Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
20
|
pubmed:dateCreated |
1976-1-2
|
pubmed:abstractText |
The subcellular distribution and properties of rat hypothalamic progesterone 5 alpha-reductase, which accelerates the conversion of progesterone to 5 alpha-pregnane-3,20-dione, have been investigated by utilizing 3H-labeled substrate and a reverse isotopic dilution assay system. The enxymic activity was associated primarily with a cell debris-membranes fraction deribed from the 100 x g pellet. This fraction contained mainly membrane-like particulates and was free of nuclei. Little or no activity was associated with the purified nuclei. The hypothalamic 5 alpha-reductase was stimulated by NADPH but not by NADH. The reaction proceeded optimally over a pH range of 6.0 to 7.2 and at a temperaturhe substrate specificity of the enzyme for other delta 4-3-ketosteroids and the ability of these steroids to inhibit the 5 alpha reduction of [1,2-3H]progesterone as well as the effect of 17 beta-estradiol were also studied. 20 alpha-hydroxypregn-4-en-3-one was more reactive that progesterone, while testosterone was the least reactive. The estimated Km for 20 alpha-hydroxypregn-4-en-3-one was 8.6 +/- 1.9 x 10(-7) M, and for testosterone, 1.6 +/- 1.4 x 10(-5) M. The inhibition studies indicate that 20 alpha-hydroxypregn-4-en-3-one and 17 beta-estradiol are competitive and noncompetitive inhibitors, respectively, of the 5 alpha reduction of progesterone with Ki of 6.0 +/- 3.0 x 10(-8) M for 20 alpha-hydroxypregn-4-en-3-one and Kii (intercept inhibition constant) of 2.6 +/- 0.7 x 10(-5) M and Kis (slope inhibition constant) of 3.6 +/- 0.6 x 10(-5) M for 17 beta-estradiol. Testosterone is a poor competitive inhibitor of the reaction.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/20-alpha-Dihydroprogesterone,
http://linkedlifedata.com/resource/pubmed/chemical/Estradiol,
http://linkedlifedata.com/resource/pubmed/chemical/Hydroxysteroid Dehydrogenases,
http://linkedlifedata.com/resource/pubmed/chemical/Progesterone,
http://linkedlifedata.com/resource/pubmed/chemical/Progesterone Reductase,
http://linkedlifedata.com/resource/pubmed/chemical/Testosterone
|
pubmed:status |
MEDLINE
|
pubmed:month |
Oct
|
pubmed:issn |
0021-9258
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
25
|
pubmed:volume |
250
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
7997-8003
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:240847-20-alpha-Dihydroprogesterone,
pubmed-meshheading:240847-Animals,
pubmed-meshheading:240847-Cell Fractionation,
pubmed-meshheading:240847-Escherichia coli,
pubmed-meshheading:240847-Estradiol,
pubmed-meshheading:240847-Female,
pubmed-meshheading:240847-Hydrogen-Ion Concentration,
pubmed-meshheading:240847-Hydroxysteroid Dehydrogenases,
pubmed-meshheading:240847-Hypothalamo-Hypophyseal System,
pubmed-meshheading:240847-Kinetics,
pubmed-meshheading:240847-Median Eminence,
pubmed-meshheading:240847-Progesterone,
pubmed-meshheading:240847-Progesterone Reductase,
pubmed-meshheading:240847-Rats,
pubmed-meshheading:240847-Subcellular Fractions,
pubmed-meshheading:240847-Temperature,
pubmed-meshheading:240847-Testosterone
|
pubmed:year |
1975
|
pubmed:articleTitle |
Subcellular distribution and properties of progesterone (delta4-steroid) 5alpha-reductase in rat medial basal hypothalamus.
|
pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
|