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Genomic-scale measurement of mRNA turnover and the mechanisms of action of the anti-cancer drug flavopiridol
BackgroundFlavopiridol, a flavonoid currently in cancer clinical trials, inhibits cyclin-dependent kinases (CDKs) by competitively blocking their ATP-binding pocket. However, the mechanism of actionExpand
Relationships between drug activity in NCI preclinical in vitro and in vivo models and early clinical trials
An analysis of the activity of compounds tested in pre-clinical in vivo and in vitro assays by the National Cancer Institute's Developmental Therapeutics Program was performed. For 39 agents withExpand
In vivo cultivation of tumor cells in hollow fibers.
Advancement of potential anti-cancer agents from "discovery" in an in vitro screen to pre-clinical development requires a demonstration of in vivo efficacy in one or more animal models of neoplasticExpand
Synthesis and biological evaluation of novel curcumin analogs as anti-cancer and anti-angiogenesis agents.
A series of novel curcumin analogs were synthesized and screened for anti-cancer and anti-angiogenesis activities at Emory University and at the National Cancer Institute (NCI). These compounds areExpand
Sodium dichloroacetate selectively targets cells with defects in the mitochondrial ETC
The “Warburg effect,” also termed aerobic glycolysis, describes the increased reliance of cancer cells on glycolysis for ATP production, even in the presence of oxygen. Consequently, there isExpand
Human Tumor Xenograft Models in NCI Drug Development
The methods used by the National Cancer Institute (NCI) for in vivo preclinical development of anticancer drugs were described in detail in the first edition of this book (1). In addition, a seriesExpand
The National Cancer Institute ALMANAC: A Comprehensive Screening Resource for the Detection of Anticancer Drug Pairs with Enhanced Therapeutic Activity.
To date, over 100 small-molecule oncology drugs have been approved by the FDA. Because of the inherent heterogeneity of tumors, these small molecules are often administered in combination to preventExpand
Enhanced Tumor Cell Radiosensitivity and Abrogation of G2 and S Phase Arrest by the Hsp90 Inhibitor 17-(Dimethylaminoethylamino)-17-demethoxygeldanamycin
Purpose: Because of the potential for affecting multiple signaling pathways, inhibition of Hsp90 may provide a strategy for enhancing tumor cell radiosensitivity. Therefore, we have investigated theExpand
Schedule-dependent Inhibition of Hypoxia-inducible Factor-1α Protein Accumulation, Angiogenesis, and Tumor Growth by Topotecan in U251-HRE Glioblastoma Xenografts
We have previously shown that topotecan, a topoisomerase I poison, inhibits hypoxia-inducible factor (HIF)-1α protein accumulation by a DNA damage-independent mechanism. Here, we report that dailyExpand
Aryl hydrocarbon receptor activation of an antitumor aminoflavone: basis of selective toxicity for MCF-7 breast tumor cells.
Aminoflavone (4H-1-benzopyran-4-one, 5-amino-2-(4-amino-3-fluorophenyl)-6,8-difluoro-7-methyl; NSC 686288) demonstrates differential antiproliferative activity in the National Cancer Institute'sExpand