Potential Repurposing of Known Drugs as Potent Bacterial β-Glucuronidase Inhibitors
نویسندگان
چکیده
منابع مشابه
Old drug new use - Amoxapine and its metabolites as potent bacterial 1 β - glucuronidase inhibitors for alleviating cancer drug toxicity
*To whom correspondence should be addressed: 18 Hong Zhao 19 Department of Systems Medicine and Bioengineering 20 Houston Methodist Research Institute, Weill Cornell Medical College 21 6670 Bertner Ave., R6-216, Houston, TX 77030 22 E-mail: [email protected] 23 Phone: 713-441-3557; Fax: 713-441-7189 24 John E. Scott 25 Biomanufacturing Research Institute and Technology Enterprise 26 No...
متن کاملOld drug new use--amoxapine and its metabolites as potent bacterial β-glucuronidase inhibitors for alleviating cancer drug toxicity.
PURPOSE Irinotecan (CPT-11) induced diarrhea occurs frequently in patients with cancer and limits its usage. Bacteria β-glucuronidase (GUS) enzymes in intestines convert the nontoxic metabolite of CPT-11, SN-38G, to toxic SN-38, and finally lead to damage of intestinal epithelial cells and diarrhea. We previously reported amoxapine as a potent GUS inhibitor in vitro. To further understand the m...
متن کاملPhenoxyacetohydrazide Schiff bases: β-glucuronidase inhibitors.
Phenoxyacetohydrazide Schiff base analogs 1-28 have been synthesized and their in vitro β-glucouoronidase inhibition potential studied. Compounds 1 (IC50=9.20±0.32 µM), 5 (IC50=9.47±0.16 µM), 7 (IC50=14.7±0.19 µM), 8 (IC50=15.4±1.56 µM), 11 (IC50=19.6±0.62 µM), 12 (IC50=30.7±1.49 µM), 15 (IC50=12.0±0.16 µM), 21 (IC50=13.7±0.40 µM) and 22 (IC50=22.0±0.14 µM) showed promising β-glucuronidase inhi...
متن کاملA High Throughput Assay for Discovery of Bacterial β-Glucuronidase Inhibitors
CPT-11 is a widely-used anti-cancer drug that is converted in vivo to its active metabolite, SN-38. In the liver, enzymes detoxify SN-38 by coupling it to a glucuronidate moiety and this inactive compound (SN-38G) is excreted into the gastrointestinal tract. In the intestine, commensal bacteria convert the SN-38G back to the active and toxic SN-38 using bacterial β-glucuronidase enzyme (GUS). T...
متن کاملSynthesis of potent inhibitors of β-ketoacyl-acyl carrier protein synthase III as potential antimicrobial agents.
Mycobacterium tuberculosis FabH, an essential enzyme in the mycolic acid biosynthetic pathway, is an attractive target for novel anti-tubercolosis agents. Structure-based design and synthesis of 1-(4-carboxybutyl)-4-(4-(substituted benzyloxy)phenyl)-1H-pyrrole-2-carboxylic acid derivatives 7a-h, a subset of eight potential FabH inhibitors, is described in this paper. The Vilsmeier-Haack reactio...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Journal of Biomolecular Screening
سال: 2012
ISSN: 1087-0571,1552-454X
DOI: 10.1177/1087057112444927