Linked Life Data

7655426

Source:http://linkedlifedata.com/resource/pubmed/id/7655426

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1995-10-5
pubmed:abstractText
19-Nor (2) and 5 alpha-reduced (3) derivatives of androst-4-ene-3,6,17-trione (1) as well as 5 alpha-androstan-17-ones 4-6 were tested for their abilities to inhibit aromatase in human placental microsomes. All the steroids except 5 alpha-6-one 4 were fair to good competitive inhibitors of the enzyme, with apparent Ki's ranging from 50 to 820 nM in which 5 alpha-3-one 5 was the most potent among them. The inhibitory activities of the 19-nor and 5 alpha-reduced derivatives (2 and 3) were less potent than that of the parent compound 1. Inhibitor 2 caused a time-dependent, pseudo-first-order inactivation of aromatase activity with a rate constant for inactivation of 0.148 min-1 in the presence of NADPH in air. The substrate androstenedione prevented the inactivation and L-cysteine did not protect aromatase from the inactivation.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0918-6158
pubmed:author
pubmed:issnType
Print
pubmed:volume
18
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
555-8
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1995
pubmed:articleTitle
Biochemical studies of estr-4-ene-3,6,17-trione and 5 alpha-androstan-17-ones with or without a carbonyl function at C-3 and/or C-6 as aromatase inhibitors.
pubmed:affiliation
Tohoku College of Pharmacy, Sendai, Japan.
pubmed:publicationType
Journal Article, In Vitro