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Carrier- and receptor-mediated transport of folate antagonists targeting folate-dependent enzymes: correlates of molecular-structure and biological activity.
The transport properties and growth-inhibitory potential of 37 classic and novel antifolate compounds have been tested in vitro against human and murine cell lines expressing different levels of theExpand
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A potent antitumour quinazoline inhibitor of thymidylate synthetase: synthesis, biological properties and therapeutic results in mice.
Abstract We describe the synthesis and some biological properties of N-(4-N-[2-amino-4-hydroxy-6-quinazolinyl)methyl]prop-2-ynylaminobenzoyl)- l -glutamic acid (CB 3717), a potent antifolateExpand
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HPV16 E6 augments Wnt signaling in an E6AP-dependent manner.
In this study we investigated the effect of HPV16 E6 on the Wnt/beta-catenin oncogenic signaling pathway. Luciferase reporter assays indicated that ectopically expressed E6 significantly augmentedExpand
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Folate-based thymidylate synthase inhibitors as anticancer drugs.
The enzyme, thymidylate synthase (TS) is considered an important target for the development of new anticancer agents. Moreover, the folate-binding site in TS is believed to offer better opportunitiesExpand
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bcl-2 modulation of apoptosis induced by anticancer drugs: resistance to thymidylate stress is independent of classical resistance pathways.
The hypothesis was tested that expression of bcl-2 could provide protection against apoptosis induced by cytotoxic drugs via a mechanism which was different from the classical determinants of drugExpand
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ZD1694 (Tomudex): a new thymidylate synthase inhibitor with activity in colorectal cancer.
ZD1694 (Tomudex) is a new antifolate which is a specific inhibitor of thymidylate synthase (TS). Evidence suggests that ZD1694 has a spectrum of activity that only partially overlaps withExpand
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Cellular pharmacology and in vivo activity of a new anticancer agent, ZD9331: a water-soluble, nonpolyglutamatable, quinazoline-based inhibitor of thymidylate synthase.
ZD9331 is a drug that was developed from a potent class of water-soluble, C7-methyl-substituted, quinazoline-based inhibitors of thymidylate synthase (TS) that are transported into cells via aExpand
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Redistribution of nucleoside transporters to the cell membrane provides a novel approach for imaging thymidylate synthase inhibition by positron emission tomography.
Thymidylate synthase (EC 2.1.1.45) is a key enzyme for the de novo synthesis of DNA and as such a target for anticancer drug development. There is a need to develop noninvasive methods for assessingExpand
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ICI D1694, an inhibitor of thymidylate synthase for clinical study.
The TS inhibitor, ICI D1694, is a highly potent inhibitor of tumour growth in vitro and in vivo. Uptake via the RFC and rapid metabolism to polyglutamate forms appear to be responsible for potency.Expand
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HPV16 E6 natural variants exhibit different activities in functional assays relevant to the carcinogenic potential of E6.
Genetic studies have revealed natural amino acid variations within the human papillomavirus (HPV) type 16 E6 oncoprotein. To address the functional significance of E6 polymorphisms, 10 HPV16 E6Expand
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