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Titolo:
(23S)- and (23R)-25-dehydro-1 alpha-hydroxyvitamin D-3-26,23-lactone function as antagonists of vitamin D receptor-mediated genomic actions of 1 alpha,25-dihydroxyvitamin D-3
Autore:
Ishizuka, S; Miura, D; Ozono, K; Saito, M; Eguchi, H; Chokki, M; Norman, AW;
Indirizzi:
Teijin Inst Biomed Res, Dept Bone & Calcium Metab, Hino, Tokyo 1918512, Japan Teijin Inst Biomed Res Hino Tokyo Japan 1918512 ino, Tokyo 1918512, Japan Teijin Inst Biomed Res, Safety Res Dept, Hino, Tokyo 1918512, Japan TeijinInst Biomed Res Hino Tokyo Japan 1918512 ino, Tokyo 1918512, Japan Osaka Med Ctr, Dept Environm Med, Osaka 5941101, Japan Osaka Med Ctr Osaka Japan 5941101 ept Environm Med, Osaka 5941101, Japan Res Inst Maternal & Child Hlth, Osaka 5941101, Japan Res Inst Maternal & Child Hlth Osaka Japan 5941101 Osaka 5941101, Japan Univ Calif Riverside, Dept Biochem, Riverside, CA 92521 USA Univ Calif Riverside Riverside CA USA 92521 chem, Riverside, CA 92521 USA Univ Calif Riverside, Div Biomed Sci, Riverside, CA 92521 USA Univ Calif Riverside Riverside CA USA 92521 Sci, Riverside, CA 92521 USA
Titolo Testata:
STEROIDS
fascicolo: 3-5, volume: 66, anno: 2001,
pagine: 227 - 237
SICI:
0039-128X(200103/05)66:3-5<227:(A(ADF>2.0.ZU;2-A
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROMYELOCYTIC LEUKEMIA-CELLS; BIOLOGICAL-ACTIVITY ASSESSMENT; 1,25-DIHYDROXYVITAMIN D-3; MONOCYTIC DIFFERENTIATION; NUCLEAR RECEPTOR; PROTEIN-KINASE; NB4 CELLS; D ANALOG; HL-60; PHOSPHORYLATION;
Keywords:
1 alpha,25-(OH)(2)D-3; 1 alpha,25-(OH)(2)D-3-26,23-lactone analogues Antagonist; 25-OH-D-3-24-hydroxylase; cell differentiation; HL-60 cells;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
37
Recensione:
Indirizzi per estratti:
Indirizzo: Ishizuka, S Teijin Inst Biomed Res, Dept Bone & Calcium Metab, 4-3-2 Asahigaoka, Hino,Tokyo 1918512, Japan Teijin Inst Biomed Res 4-3-2 Asahigaoka Hino Tokyo Japan 1918512
Citazione:
S. Ishizuka et al., "(23S)- and (23R)-25-dehydro-1 alpha-hydroxyvitamin D-3-26,23-lactone function as antagonists of vitamin D receptor-mediated genomic actions of 1 alpha,25-dihydroxyvitamin D-3", STEROIDS, 66(3-5), 2001, pp. 227-237

Abstract

We synthesized various analogues of 1 alpha ,25-(OH)(2)D-3-26,23-lactone and examined the effects of them on HL-60 cell differentiation using the evaluation system of the genomic action of 1 alpha ,25-(OH)(2)D-3. We found that (23S)- and (23R)-25-dehydro-1 alpha -OH-D-3-26,23-lactone (TEI-9647 and TEI-9648) strongly bound to the VDR, but did not induce HL-60 cell differentiation. Intriguingly, TEI-9647 and TEI-9648 did inhibit that induced by 1 alpha ,25-(OH)(2)D-3,D- whereas they did not suppress that caused by retinoic acid or TPA. On the contrary, the similar 25-dehydrated 24-dehydro analogues, TEI-D1807 and TEI-D1808, weakly but significantly induced HL-60 cell differentiation, never showing inhibitory effect on HL-60 cell differentiation induced by 1 alpha .25-(OH)(2)D-3. In other experiments, TEI-9637 and TEI-9648 markedly suppressed 25-OH-D-3-24-hydroxylase gene expression induced by 1 alpha ,25-(OH)(2)D-3 in HL-60 cells. TEI-9647 also inhibited the heterodimer formation between VDR and RXR alpha, and the VDR interaction with co-activator SRC-1 according to the results obtained from the mammalian two-hybrid system in Saos-2 cells. Taking all these results into consideration, we reached a manifest conclusion that TEI-9647 and TEI-9648 are the specific and first antagonists of 1 alpha ,25-(OH)(2)D-3 action, specifically VDR-VDRE mediated genomic action. (C) 2001 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 24/09/20 alle ore 20:49:22