Isoform-Selective Inhibition of the Human UDP-glucuronosyltransferase 2B7 by Isolongifolol Derivatives
✍ Scribed by Bichlmaier, Ingo; Kurkela, Mika; Joshi, Tanmaya; Siiskonen, Antti; Rüffer, Tobias; Lang, Heinrich; Suchanová, Bohumila; Vahermo, Mikko; Finel, Moshe; Yli-Kauhaluoma, Jari
- Book ID
- 126053888
- Publisher
- American Chemical Society
- Year
- 2007
- Tongue
- English
- Weight
- 162 KB
- Volume
- 50
- Category
- Article
- ISSN
- 0022-2623
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## Abstract The tricyclic sesquiterpenol (+)‐longifolol served as a lead structure for the design of inhibitors of the human UDP‐glucuronosyltransferase (UGT) 2B7. Twenty‐four homochiral and epimeric longifolol derivatives were synthesized and screened for their ability to inhibit the enzyme. The a
## Abstract Stereoselective metabolism of propranolol side‐chain glucuronidation was studied for two recombinant human uridine diphosphate glucuronosyltransferases (UGTs), UGT1A9 and UGT2B7. The __S__‐ and __R__‐propranolol side‐chain glucuronides produced in the incubation mixtures were assayed si