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Discovery of a Novel Mode of Protein Kinase Inhibition Characterized by the Mechanism of Inhibition of Human Mesenchymal-epithelial Transition Factor (c-Met) Protein Autophosphorylation by ARQ 197
A number of human malignancies exhibit sustained stimulation, mutation, or gene amplification of the receptor tyrosine kinase human mesenchymal-epithelial transition factor (c-Met). ARQ 197 is aExpand
Identification of the in Vitro Metabolites of 3,4-Dihydro-2,2-dimethyl-2H-naphthol[1,2-b]pyran-5,6-dione (ARQ 501; β-Lapachone) in Whole Blood
3,4-Dihydro-2,2-dimethyl-2H-naphthol[1,2-b]pyran-5,6-dione (ARQ 501; β-lapachone) showed promising anticancer activity in phase I clinical trials as monotherapy and in combination with cytotoxicExpand
Plasma and cerebrospinal fluid pharmacokinetics of cytosine arabinoside in dogs
SummaryCytosine arabinoside (ara-C) is a component of many protocols for the treatment of CNS (central nervous system) leukemia and lymphoma in humans and dogs. It is also used for the prophylaxis ofExpand
Synthetic methods for the preparation of ARQ 501 (beta-Lapachone) human blood metabolites.
ARQ 501 (3,4-dihydro-2,2-dimethyl-2H-naphthol[1,2-b] pyran-5,6-dione), a synthetic version of beta-Lapachone, is a promising anti-cancer agent currently in multiple Phase II clinical trials.Expand
A Novel Mode of Protein Kinase Inhibition Exploiting Hydrophobic Motifs of Autoinhibited Kinases
Protein kinase inhibitors with enhanced selectivity can be designed by optimizing binding interactions with less conserved inactive conformations because such inhibitors will be less likely toExpand
D-501036, a novel selenophene-based triheterocycle derivative, exhibits potent in vitro and in vivo antitumoral activity which involves DNA damage and ataxia telangiectasia–mutated nuclear protein
D-501036 [2,5-bis(5-hydroxymethyl-2-selenienyl)-3-hydroxymethyl-N-methylpyrrole] is herein identified as a novel antineoplastic agent with a broad spectrum of antitumoral activity against severalExpand
Augmentation of 1-beta-D-arabinofuranosylcytosine cytotoxicity in human tumor cells by inhibiting drug efflux.
  • T. Chan
  • Biology, Medicine
  • Cancer research
  • 15 May 1989
Dipyridamole is a potent inhibitor of membrane nucleoside transport into mammalian cells. Since the membrane transporter mediates both the influx and the efflux of nucleosides, dipyridamole should beExpand
Synergism between dipyridamole and cisplatin in human ovarian carcinoma cells in vitro.
Dipyridamole (DPM), a nucleoside membrane transport inhibitor, enhanced the cytotoxicity of cisplatin (DDP) for human ovarian carcinoma 2008 cells by a factor of 4.7 +/- 0.4-fold (mean +/- SD) andExpand
Oncogene signal transduction inhibitors from Chinese medicinal plants
Oncogene modulated signal transduction based on intracellular phosphorylation of protein tyrosine or serine/threonine has been utilized as a target for oncogene-based anti-cancer drug discovery.Expand
Bicinchoninic acid protein assay in the determination of adriamycin cytotoxicity modulated by the MDR glycoprotein.
The development of simultaneous resistance to structurally unrelated drugs in cancer cells is a major obstacle to effective cancer chemotherapy. This multidrug-resistance (MDR) phenomenon is largelyExpand