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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
MeSH Review

Inhibitory Concentration 50

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Disease relevance of Inhibitory Concentration 50


Psychiatry related information on Inhibitory Concentration 50

  • Individual differences in prednisolone IC50 values were spread from 1 to 3500 ng/ml [6].
  • No changes were detected in the IC50 values for inhibition by zinc in the Alzheimer's samples compared to control although 'glycine-dependent' binding of the [3H]-ligand was significantly reduced in Alzheimer's disease [7].
  • Dixon plots of PEP inhibition showed oleic, linoleic, and arachidonic acids, EPA, and DHA are noncompetitive inhibitors; despite higher IC50 values of these unsaturated fatty acids than strong natural inhibitors, they may have potential use in preventing memory loss [8].

High impact information on Inhibitory Concentration 50


Chemical compound and disease context of Inhibitory Concentration 50

  • We describe here for the first time that the synthetic retinoid CD437 has a strong dose-dependent antiproliferative effect on human melanoma cells (IC50: 5 x 10(-6) M) via the induction of programmed cell death, as judged by analysis of cell morphology, electron microscopical features, and DNA fragmentation [14].
  • Inhibition studies indicated that the HIV proteinase was inhibited by pepstatin A with an IC50 of 0.7 microM [15].
  • The IC50 of the alpha-APA derivative R 89439 for HIV-1 cytopathicity in MT-4 cells was 13 nM [16].
  • One clinical HIV strain with high-level ZDV resistance displayed a 5-fold increase in 2',3'-dideoxyinosine IC50 compared to that of HTLV-IIIB [17].
  • We conducted a retrospective genotypic and phenotypic resistance study (expressed as stavudine phenotypic index, calculated by dividing the inhibitory concentrations 50% [IC50] by the mean value of the sensitive viruses) to evaluate the factors associated with decrease in plasma HIV-1 RNA [18].

Biological context of Inhibitory Concentration 50


Anatomical context of Inhibitory Concentration 50


Associations of Inhibitory Concentration 50 with chemical compounds

  • I report here that picomolar concentrations of melatonin (IC50 9pM) selectively inhibited the calcium-dependent release of 3H-dopamine from rabbit retina, but not from striatum [29].
  • Replacement of the two aliphatic residues with a benzodiazepine-based mimic of a peptide turn generated potent inhibitors of farnesyltransferase [50 percent inhibitory concentration (IC50) < 1 nM] [30].
  • The IC50 of IL-10 for the suppression of TNF-alpha release induced by 0.5 microgram/ml lipopolysaccharide was 0.04 +/- 0.03 U/ml, with as little as 1 U/ml suppressing TNF-alpha production by a factor of 21.4 +/- 2 [31].
  • The Rantes receptor appears to be G protein linked, as binding activity is abolished by guanosine 5'-O-(3-thiotriphosphate) (IC50, 7.3 nM) [32].
  • The 50% inhibitory concentration is approximately 10(-7) M, and this is reduced to approximately 10(-8) M when endogenous PGE production is blocked [33].

Gene context of Inhibitory Concentration 50

  • The IC50 values for IL-1ra binding (ranging from 2 to 4 ng/ml) were similar to those of IL-1 alpha [34].
  • These analogues were antagonists of MCP-1 activity with the most potent being the 9-76 analogue (IC50 = 20 nM) The 9-76 specifically bound to MCP-1 receptors with a Kd of 8.3 nM, which was three-fold higher than MCP-1 (Kd 2.8 nM) [35].
  • By use of a colony-forming assay, the 1-hour IC50 (i.e., the concentration of drug required for 1 hour to achieve 50% cell kill) for cisplatin was 2 microM or less for parental and vector-transfected clones (n = 4), whereas it was 25 microM or more for all MDA-468/AS-EGFR clones (n = 3) [36].
  • An MDA-468 subline selected after long-term treatment with a TGF-alpha-Pseudomonas exotoxin A fusion protein 40 lacked EGF binding and also exhibited cisplatin resistance (1-hour IC50: > 30 microM) compared with parental cells [36].
  • Sera from patients on long-term dialysis with low AHSG concentrations showed impaired ex-vivo capacity to inhibit CaxPO4 precipitation (mean IC50: 9.0 microL serum [SD 3.1] vs 7.5 [0.8] in short-term patients and 6.4 [2.6] in controls) [37].

