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- W1977095846 abstract "N-[4-[2-Propyn-1-yl[(6S)-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3H-cyclopenta[g]quinazolin-6-yl]amino]benzoyl]-l-γ-glutamyl-d-glutamic acid 1 (BGC 945, now known as ONX 0801), is a small molecule thymidylate synthase (TS) inhibitor discovered at the Institute of Cancer Research in London. It is licensed by Onyx Pharmaceuticals and is in phase 1 clinical studies. It is a novel antifolate drug resembling TS inhibitors plevitrexed and raltitrexed that combines enzymatic inhibition of thymidylate synthase with α-folate receptor-mediated targeting of tumor cells. Thus, it has potential for efficacy with lower toxicity due to selective intracellular accumulation through α-folate receptor (α-FR) transport. The α-FR, a cell-surface receptor glycoprotein, which is overexpressed mainly in ovarian and lung cancer tumors, has an affinity for 1 similar to that for its natural ligand, folic acid. This study describes a novel synthesis of 1, an X-ray crystal structure of its complex with Escherichia coli TS and 2′-deoxyuridine-5′-monophosphate, and a model for a similar complex with human TS." @default.
- W1977095846 created "2016-06-24" @default.
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- W1977095846 date "2013-06-21" @default.
- W1977095846 modified "2023-09-29" @default.
- W1977095846 title "Development and Binding Mode Assessment of <i>N</i>-[4-[2-Propyn-1-yl[(6<i>S</i>)-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3<i>H</i>-cyclopenta[<i>g</i>]quinazolin-6-yl]amino]benzoyl]-<scp>l</scp>-γ-glutamyl-<scp>d</scp>-glutamic Acid (BGC 945), a Novel Thymidylate Synthase Inhibitor That Targets Tumor Cells" @default.
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- W1977095846 doi "https://doi.org/10.1021/jm400490e" @default.
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