Local view for "https://dbmi-icode-01.dbmi.pitt.edu/dikb/resource/Evidence/1448"
| Predicate | Value (sorted: default) |
|---|---|
| rdfs:label | |
| rdf:type | |
| ?:Evidence_enzyme_system | |
| ?:Evidence_type | |
| ?:content |
"Enzyme system: human liver microsomes
NADPH added: yes
inhibitor used: n/a
reaction: beta-OH-lovastatin-->6'beta-Hydroxylovastatin
Quote:
Lovastatin was metabolized by human liver microsomes to two major metabolites: 6'beta-hydroxy [Michaelis-Menten constant (Km): 7.8 +/- 2.7 microM] and 6'-exomethylene lovastatin (Km,10.3 +/- 2.6 microM). 6'beta-Hydroxylovastatin formation in the liver was inhibited by the specific CYP3A inhibitors cyclosporine (Ki, 7.6 +/- 2.3 microM), ketoconazole (Ki, 0.25 +/- 0.2 microM), and troleandomycin (Ki, 26.6 +/- 18.5 microM).
NOTE: though not clearly stated in the paper, the authors mention that lovastatin itself it fully converted by esterases to its open ring acid form which we in the DIKB infer to be beta-OH-lovastatin"
|
| dc:creator | |
| dc:date |
"09/28/2007 13:25:31"
|
| rdfs:seeAlso |
All properties reside in the graph file:///home/swish/src/ClioPatria/guidelines/dikb.ttl
The resource appears as object in one triple:
{ beta-hydroxy-lovastatin_has_metabolite_6'beta-hydroxy-lovastatin, <http://purl.org/swan/1.2/swan-commons#citesAsSupportingEvidence>, evidence_1823 }