Analytical, diagnostic and therapeutic context of Inhibitory Concentration 50


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  2. Effects of anti-epidermal growth factor (EGF) receptor antibodies and an anti-EGF receptor recombinant-ricin A chain immunoconjugate on growth of human cells. Taetle, R., Honeysett, J.M., Houston, L.L. J. Natl. Cancer Inst. (1988) [Pubmed]
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  7. The N-methyl-D-aspartate receptor complex in Alzheimer's disease: reduced regulation by glycine but not zinc. Steele, J.E., Palmer, A.M., Stratmann, G.C., Bowen, D.M. Brain Res. (1989) [Pubmed]
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  10. Efficiency of signalling through cytokine receptors depends critically on receptor orientation. Syed, R.S., Reid, S.W., Li, C., Cheetham, J.C., Aoki, K.H., Liu, B., Zhan, H., Osslund, T.D., Chirino, A.J., Zhang, J., Finer-Moore, J., Elliott, S., Sitney, K., Katz, B.A., Matthews, D.J., Wendoloski, J.J., Egrie, J., Stroud, R.M. Nature (1998) [Pubmed]
  11. FK-506- and CsA-sensitive activation of the interleukin-2 promoter by calcineurin. O'Keefe, S.J., Tamura, J., Kincaid, R.L., Tocci, M.J., O'Neill, E.A. Nature (1992) [Pubmed]
  12. Proton inhibition of N-methyl-D-aspartate receptors in cerebellar neurons. Traynelis, S.F., Cull-Candy, S.G. Nature (1990) [Pubmed]
  13. Novel renin inhibitors containing the amino acid statine. Boger, J., Lohr, N.S., Ulm, E.H., Poe, M., Blaine, E.H., Fanelli, G.M., Lin, T.Y., Payne, L.S., Schorn, T.W., LaMont, B.I., Vassil, T.C., Stabilito, I.I., Veber, D.F., Rich, D.H., Bopari, A.S. Nature (1983) [Pubmed]
  14. Treatment of melanoma cells with the synthetic retinoid CD437 induces apoptosis via activation of AP-1 in vitro, and causes growth inhibition in xenografts in vivo. Schadendorf, D., Kern, M.A., Artuc, M., Pahl, H.L., Rosenbach, T., Fichtner, I., Nürnberg, W., Stüting, S., von Stebut, E., Worm, M., Makki, A., Jurgovsky, K., Kolde, G., Henz, B.M. J. Cell Biol. (1996) [Pubmed]
  15. Activity of purified biosynthetic proteinase of human immunodeficiency virus on natural substrates and synthetic peptides. Kräusslich, H.G., Ingraham, R.H., Skoog, M.T., Wimmer, E., Pallai, P.V., Carter, C.A. Proc. Natl. Acad. Sci. U.S.A. (1989) [Pubmed]
  16. Potent and highly selective human immunodeficiency virus type 1 (HIV-1) inhibition by a series of alpha-anilinophenylacetamide derivatives targeted at HIV-1 reverse transcriptase. Pauwels, R., Andries, K., Debyser, Z., Van Daele, P., Schols, D., Stoffels, P., De Vreese, K., Woestenborghs, R., Vandamme, A.M., Janssen, C.G. Proc. Natl. Acad. Sci. U.S.A. (1993) [Pubmed]
  17. Detection of human immunodeficiency virus type 1 clinical isolates with reduced sensitivity to zidovudine and dideoxyinosine by RNA.RNA hybridization. Japour, A.J., Chatis, P.A., Eigenrauch, H.A., Crumpacker, C.S. Proc. Natl. Acad. Sci. U.S.A. (1991) [Pubmed]
  18. Impact of stavudine phenotype and thymidine analogues mutations on viral response to stavudine plus lamivudine in ALTIS 2 ANRS trial. Calvez, V., Costagliola, D., Descamps, D., Yvon, A., Collin, G., Cécile, A., Delaugerre, C., Damond, F., Marcelin, A.G., Matheron, S., Simon, A., Valantin, M.A., Katlama, C., Brun-Vézinet, F. Antivir. Ther. (Lond.) (2002) [Pubmed]
  19. N-Acetylcysteine potentiates inhibition of platelet aggregation by nitroglycerin. Loscalzo, J. J. Clin. Invest. (1985) [Pubmed]
