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  • 1
    Electronic Resource
    Electronic Resource
    Inhibition of collagenase by aranciamycin and aranciamycin derivatives. (1992)
    s.l. : American Chemical Society
    Journal of medicinal chemistry 35 (1992), S. 2768-2771 
    Details
    ISSN: 1520-4804
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/jm00093a008
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Captopril (SQ 14,225): In vitro and in vivo influence on the proliferative response of rat lymphocytes (1982)
    Springer
    Cellular and molecular life sciences 38 (1982), S. 399-401 
    Details
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary Captopril in vitro (50–500 μg/ml) increased3H-TdR incorporation in unstimulated and mitogen-stimulated cultures of rat lymphocytes. Unseparated spleen and lymph node cells of rats orally treated with captopril (50 mg/kg/day×4) showed decreased basal and mitogen stimulated3H-TdR incorporation. The removal of macrophages abrogated this inhibitory effect. Leucine aminopeptidase activity of macrophages was reduced — in vivo and in vitro — by captopril.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01949416
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Effects of the H2-receptor agonist dimaprit on lymphocyte responsivenessin vitro (1984)
    Springer
    Inflammation research 15 (1984), S. 119-124 
    Details
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The histamine H2-agonist dimaprit was found to increase the response of rat spleen cells to the T-cell mitogen Concanavalin A, when present at concentrations of 10−5 and 10−4 M. Higher concentrations of dimaprit were cytotoxic. The enhanced response seemed to be associated with an inhibitory effect of dimaprit on T-suppressor cell activity rather than with a direct mitogen-like stimulation of lymphocyte proliferation or with an interference with monocyte/macrophage functions. The stimulatory effects of dimaprit were not reversed by the H2-receptor antagonist, cimetidine, nor by the β-receptor antagonists metoprolol and H 35/25. Addition of the H1-receptor antagonist, mepyramine, further increased the stimulatory effect of dimaprit on lymphocyte responsiveness.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01972336
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    Paper (German National Licenses)
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  • 4
    Electronic Resource
    Electronic Resource
    1α,25-Dihydroxyvitamin D3 inhibits the invasive potential of human breast cancer cellsin vitro (1994)
    Springer
    Clinical & experimental metastasis 12 (1994), S. 195-202 
    Details
    ISSN: 1573-7276
    Keywords: breast cancer ; cell proliferation ; invasion ; migration ; 1α ; 25-dihydroxyvitamin D3
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Using the Boyden chamber invasion assay, the effect of 1α,25-dihydroxyvitamin D3 [1α,25(OH)2D3] on the invasiveness of the highly invasive, oestrogen receptor-negative human breast cancer cell line MDA-MB-231 was examined. The MDA-MB-231 cells were shown to contain high-affinity receptors for 1α,25(OH)2D3 with a Kd of 1.5 × 10−11 M. When the cells were treated with 1α,25(OH)2D3 for 4 days before the assay was performed, a dose-dependent inhibition of their invasive potential was demonstrated. Fifty per cent inhibition of invasion was obtained with a concentration of 13 pM of 1α,25(OH)2D3. However, when the cells were treated for only 6 h during the assay, no inhibitory effect was seen. The process of migration was also affected by treatment with 1α,25(OH)2D3 for 4 days, although the inhibition was not of the same magnitude as seen for the invasion. Fifty per cent inhibition of migration occurred at a concentration of 3.2 nM of 1α,25(OH)2D3 (250 times higher than in the invasion assay). Inhibition of invasion and migration was not due to the known anti-proliferative effect of 1α,25(OH)2D3, as no growth reduction could be demonstrated with treatment up to 5 days. Based on the present investigation it can therefore be concluded that 1α,25(OH)2D3 is able to inhibit tumour cell invasiveness by a mechanism which is not exclusively based on its anti-proliferative and anti-migrative effects.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01753887
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  • 5
    Electronic Resource
    Electronic Resource
    Combined effect of vitamin D3 analogs and paclitaxel on the growth of MCF-7 breast cancer cells in vivo (1999)
    Springer
    Breast cancer research and treatment 53 (1999), S. 113-120 
    Details
    ISSN: 1573-7217
    Keywords: breast cancer ; BNX nude mouse ; paclitaxel ; Vitamin D3 analogs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Vitamin D3 analogs and paclitaxel (Taxol) are able to inhibit the in vitro growth of a variety of malignant cells including breast cancer cells. These two compounds decrease growth by different mechanisms and they have non-overlapping toxicities. We examined the abilities of three vitamin D3 compounds to inhibit growth of a human mammary cancer (MCF-7) in BNX triple immunodeficient mice either alone or with Taxol. Vitamin D3 analogs were 1,25(OH)2D3 (code name, Compound C), 1,25(OH)2-16-ene-23-yne-19-n or-26,27-F6-D3 (Compound LH), and 24a,26a,27a,-trihomo-22,24-diene-1,25(OH)2D3 (EB1089). At the doses chosen, the antitumor effect of vitamin D3 analogs alone was greater than that of Taxol alone, and an additive effect was observed when a vitamin D3 analog and Taxol were administered together. EB1089 was the most potent compound, and the EB1089 plus Taxol was the most active combination, decreasing the tumor mass nearly 4-fold compared to controls. Weight-gain in each of the experimental cohorts at the end of the study was less than the control group, but the gain was significantly less in only two experimental groups (those receiving either EB1089 or Compound C plus Taxol). None of the animals became hypercalcemic, and their complete blood counts, serum electrolyte analyses, and liver and renal functions were all fairly similar and within the normal range. In summary, this combination of a vitamin D3 analog and Taxol has the potential to be a therapy for breast cancer.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1006123819675
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  • 6
    Electronic Resource
    Electronic Resource
    High-affinity nuclear receptor binding of 20-epi analogues of 1,25-dihydroxyvitamin D3 correlates well with gene activation (1996)
    New York, N.Y. : Wiley-Blackwell
    Journal of Cellular Biochemistry 62 (1996), S. 325-333 
    Details
    ISSN: 0730-2312
    Keywords: regulation of transcription ; vitamin D3 analogues ; vitamin D3 receptor ; receptor binding ; limited protease digestion assay ; structure-activity relationships ; Life and Medical Sciences ; Cell & Developmental Biology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Biology , Chemistry and Pharmacology , Medicine
    Notes: The hormone 1,25-dihydroxyvitamin D3 (VD) has the potential for clinical use in several diseases, such as cancer, osteoporosis, and psoriasis. The action of VD is mediated by primary responding genes that contain in their promoter region a binding site for the transcription factor VDR. Most of the known VD response elements are formed by a direct repeat of two hexameric core binding motifs spaced by three nucleotides (DR3) bound by a heterodimer of VDR and the retinoid X receptor (RXR). Various VD analogues have been developed in order to optimize the therapeutic profile of VD. This report presents a novel experimental system that may help in the understanding of the structural basis for the high potency of a VD analogue like KH1060, which is a 20-epi-22-oxa-derivative of VD. In human breast cancer cells, MCF-7, the half-maximal gene activation values for KH1060 and seven of its structural precursors were determined on a DR3-type VD response element. These eight analogues cover conservative structural changes from 20-epi-VD (MC1288) to KH1060. With a modified version of the limited protease digestion assay the functional affinity of the analogues to VDR was measured. The functional receptor affinity of the eight analogues was found to be directly proportional to their potency in VDR-RXR-mediated gene activity. © 1996 Wiley-Liss, Inc.
    Additional Material: 4 Ill.
    Type of Medium: Electronic Resource
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