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发表于 2009-5-10 17:39:16
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来自: 中国江苏南京
About Deforolimus
Deforolimus Is a Non-prodrug Inhibitor of the Protein mTOR
Deforolimus is an investigational drug and has not been approved by the US Food and Drug Administration (FDA) or regulatory agencies in any other country.
Deforolimus is a non-prodrug analog of rapamycin and a small molecule inhibitor of the protein mTOR. The mTOR protein is hypothesized as a "master switch" of cellular catabolism and anabolism, determining whether certain tumor cells grow and proliferate.1
Deforolimus targets the protein kinase mTOR, which regulates the production of proteins critical for cell growth and division via activation of S6 ribosomal protein kinase 1 and inhibition of the eIF4E inhibitor 4E-BP1. mTOR also inhibits the turnover of Cyclin D1 and stimulates the elimination of the cyclin-dependent kinase (CDK) inhibitor p27kip1. Blocking mTOR appears to create a starvation-like effect in cancer cells by interfering with cell growth, division, metabolism, and angiogenesis.2
ARIAD Pharmaceuticals, Inc. and Merck & Co., Inc. have a global collaboration to jointly investigate deforolimus for the treatment of cancer. |
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