Detail of "134404-52-7"

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Functional characterization of a novel type of 1a,25-dihydroxyvitamin D3 response element identified in the mouse c-fos promoter

Functional characterization of a novel type of 1a,25-dihydroxyvitamin D3 response element identified in the mouse c-fos promoter. Schraeder, Magdalena; Kahlen, Jean-Pierre; Carlberg, Carsten ( Clinique de Dermatologie, Hopital Cantonal Universitaire, Geneva CH-1211, Switz.). Biochemical and Biophysical Research Communications, 230(3), 646-651 (English) 1997 Academic. CODEN: BBRCA9. ISSN: 0006-291X. DOCUMENT TYPE: Journal CA Section: 3 (Biochemical Genetics) Section cross-reference(s): 2, 13 The seco-steroid 1a,25-dihydroxyvitamin D3 (VD) is known to inhibit cellular proliferation and to induce differentiation as well as programmed cell death (apoptosis).There are some reagents with their cas registry numbers 134404-52-7 and 5300-03-8 are used in this study. VD is the ligand of the transcription factor VDR, which is a member of the nuclear receptor superfamily. Primary VD responding genes contain a VD response element (VDRE), on which VDR binds as a dimeric complex. The main heterodimeric partner of VDR is the retinoid X receptor (RXR) and the majority of the known natural VDREs are formed by a direct repeat of hexameric core binding motifs spaced by 3 nucleotides. Most of the genes carrying DR3-type VDREs are assocd. with the hormone's classical function, which is the regulation of calcium homeostasis. Recently, it has been found that inverted palindromic arrangements spaced by 9 nucleotides also form functional VDREs. This paper reports the identification of a novel IP9-type VDRE in the mouse c-fos promoter. This elements is bound with high affinity by VDR-RXR heterodimers and responds at 10-fold lower concns. to the potent anti-proliferative VD analog EB1089 than to VD. VD may be directly involved in the transcriptional regulation of the cell cycle via the activation of the c-fos gene. .

Effects of the synthetic vitamin D analog EB 1089 and tamoxifen on the growth of experimental rat mammary tumors

Effects of the synthetic vitamin D analog EB 1089 and tamoxifen on the growth of experimental rat mammary tumors. Mackay, A. G.; Ofori-Kuragu, E. A.; Lansdown, A.; Coombes, R. C.; Binderup, L.; Colston, K. W. (Department of Clinical Biochemistry, St George's Hospital Medical School, London SW17 ORE, UK). Endocrine-Related Cancer, 3(4), 327-335 (English) 1996 Journal of Endocrinology. CODEN: ERCAE9. ISSN: 1351-0088. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The anti-tumor effect of EB 1089, a novel vitamin D analog with reduced calcemic activity, was examd. in vivo using the N-methyl-nitrosourea-induced rat mammary tumor model. The vitamin D compd. was given orally at a dose of 1 mg/kg body wt. alone and in combination with tamoxifen (1 mg/kg). Effects were compared with oral tamoxifen treatment alone. EB 1089 significantly inhibited tumor progression compared with controls with a response rate of 58% and a regression rate of 92%. As expected, tamoxifen at the dose given also caused significant inhibition of tumor progression with a response rate of 73%. Combination of these two compds. did not lead to a marked increase in their effectiveness. Histol. examn. of tumors from EB 1089-treated rats showed a marked redn.There are some commonly used reagents with their cas registry numbers 1406-16-2 and 134404-52-7 in this article. in cellularity and mitotic activity. At the dose given, EB 1089 produced a significant rise in serum calcium concn. and urinary calcium excretion. Tamoxifen treatment alone did not significantly alter serum calcium levels. However, combined treatment with tamoxifen and EB 1089 led to a significant redn. in hypercalcemia compared with EB 1089 alone. It is suggested that vitamin D analogs with reduced calcemic activity may provide a new therapeutic strategy for certain malignancies, either alone or in combination with established treatment regimens. .