction (EF) were determined by means of normal-phase high-performance liquid chromatography (HPLC) with diode array detection (DAD) and a(More)
In our continued efforts to search for potent and novel receptor tyrosine kinase (RTK) inhibitors as potential anticancer agents, we discovered, through a structure-based design, that 3-aminoindazole could serve as an efficient hinge-binding template for kinase inhibitors. By incorporating an N,N'-diaryl urea moiety at the C4-position of 3-aminodazole, a(More)