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Uridine diphosphoglucuronosyltransferase pharmacogenetics and cancer
This review examines in detail each UGT isozyme known to be associated with cancer and carcinogenesis, and the functionally relevant genetic polymorphisms of UGTs are reviewed.
Glucuronidation of Dihydrotestosterone and trans-Androsterone by Recombinant UDP-Glucuronosyltransferase (UGT) 1A4: Evidence for Multiple UGT1A4 Aglycone Binding Sites
The results suggest that multiple aglycone binding sites exist within UGT1A4, which may result in atypical kinetics (both homotropic and heterotropic) in a substrate-dependent fashion.
Concise review of the cytochrome P450s and their roles in toxicology.
- C. J. Omiecinski, R. Remmel, V. Hosagrahara
- Biology, MedicineToxicological sciences : an official journal of…
- 1 April 1999
The purpose of this current review is to highlight some of the more important mammalian P450s with respect to their expression, inducibility and inhibition character, and substrate preferences, especially as they relate to human toxicology.
Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.
- A. Kalgutkar, B. Crews, +4 authors L. Marnett
- Chemistry, MedicineProceedings of the National Academy of Sciences…
- 18 January 2000
Indomethacin amides are orally active, nonulcerogenic, anti-inflammatory agents in an in vivo model of acute inflammation and can be envisioned for the modification of all carboxylic acid-containing NSAIDs into selective COX-2 inhibitors.
Expression of the Human UGT1 Locus in Transgenic Mice by 4-Chloro-6-(2,3-xylidino)-2-pyrimidinylthioacetic Acid (WY-14643) and Implications on Drug Metabolism through Peroxisome…
- K. Senekeo-Effenberger, Shujuan Chen, +9 authors R. Tukey
- Biology, MedicineDrug Metabolism and Disposition
- 1 March 2007
Oral fibrate treatment in humans will induce the UGT1A family of proteins in the gastrointestinal tract and liver, influencing bile acid glucuronidation and first-pass metabolism of other drugs that are taken concurrently with hypolipidemic therapy.
Reactivity of mefenamic acid 1-o-acyl glucuronide with proteins in vitro and ex vivo.
- K. McGurk, R. Remmel, V. Hosagrahara, D. Tosh, B. Burchell
- Chemistry, MedicineDrug metabolism and disposition: the biological…
- 1 August 1996
Mefenamic acid glucuronide, although extremely stable in buffer at physiological pH, was found to bind irreversibly to human serum albumin in vitro and Irreversible binding to cellular proteins in culture was also evident with the addition of mefenamic acid to the heterologous Chinese hamster lung fibroblast cell line V79 expressing the human UDP-glucuronosyltransferase isoenzyme UGT1*02.
Relationship of mycophenolic acid exposure to clinical outcome after hematopoietic cell transplantation
- P. Jacobson, J. Rogosheske, +8 authors P. Mcglave
- MedicineClinical pharmacology and therapeutics
- 1 November 2005
Therapeutic monitoring of MPA concentrations with dose adjustment into the therapeutic target appears to be necessary for the most effective use of mycophenolate mofetil.
Primary hepatocytes outperform Hep G2 cells as the source of biotransformation functions in a bioartificial liver.
Primary rat hepatocytes were superior to the Hep G2 cell line as the source of hepatic function in a bioart artificial liver and avoided the potential risk of tumor transmigration from the bioartificial liver into the patient's circulation.
Effect of Aging on Glucuronidation of Valproic Acid in Human Liver Microsomes and the Role of UDP-Glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10
This investigation revealed no differences in VPAG formation in younger versus elderly HMLs and revealed three other UGTs that form VPAGs in vitro, the first reported activity of these UGTS toward VPA glucuronidation.
Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors.
- A. Kalgutkar, A. Marnett, B. Crews, R. Remmel, L. Marnett
- Chemistry, MedicineJournal of medicinal chemistry
- 8 July 2000
Conversion of indomethacin into ester and amide derivatives provides a facile strategy for generating highly selective COX-2 inhibitors and eliminating the gastrointestinal side effects of the parent compound.