Reductive metabolism of the dinitrobenzamide mustard anticancer prodrug PR-104 in mice

No abstract is available for this paper.

• Publication year

  2011

• Venue

  Cancer Chemotherapy and Pharmacology

• Publication date

  2011-03-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1007/s00280-010-1354-5PMID 20473609
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• The bioreductive prodrug PR-104A is activated under aerobic conditions by human aldo-keto reductase 1C3.

  2010influential reference
• A phase I trial of PR-104, a nitrogen mustard prodrug activated by both hypoxia and aldo-keto reductase 1C3, in patients with solid tumors

  2010cited by this paper
• Metabolism and Excretion of the Novel Bioreductive Prodrug PR-104 in Mice, Rats, Dogs, and Humans

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• Rapid and sensitive ultra-high-pressure liquid chromatography-tandem mass spectrometry analysis of the novel anticancer agent PR-104 and its major metabolites in human plasma: Application to a pharmacokinetic study.

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• The aldo-keto reductase AKR1C3 contributes to 7,12-dimethylbenz(a)anthracene-3,4-dihydrodiol mediated oxidative DNA damage in myeloid cells: implications for leukemogenesis.

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• Roles of DNA repair and reductase activity in the cytotoxicity of the hypoxia-activated dinitrobenzamide mustard PR-104A

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• DNA cross-links in human tumor cells exposed to the prodrug PR-104A: relationships to hypoxia, bioreductive metabolism, and cytotoxicity.

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• Design of anticancer prodrugs for reductive activation

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• An indomethacin analogue, N-(4-chlorobenzoyl)-melatonin, is a selective inhibitor of aldo-keto reductase 1C3 (type 2 3alpha-HSD, type 5 17beta-HSD, and prostaglandin F synthase), a potential target for the treatment of hormone dependent and hormone independent malignancies.

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• Activation of non-ischemic, hypoxia-inducible signalling pathways up-regulate cytoprotective genes in the murine liver.

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• Mechanism of Action and Preclinical Antitumor Activity of the Novel Hypoxia-Activated DNA Cross-Linking Agent PR-104

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• Synthesis of 3H‐ and 2H4‐labelled versions of the hypoxia‐activated pre‐prodrug 2‐[(2‐bromoethyl)‐2,4‐dinitro‐6‐ [[[2‐(phosphonooxy)ethyl]amino]carbonyl]anilino]ethyl methanesulfonate (PR‐104)

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• Analysis of the hypoxia-activated dinitrobenzamide mustard phosphate pre-prodrug PR-104 and its alcohol metabolite PR-104A in plasma and tissues by liquid chromatography-mass spectrometry.

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• Identification of human reductases that activate the dinitrobenzamide mustard prodrug PR-104A: a role for NADPH:cytochrome P450 oxidoreductase under hypoxia.

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• AKR1C1 and AKR1C3 may determine progesterone and estrogen ratios in endometrial cancer.

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  2017influential citation
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  2016cites this paper
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