Coggin, Joseph H. (University of Chicago, Chicago, Ill.), Muriel Loosemore, and William R. Martin. Metabolism of 6-mercaptopurine by resistant Escherichia coli cells. J. Bacteriol. 92:446-454. 1966.-6-Mercaptopurine (MP) utilization as a source of purine in MP-sensitive and -resistant cultures of Escherichia coli was investigated. The label of MP-8-C(14) appeared in adenine and guanine of ribon...

AIM We evaluated the effect of coadministration of sulphasalazine, mesalamine, and balsalazide on the pharmacokinetics and pharmacodynamics of azathioprine and 6-mercaptopurine. METHODS Thirty four patients with Crohn's disease receiving azathioprine or 6-mercaptopurine were enrolled in an eight week non-randomised parallel group drug interaction study and treated with mesalamine 4 g/day, sul...

The biological activity of 6mercaptopurine, an analogue of hypoxanthme, has been the subject of extensive studies, but the mechanism of its action has remained unclear. This drug inhibits the growth of bacteria (l-3) and mammalian cells (4, 5) in vitro and the proliferation of experimental tumors and leukemias in tiuo (6-9). It has been suggested that it interferes with the synthesis of nucleic...

BACKGROUND Measurement of 6-thioguanine nucleotide concentrations may be useful for optimising treatment with azathioprine and 6-mercaptopurine. METHODS We conducted a study of 170 patients with inflammatory bowel disease treated with azathioprine or 6-mercaptopurine to determine the relationship between 6-thioguanine nucleotide concentrations and both disease activity, as measured by the inf...

The effects of 6-thioguanine on purine biosynthesis and cell viability have been examined in H.Ep. 2 cells grown in culture. Toxicity is not reversed by aminoimidazolecarboxamide, suggesting that inhibition of purine biosynthesis de novo is not the sole mechanism of toxicity. Also, 6-(methylmercapto)purine ribonucleoside, a potent inhibitor of purine biosynthesis de novo, produces more marked r...

Structural and thermal data were obtained for a novel hemihydrate of 6-mercaptopurine. The hemihydrate shows increased solubility and bioavailability when compared to the monohydrate form, better stability against conversion in aqueous media than the anhydrate form, and a dehydration temperature of 240 °C, the highest of any known hydrate crystal.

Atherosclerosis, the underlying cause of heart attack and stroke, appears to be an inflammatory disease driven by retention of modified lipoproteins in the artery wall.1 Markers of inflammation, such as high sensitivity C-reactive protein, are independent predictors of cardiovascular (CV) events.2 If atherosclerosis truly is an inflammatory disease, then shouldn’t we be able to identify antiinf...

Drug repositioning is the application of the existing drugs to new uses and has the potential to reduce the time and cost required for the typical drug discovery process. In this study, we repositioned thiopurine drugs used for the treatment of acute leukaemia as new tyrosinase inhibitors. Tyrosinase catalyses two successive oxidations in melanin biosynthesis: the conversions of tyrosine to dih...

Methanococcus voltae incorporated exogenous adenine, guanine, hypoxanthine, and uracil, but not thymine. Growth of M. voltae was also sensitive to purine and pyrimidine analogs. Of the 20 analogs tested, 12 were inhibitory at 1 mg/ml. The most effective inhibitors were purine analogs with endocyclic substitutions. Nucleoside analogs and analogs with exocyclic substitutions or additions were les...

Multilocus genotypes have been shown to be of relevance for using pharmacogenomic principles to individualize drug therapy. As it relates to thiopurine therapy, genetic polymorphisms of TPMT are strongly associated with the pharmacokinetics and clinical effects of thiopurines (mercaptopurine and azathioprine), influencing their toxicity and efficacy. We have recently demonstrated that TPMT and ...