Abstract
Paclitaxel (Taxol) conjugated to muramyl dipeptide (MDP) is described. Biological testing showed that the conjugation of MDP at 2'-O-paclitaxel (2'- O -MTC-01) not only has antitumor activity, but also have immunoenhancement capacity. Compared with paclitaxel or MDP alone or with a mixture of paclitaxel + MDP, 2'- O -MTC-01 significantly increases the production and expression of TNF-alpha and IL-12 from mouse peritoneal macrophages, which demonstrates a synergism of MDP and paclitaxel in one conjugated molecule.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylmuramyl-Alanyl-Isoglutamine / chemical synthesis
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Acetylmuramyl-Alanyl-Isoglutamine / chemistry
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Acetylmuramyl-Alanyl-Isoglutamine / therapeutic use*
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Animals
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Drug Therapy, Combination
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Gene Expression Regulation / drug effects
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Humans
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Immunotherapy*
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Interleukin-12 / genetics
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Interleukin-12 / metabolism
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Macrophages, Peritoneal / drug effects
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Macrophages, Peritoneal / metabolism
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Mice
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Neoplasms / drug therapy*
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Paclitaxel / chemical synthesis
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Paclitaxel / chemistry
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Paclitaxel / therapeutic use*
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Tumor Necrosis Factor-alpha / genetics
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Tumor Necrosis Factor-alpha / metabolism
Substances
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Tumor Necrosis Factor-alpha
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Interleukin-12
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Acetylmuramyl-Alanyl-Isoglutamine
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Paclitaxel