Kirby, Andrew James, Le Lain, R., Maharlouie, F., Mason, P., Nicholls, P. J., Smith, H. J. and Simons, Claire ![]() |
Abstract
In a search for inhibitors of all-trans retinoic acid (RA)-metabolising enzymes as potential agents for the treatment of skin conditions and cancer we have examined 2-(4-aminophenylmethyl)-6-hydroxy-3,4-dihydronaphthalen-1(2H)-one (5). Compound (5) is a moderate inhibitor of RA-metabolising enzymes in mammalian cadaverous tissue microsomes and homogenates as well as RA-induced enzymes in cultured human genital fibroblasts and HaCat cells. Overall (5) was more potent than or equipotent with ketoconazole, a standard inhibitor, in the cadaverous systems but less active towards the RA-induced cell culture systems. Examination of the data suggests that RA-induction generates metabolising enzymes not present in the cadaverous systems, which are more susceptible to inhibition by ketoconazole than (5).
Item Type: | Article |
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Date Type: | Publication |
Status: | Published |
Schools: | Pharmacy |
Subjects: | R Medicine > RS Pharmacy and materia medica |
ISSN: | 1475-6366 |
Last Modified: | 19 Oct 2022 09:03 |
URI: | https://orca.cardiff.ac.uk/id/eprint/19824 |
Citation Data
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