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Chemical Compound Review

SureCN7181349     1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3...

Synonyms: AR-1K3017, AC1LA7LL, 1R*)]-
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Disease relevance of AIDS-104355


High impact information on AIDS-104355

  • Circulating Fc gamma 2b/gamma 1R was also detected in normal mouse serum at a concentration of 10(-9) to 10(-8) M [1].
  • The increase in cell-associated and soluble Fc gamma 2b/gamma 1R after LPS activation is attributable primarily to B cells [1].
  • 1R compromises membrane skeleton assembly in erythroid progenitors [6].
  • The combination of PGE2 and prednisolone increased the number of IL 1R on fibroblasts in an additive manner [7].
  • When a 3Q/1R ratio is restored by a mirror R-->Q substitution in the R-SNARE Snc2p, wild-type functionality is observed [8].

Chemical compound and disease context of AIDS-104355

  • Transgenic TG1306/1R (TG) mice with cardiac-specific Ang II overproduction demonstrate blood pressure-independent cardiac hypertrophy and exhibit significant increase in sudden death associated with mechanical dysfunction [9].

Biological context of AIDS-104355

  • The clone cross-hybridized at a lower frequency to rye chromosome arms 1R (long) (4.4%) and 2R (short) (2.6%), where two additional rye storage-protein loci, Sec-3 and Sec-2, respectively, have been mapped [10].
  • (1R)- and (1S)-norcamphor (> 92 enantiomeric excess) were characterized in the hydroxylation reaction with cytochrome P450cam with respect to the product profile, steady state kinetics, coupling efficiency, and free energy of substrate dissociation [11].
  • Analysis of the segregation of restriction fragment length polymorphism in crosses of inbred mice now establish that the structural genes encoding both Fc epsilon RI alpha and Fc gamma 2b/gamma 1R are indeed discrete genes and are linked at the distal end of mouse chromosome 1 [12].
  • These results suggest that IL 1R are expressed as the result of monocyte-T cell interaction in the early stage of T cell activation, and the expression of IL 1R on T cells and the responsiveness of T cells for IL 1 require the accessory function of HLA-DR-positive monocytes [13].
  • Nucleotypic modifications mediated by changes in the 1R chromosome structure include increased proximity between homologous rDNA loci in interphase, and an increase in the frequency of cells with intra-nucleolar ribosomal condensed chromatin [14].

Anatomical context of AIDS-104355

  • The regulation of interleukin 1 receptor (IL 1R) expression on human dermal fibroblasts was investigated [7].
  • When purified T cells alone were stimulated with Con A, IL 1R were only marginally expressed [13].
  • Peripheral blood lymphocytes expressed only few IL 1R without any stimulations [13].
  • However, by the addition of monocytes, IL 1R were expressed on T cells in a dose-dependent manner [13].
  • In contrast, IgG1 rosettes and IgG2b rosettes of both macrophages and lymphocytes were inhibited not only by homologous isotype but also by IgE, suggesting that IgE has some affinity for Fc gamma 1/2bR on macrophages and for both Fc gamma 1R and Fc gamma 2bR on lymphocytes [15].

Associations of AIDS-104355 with other chemical compounds

  • However, the nonselective herbicides 3-amino-1,2,4-triazole and a newly synthesized triazole [(1R*, 3R*)-[3-hydroxy-3-(2H-[1,2,4]triazole-3-yl)-cyclohexyl]- phosphonic acid], inhibited Arabidopsis and wheat IGPDs in a mixed-type and a competitive manner, respectively [16].
  • The C-2 epimer, (1R/S,4R/S)-6R/S-(N, N-dimethylamino)-5R/S-phenylbicyclo[2.2.2]oct-2R/S-yl benzoate, was selective and potent in binding to the 5-HT transporter (IC(50) = 53 nM versus 1050 nM for cocaine) as compared to the DA transporter (IC(50) = 358 nM) [17].
  • This study sought to determine whether other alpha/beta-hydrolases are stereoselectively inhibited by isomalathion and if the difference in mechanism of AChE inactivation between (1R)- and (1S,3S)-isomers is conserved for other alpha/beta-hydrolases [18].
  • Membranes were either phosphorylated with PKA in the absence/presence of a protein kinase inhibitor (PKI) or dephosphorylated with alkaline phosphatase (AP) and assayed for adenylyl cyclase activity (AC) in the presence of the beta 1R agonist isoproterenol (ISO) and/or the A1R agonist 2-chloro-N6-cyclopentyladenosine (CCPA) [19].
  • A novel tunable multi-chiral supramolecular host system was developed from non-chiral dicarboxylic acid and (1R, 2R)-diphenylethylenediamine via chirality transfer, which enabled highly efficient optical resolution of secondary alkyl alcohols by simple crystallization of host compounds from alcohol solution [20].

