A small molecule inhibitor of β-catenin/cyclic AMP response element-binding protein transcription
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- Katayoon H. Emami
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
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- Cu Nguyen
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
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- Hong Ma
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
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- Dae Hoon Kim
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
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- Kwang Won Jeong
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
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- Masakatsu Eguchi
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
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- Randall T. Moon
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
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- Jia-Ling Teo
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
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- Se Wong Oh
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
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- Hak Yeop Kim
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
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- Sung Hwan Moon
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
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- Jong Ryul Ha
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
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- Michael Kahn
- Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122; Howard Hughes Medical Institute and Departments of Pharmacology and Pathobiology, University of Washington, Seattle, WA 98195; and Choong Wae Pharma Corporation, Hwasung City 146-141, Kyunggido 445-970, Korea
書誌事項
- 公開日
- 2004-08-16
- DOI
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- 10.1073/pnas.0404875101
- 公開者
- Proceedings of the National Academy of Sciences
この論文をさがす
説明
<jats:p>Inherited and somatic mutations in the adenomatous polyposis coli occur in most colon cancers, leading to activation of β-catenin-responsive genes. To identify small molecule antagonists of this pathway, we challenged transformed colorectal cells with a secondary structure-templated chemical library, looking for compounds that inhibit a β-catenin-responsive reporter. We identified ICG-001, a small molecule that down-regulates β-catenin/T cell factor signaling by specifically binding to cyclic AMP response element-binding protein. ICG-001 selectively induces apoptosis in transformed cells but not in normal colon cells, reduces<jats:italic>in vitro</jats:italic>growth of colon carcinoma cells, and is efficacious in the Min mouse and nude mouse xenograft models of colon cancer.</jats:p>
収録刊行物
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- Proceedings of the National Academy of Sciences
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Proceedings of the National Academy of Sciences 101 (34), 12682-12687, 2004-08-16
Proceedings of the National Academy of Sciences
