In vitro inhibitor studies of vitamin D 25-hydroxylase in rat liver microsomes. 1983

B Kabakoff, and H K Schnoes, and H F DeLuca

The ability of four vitamin D analogs to inhibit the liver microsomal vitamin D-25-hydroxylase was determined. 19-Hydroxy-10(S),19-dihydrovitamin D3,25-fluorovitamin D3, 3 beta-hydroxy-9,10-seco-5,7,10(19)-choletrien-24-oic acid dimethylamide and 25-aza-vitamin D3 were competitive inhibitors with apparent KI values of 44, 137, and 870 nM, and 6.4 microM, respectively. The values for the 19-hydroxy-10(S), 19-dihydrovitamin D3, 25-fluorovitamin D3, and 25-aza-vitamin D3 correspond well to other literature reports with respect to their relative in vivo inhibitory properties. 24-Oxovitamin D3 oxime also proved to be a potent inhibitor but a detailed analysis was prohibited by the lack of material. The 3 beta-hydroxy-9,10-seco-5,7,10(19)-choletrien-24-oic acid dimethylamide was also tested in vivo but had no antagonistic activity when provided at a 2000-fold excess over vitamin D3.

UI MeSH Term Description Entries
D008297 Male Males
D008862 Microsomes, Liver Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough. Liver Microsomes,Liver Microsome,Microsome, Liver
D008954 Models, Biological Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment. Biological Model,Biological Models,Model, Biological,Models, Biologic,Biologic Model,Biologic Models,Model, Biologic
D002621 Chemistry A basic science concerned with the composition, structure, and properties of matter; and the reactions that occur between substances and the associated energy exchange.
D002762 Cholecalciferol Derivative of 7-dehydroxycholesterol formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. It differs from ERGOCALCIFEROL in having a single bond between C22 and C23 and lacking a methyl group at C24. Vitamin D 3,(3 beta,5Z,7E)-9,10-Secocholesta-5,7,10(19)-trien-3-ol,Calciol,Cholecalciferols,Vitamin D3
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013250 Steroid Hydroxylases Cytochrome P-450 monooxygenases (MIXED FUNCTION OXYGENASES) that are important in steroid biosynthesis and metabolism. Steroid Hydroxylase,Steroid Monooxygenases,Hydroxylase, Steroid,Hydroxylases, Steroid,Monooxygenases, Steroid
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus
D053493 Cholestanetriol 26-Monooxygenase An NAPH-dependent cytochrome P450 enzyme that catalyzes the oxidation of the side chain of sterol intermediates such as the 27-hydroxylation of 5-beta-cholestane-3-alpha,7-alpha,12-alpha-triol. 5-beta-Cholestane-3-alpha,7-alpha,12-alpha-triol 27-Hydroxylase,C27-Steroid 26-Hydroxylase,Cytochrome P-450 Steroid 27-Hydroxylase,Cytochrome P-450 Sterol 26-Hydroxylase,Steroid 25-Hydroxylase,Steroid 27-Hydroxylase,Sterol 26-Hydroxylase,Sterol 27-Hydroxylase,Vitamin D3 25-Hydroxylase,C27 Steroid 26 Hydroxylase,Cholestanetriol 26 Monooxygenase,Cytochrome P 450 Steroid 27 Hydroxylase,Cytochrome P 450 Sterol 26 Hydroxylase,Steroid 25 Hydroxylase,Steroid 27 Hydroxylase,Sterol 26 Hydroxylase,Sterol 27 Hydroxylase,Vitamin D3 25 Hydroxylase
D055598 Chemical Phenomena The composition, structure, conformation, and properties of atoms and molecules, and their reaction and interaction processes. Chemical Concepts,Chemical Processes,Physical Chemistry Concepts,Physical Chemistry Processes,Physicochemical Concepts,Physicochemical Phenomena,Physicochemical Processes,Chemical Phenomenon,Chemical Process,Physical Chemistry Phenomena,Physical Chemistry Process,Physicochemical Phenomenon,Physicochemical Process,Chemical Concept,Chemistry Process, Physical,Chemistry Processes, Physical,Concept, Chemical,Concept, Physical Chemistry,Concept, Physicochemical,Concepts, Chemical,Concepts, Physical Chemistry,Concepts, Physicochemical,Phenomena, Chemical,Phenomena, Physical Chemistry,Phenomena, Physicochemical,Phenomenon, Chemical,Phenomenon, Physicochemical,Physical Chemistry Concept,Physicochemical Concept,Process, Chemical,Process, Physical Chemistry,Process, Physicochemical,Processes, Chemical,Processes, Physical Chemistry,Processes, Physicochemical

Related Publications

B Kabakoff, and H K Schnoes, and H F DeLuca
October 1986, Archives of biochemistry and biophysics,
B Kabakoff, and H K Schnoes, and H F DeLuca
November 1988, Archives of biochemistry and biophysics,
B Kabakoff, and H K Schnoes, and H F DeLuca
May 1988, Journal of biochemistry,
B Kabakoff, and H K Schnoes, and H F DeLuca
October 1988, The Journal of biological chemistry,
B Kabakoff, and H K Schnoes, and H F DeLuca
September 1984, Biochemical and biophysical research communications,
B Kabakoff, and H K Schnoes, and H F DeLuca
January 2004, Molecular genetics and metabolism,
B Kabakoff, and H K Schnoes, and H F DeLuca
November 1992, The Biochemical journal,
B Kabakoff, and H K Schnoes, and H F DeLuca
March 1991, FEBS letters,
B Kabakoff, and H K Schnoes, and H F DeLuca
August 2001, American journal of physiology. Endocrinology and metabolism,
B Kabakoff, and H K Schnoes, and H F DeLuca
August 2012, Poultry science,
Copied contents to your clipboard!