Gene context of AIDS-104355

  • Furthermore the binding of 125I-labeled IL 1 alpha to IL 1R on T cells was inhibited by the addition of either cold IL 1 alpha or IL beta, but not by interleukin 2 or interferons [13].
  • The expression of interleukin 1 receptors (IL 1R) on human peripheral T cells was studied by the binding assay with 125I-labeled recombinant human interleukin 1 (IL 1) alpha and IL 1 beta and by the flow cytofluorometry with the fluorescein isothiocyanate (FITC)-conjugated IL 1 alpha [13].
  • Ligand-binding studies were performed to compare solubilized EL 4 NOB.1 cell membrane IL 1 receptor (sIL 1R) with semi-purified IL 1 beta binding protein from pooled synovial fluid [21].
  • We compared the growth rates, IGFBP production, IGF I binding characteristics, IGF 1R protein and mRNA levels, and the acute IGF I response (stimulation of glycogen synthesis) after pretreatment of the cells in serum-free medium with or without added IGF I or medium supplemented with 5% fetal calf serum (FCS) [4].
  • The expression of IL-6 mRNA in the hypothalamus did not change in 1R group but decreased in 2R and 3R groups [22].

Analytical, diagnostic and therapeutic context of AIDS-104355

  • The circulating Fc gamma 2b/gamma 1R bound to IgG-Sepharose, and was partially purified by affinity chromatography on 2.4G2 Fab-Sepharose [1].
  • After radiolabeling and immunoprecipitation with rabbit anti-Fc gamma 2b/gamma 1R serum, one component of Mr 48,000, was detected [1].
  • The maximum IL 1R-positive T cells were approximately 30% by the detection of the flow cytofluorometry with FITC-conjugated IL 1 alpha [13].
  • By using intact or Fab fragments of rat monoclonal antibodies against murine Fc gamma 2b/gamma 1 receptor, in a solid phase radioimmunoassay, we demonstrated the occurrence of circulating cellfree Fc gamma 2b/gamma 1 receptors (Cf-Fc gamma 2b/gamma 1R) in normal mouse serum [23].
  • In hypothalamic astroglial cell cultures the adrenergic stimulus of IPs generation was also mediated by alpha 1R [24].


