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The Wnt/β-catenin signaling pathway is important for tumor initiation and progression. The low density lipoprotein receptor-related protein-6 (LRP6) is an essential Wnt co-receptor for Wnt/β-catenin signaling and represents a promising anticancer target. Recently, the antihelminthic drug, niclosamide was found to inhibit Wnt/β-catenin signaling, although(More)
PURPOSE To develop a rapidly dissolving porous particle formulation of paclitaxel without Cremophor EL that is appropriate for quick intravenous administration. METHODS A rapidly dissolving porous particle formulation of paclitaxel (AI-850) was created using spray drying. AI-850 was compared to Taxol following intravenous administration in a rat(More)
(S)-10-(2,6-Dimethyl-4-pyridinyl)-9-fluoro-3-methyl-7-oxo-2,3-dihydro-7H - pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acid (WIN 58161) is an enantiomerically pure quinolone with outstanding bacterial topoisomerase II (DNA gyrase, EC 5.99.1.3) inhibitory and antibacterial activity. Unlike most quinolones, WIN 58161 also exhibits significant inhibitory(More)
Temozolomide, a methylating agent with clinical activity against brain tumors, demonstrated excellent antitumor activity following p.o. administration to athymic mice bearing human brain tumor xenografts. In the early stage s.c. implanted SNB-75 astrocytoma model, a 400-mg/kg dose administered on Day 5 produced 10 of 10 Day 54 tumor-free mice. In later(More)
Purine nucleoside analogs are an important class of drugs that are used in the treatment of cancer. Five purine analogs have been approved by the FDA (mercaptopurine, thioguanine, fludarabine monophosphate, deoxycoformycin and cladribine) and four compounds are currently being evaluated clinically (clofarabine, immucillin-H, nelarabine and(More)
PURPOSE Sorafenib tosylate (sorafenib, BAY 43-9006, Nexavar) is a multi-kinase inhibitor that targets tumor cell proliferation and angiogenesis. These studies evaluated the efficacy and tolerability of combinations of sorafenib plus agents used to treat non-small cell lung cancer (NSCLC) using preclinical models of that disease. METHODS Intravenous (iv)(More)
Cl-F-ara-A, an analog of fludarabine, was evaluated against a spectrum of tumor systems in culture and in mice. The compound exhibited significant cytotoxicity against a variety of human tumor cell lines. More importantly, the compound showed selectivity in vivo, with excellent activity being demonstrated against human colon and renal tumors. Human nonsmall(More)
The uptake of cis-[14C]dichloro(ethylenediamine)platinum(II) (cis-DEP) is reduced in cis-diamminedichloroplatinum(II) (cis-DDP)-resistant L1210 cells [L1210/DDP (SRI)] in comparison to cis-DDP-sensitive L1210 cells (L1210/0). A difference in uptake is observed as early as 6 min after addition of cis-[14C]DEP and increases to approximately 3-fold after 30(More)