  20. Potential use of imatinib in Ewing's Sarcoma: evidence for in vitro and in vivo activity. Merchant, M.S., Woo, C.W., Mackall, C.L., Thiele, C.J. J. Natl. Cancer Inst. (2002) [Pubmed]
  21. Regional chemotherapy for bladder neoplasms using continuous intravesical infusion of doxorubicin: impact of concomitant administration of dimethyl sulfoxide on drug absorption and antitumor activity. See, W.A., Xia, Q. J. Natl. Cancer Inst. (1992) [Pubmed]
  22. In vitro and in vivo effects of leukotriene B4 antagonism in a primate model of asthma. Turner, C.R., Breslow, R., Conklyn, M.J., Andresen, C.J., Patterson, D.K., Lopez-Anaya, A., Owens, B., Lee, P., Watson, J.W., Showell, H.J. J. Clin. Invest. (1996) [Pubmed]
  23. Peroxynitrite-induced apoptosis in human intestinal epithelial cells is attenuated by mesalamine. Sandoval, M., Liu, X., Mannick, E.E., Clark, D.A., Miller, M.J. Gastroenterology (1997) [Pubmed]
  24. The IP-10 chemokine binds to a specific cell surface heparan sulfate site shared with platelet factor 4 and inhibits endothelial cell proliferation. Luster, A.D., Greenberg, S.M., Leder, P. J. Exp. Med. (1995) [Pubmed]
  25. Correlation of intrinsic chemoresistance of non-small-cell lung cancer cell lines with HER-2/neu gene expression but not with ras gene mutations. Tsai, C.M., Chang, K.T., Perng, R.P., Mitsudomi, T., Chen, M.H., Kadoyama, C., Gazdar, A.F. J. Natl. Cancer Inst. (1993) [Pubmed]
  26. Glucagon-like peptide-1 is a physiological incretin in rat. Wang, Z., Wang, R.M., Owji, A.A., Smith, D.M., Ghatei, M.A., Bloom, S.R. J. Clin. Invest. (1995) [Pubmed]
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  28. Upregulation of the rat cardiac sodium channel by in vivo treatment with a class I antiarrhythmic drug. Taouis, M., Sheldon, R.S., Duff, H.J. J. Clin. Invest. (1991) [Pubmed]
  29. Melatonin is a potent modulator of dopamine release in the retina. Dubocovich, M.L. Nature (1983) [Pubmed]
  30. Benzodiazepine peptidomimetics: potent inhibitors of Ras farnesylation in animal cells. James, G.L., Goldstein, J.L., Brown, M.S., Rawson, T.E., Somers, T.C., McDowell, R.S., Crowley, C.W., Lucas, B.K., Levinson, A.D., Marsters, J.C. Science (1993) [Pubmed]
  31. Macrophage deactivation by interleukin 10. Bogdan, C., Vodovotz, Y., Nathan, C. J. Exp. Med. (1991) [Pubmed]
  32. Characterization and species distribution of high affinity GTP-coupled receptors for human rantes and monocyte chemoattractant protein 1. Van Riper, G., Siciliano, S., Fischer, P.A., Meurer, R., Springer, M.S., Rosen, H. J. Exp. Med. (1993) [Pubmed]
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  34. Inhibition of interleukin 1 (IL-1) binding and bioactivity in vitro and modulation of acute inflammation in vivo by IL-1 receptor antagonist and anti-IL-1 receptor monoclonal antibody. McIntyre, K.W., Stepan, G.J., Kolinsky, K.D., Benjamin, W.R., Plocinski, J.M., Kaffka, K.L., Campen, C.A., Chizzonite, R.A., Kilian, P.L. J. Exp. Med. (1991) [Pubmed]
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  37. Association of low fetuin-A (AHSG) concentrations in serum with cardiovascular mortality in patients on dialysis: a cross-sectional study. Ketteler, M., Bongartz, P., Westenfeld, R., Wildberger, J.E., Mahnken, A.H., Böhm, R., Metzger, T., Wanner, C., Jahnen-Dechent, W., Floege, J. Lancet (2003) [Pubmed]
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