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  2. Sodium butyrate induces histone hyperacetylation and differentiation of murine embryonal carcinoma cells. McCue, P.A., Gubler, M.L., Sherman, M.I., Cohen, B.N. J. Cell Biol. (1984) [Pubmed]
  3. Elimination of glucagon-like peptide 1R signaling does not modify weight gain and islet adaptation in mice with combined disruption of leptin and GLP-1 action. Scrocchi, L.A., Hill, M.E., Saleh, J., Perkins, B., Drucker, D.J. Diabetes (2000) [Pubmed]
  4. Insulin-like growth factor (IGF) I down-regulates type 1 IGF receptor (IGF 1R) and reduces the IGF I response in A549 non-small-cell lung cancer and Saos-2/B-10 osteoblastic osteosarcoma cells. Bostedt, K.T., Schmid, C., Ghirlanda-Keller, C., Olie, R., Winterhalter, K.H., Zapf, J. Exp. Cell Res. (2001) [Pubmed]
  5. Gastric cancer: the role of insulin-like growth factor 2 (IGF 2) and its receptors (IGF 1R and M6-P/IGF 2R). Pavelić, K., Kolak, T., Kapitanović, S., Radosević, S., Spaventi, S., Kruslin, B., Pavelić, J. J. Pathol. (2003) [Pubmed]
  6. Protein 4.1R-deficient mice are viable but have erythroid membrane skeleton abnormalities. Shi, Z.T., Afzal, V., Coller, B., Patel, D., Chasis, J.A., Parra, M., Lee, G., Paszty, C., Stevens, M., Walensky, L., Peters, L.L., Mohandas, N., Rubin, E., Conboy, J.G. J. Clin. Invest. (1999) [Pubmed]
  7. Interleukin 1 stimulates its own receptor expression on human fibroblasts through the endogenous production of prostaglandin(s). Akahoshi, T., Oppenheim, J.J., Matsushima, K. J. Clin. Invest. (1988) [Pubmed]
  8. Exocytosis requires asymmetry in the central layer of the SNARE complex. Ossig, R., Schmitt, H.D., de Groot, B., Riedel, D., Keränen, S., Ronne, H., Grubmüller, H., Jahn, R. EMBO J. (2000) [Pubmed]
  9. Chronic angiotensin II stimulation in the heart produces an acquired long QT syndrome associated with IK1 potassium current downregulation. Domenighetti, A.A., Boixel, C., Cefai, D., Abriel, H., Pedrazzini, T. J. Mol. Cell. Cardiol. (2007) [Pubmed]
  10. Physical mapping of a low-copy DNA sequence in rye (Secale cereale L.). Gustafson, J.P., Butler, E., McIntyre, C.L. Proc. Natl. Acad. Sci. U.S.A. (1990) [Pubmed]
  11. Stereoselective hydroxylation of norcamphor by cytochrome P450cam. Experimental verification of molecular dynamics simulations. Loida, P.J., Sligar, S.G., Paulsen, M.D., Arnold, G.E., Ornstein, R.L. J. Biol. Chem. (1995) [Pubmed]
  12. Receptors for Fc epsilon and Fc gamma are linked on mouse chromosome 1. Huppi, K., Mock, B.A., Hilgers, J., Kochan, J., Kinet, J.P. J. Immunol. (1988) [Pubmed]
  13. Expression of interleukin 1 receptors on human peripheral T cells. Shirakawa, F., Tanaka, Y., Ota, T., Suzuki, H., Eto, S., Yamashita, U. J. Immunol. (1987) [Pubmed]
  14. Genome restructuring in rye affects the expression, organization and disposition of homologous rDNA loci. Caperta, A.D., Neves, N., Morais-Cecílio, L., Malhó, R., Viegas, W. J. Cell. Sci. (2002) [Pubmed]
  15. Induction of Fc epsilon receptors on mouse macrophages and lymphocytes by homologous IgE. Daeron, M., Ishizaka, K. J. Immunol. (1986) [Pubmed]
  16. Insect cell expression of recombinant imidazoleglycerolphosphate dehydratase of Arabidopsis and wheat and inhibition by triazole herbicides. Tada, S., Hatano, M., Nakayama, Y., Volrath, S., Guyer, D., Ward, E., Ohta, D. Plant Physiol. (1995) [Pubmed]
  17. Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes. Javanmard, S., Deutsch, H.M., Collard, D.M., Kuhar, M.J., Schweri, M.M. J. Med. Chem. (1999) [Pubmed]
  18. Probing the active sites of butyrylcholinesterase and cholesterol esterase with isomalathion: conserved stereoselective inactivation of serine hydrolases structurally related to acetylcholinesterase. Doorn, J.A., Talley, T.T., Thompson, C.M., Richardson, R.J. Chem. Res. Toxicol. (2001) [Pubmed]
  19. Beta-adrenergic and antiadrenergic modulation of cardiac adenylyl cyclase is influenced by phosphorylation. Dobson, J.G., Shea, L.G., Fenton, R.A. Am. J. Physiol. Heart Circ. Physiol. (2003) [Pubmed]
  20. Efficient optical resolution of secondary alkyl alcohols by chiral supramolecular hosts. Imai, Y., Sato, T., Kuroda, R. Chem. Commun. (Camb.) (2005) [Pubmed]
  21. A soluble binding protein specific for interleukin 1 beta is produced by activated mononuclear cells. Symons, J.A., Eastgate, J.A., Duff, G.W. Cytokine (1990) [Pubmed]
  22. Effects of repeated stress on expression of interleukin-6 (IL-6) and IL-6 receptor mRNAs in rat hypothalamus and midbrain. Miyahara, S., Komori, T., Fujiwara, R., Shizuya, K., Yamamoto, M., Ohmori, M., Okazaki, Y. Life Sci. (2000) [Pubmed]
  23. Circulating cellfree Fc gamma 2b/gamma 1 receptor in normal mouse serum: its detection and specificity. Khayat, D., Dux, Z., Anavi, R., Shlomo, Y., Witz, I.P., Ran, M. J. Immunol. (1984) [Pubmed]
  24. Alpha 1-adrenergic receptor coupling with phospholipase-C is negatively regulated by protein kinase-C in primary cultures of hypothalamic neurons and glial cells. Drouva, S.V., Faivre-Bauman, A., Loudes, C., Laplante, E., Kordon, C. Endocrinology (1991) [Pubmed]
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