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Sachiko YAMADA, Keiko YAMAMOTO, Hiroyuki MASUNO, Masato SHIMIZU
Article type: Article
1999 Volume 73 Issue 9 Pages
511-525
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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On the basis of conformational analysis of the side chain of 1, 25-(OH)_2D_3 (1) and its 20-epimer (2), we grouped region in space, where the side chain of these vitamin D can move about, into four, A, G, EA and EG. We then designed and synthesized analogs whose side chain mobility is restricted in one of these four regions: four diastereomers at C-20 and -22 of 22-methyl-1, 25-(OH)_2D_3 (3〜6). We evaluated various activities of these analogs (3〜6). The results lead us to delineate space group-activity relationship. We similarly analyzed the conformation of nearly fifty highly active known vitamin D analogs and defined another space region F. The results show that our active space group concept can be applicable to almost all these side chain analogs. Altogether, the following space group-activity relationship was found: VDR affinity, EA>A>F>G>EG; DBP affinity, A only; Cell differentiation, EA>F>A>EG and G; Calcemic, EA>A and G>F>EG.
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Katsumi SHIBATA, Shin-Ichi FUKUOKA, Masumi OKUMURA, Tsutomu FUKUWATARI ...
Article type: Article
1999 Volume 73 Issue 9 Pages
527-532
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
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Quinolinic acid, a key intermediate in the de novo biosynthesis of niacin, is biosynthesized from L-tryptophan in mammals while it is biosynthesized from L-aspartic acid and dihydroxyacetone phosphate in Escherichia coil. Quinolinate synthetase of E. coli consists of two components A and B proteins. The B protein has been identified as L-aspartic acid oxidase that generates iminoaspartic acid. Iminoaspartic acid is then conjugated with dihydroxyacetone phosphate to generate quinolinic acid by the A protein. In the mammalian liver, unlike in E. coli, D-aspartic acid oxidase has been found, by which also iminoaspartic acid is generated. Significant amounts of D-aspartic acid are contained in tortillas (lime-treated corn) which has been served as anti-pellagra foodstuff. Therefore, we postulated and examined a possibility of the biosynthesis of niacin from D-aspartic acid in mammals. Administration of D-aspartic acid to rats and humans did not increase urinary excretion of niacin and its metabolites. In rats, administration of D-aspartic acid did not improve the growth of weaning rats fed a tryptophan-limiting and niacin free diet. Based on those results, the possibility of biosynthesis of niacin from D-aspartic acid in mammals was denied.
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[in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
533-537
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
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[in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
539-544
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
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[in Japanese], [in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
545-549
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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[in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
551-559
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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[in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
561-566
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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[in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
567-568
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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[in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
568-570
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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[in Japanese], [in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
570-571
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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[in Japanese], [in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
571-574
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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[in Japanese], [in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
574-576
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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[in Japanese], [in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
576-577
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
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[in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
579-580
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
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[in Japanese], [in Japanese], [in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
581-
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
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[in Japanese], [in Japanese], R. Pittelkow M.
Article type: Article
1999 Volume 73 Issue 9 Pages
581-
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
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[in Japanese], [in Japanese], [in Japanese], [in Japanese], [in Japane ...
Article type: Article
1999 Volume 73 Issue 9 Pages
582-
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
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[in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
582-583
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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[in Japanese], [in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
583-584
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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[in Japanese], [in Japanese], [in Japanese], [in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
585-
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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[in Japanese], [in Japanese], [in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
586-
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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[in Japanese], [in Japanese], [in Japanese]
Article type: Article
1999 Volume 73 Issue 9 Pages
586-587
Published: September 25, 1999
Released on J-STAGE: December 26, 2017
JOURNAL
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