Graitec OMD 2015 Repack

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Although camptothecin (CPT) is known to be a potent inhibitor of DNA topoisomerase I, the therapeutic use of this antitumor drug is limited by its toxic effects and an increased side-effect, for example, diarrhea. The effects of CPT on the transport of glutathione S-conjugates (GSH, glutathione disulfide, GS-SG and glutathione thioglycolate) were examined in everted monolayers of Caco-2 cells. The order of potencies of the GSH conjugates were GS-SG > GSH > glutathione pentane-2,3-dithiolyl disulfide (GSSG). CPT potently inhibited the transport of both the GSH and GS-SG conjugates, but did not affect the transport of GSSG. The effects of a nontoxic concentration of CPT (approximately 10 nM) on the accumulation of the GSH conjugates were also examined. The CPT treatment inhibited [35S]GSH and GS-SG conjugate transport by approximately 80%. These data demonstrate that CPT inhibits the transport of GSH and GS-SG conjugates in the intestinal epithelium, and suggest that this may be a factor in the diarrheal side-effect of the drug.Friday, September 14, 2008

Inauguration: Back home from Washington

It was such a whirlwind two weeks with a lot of learning and being great company. To paraphrase Mr. M, “It was good to be away.” I’m sure that none of my readers will doubt that. He noted “We all have to get back to our normal lives”. He really meant it in an all encompassing way, that we get to take a breather from his normal life and get back to our

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