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Arvanitis AG Rescinito JT Arnold CR Wilde RG Fitzgerald LW Zaczek R Hartig PR Grossman S Arneric SP Gilligan PJ Olson RE Robertson DW 《Bioorganic & medicinal chemistry letters》2003,13(1):129-131
A series of high affinity CRF receptor ligands with an imidazo[4,5-c]pyridine core is described. Individual analogues were synthesized and tested in vitro in rat brain receptors to determine binding affinity. The best compound was further tested in the dog N-in-1 pharmacokinetic model to assess oral bioavailability at 1 mg/kg po. 相似文献
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Sardha P. Suriyapperuma Larissa Lozovatsky Steven L. Ciciotte Luanne L. Peters Diana M. Gilligan 《Mammalian genome》2000,11(1):16-23
Mouse cDNA sequences encoding α, β, and γ adducins were cloned from a mouse reticulocyte cDNA library. The purified clones
contain alternatively spliced exons from all three adducin genes. In the case of α and β, the inclusion of the alternatively
spliced exons results in truncated polypeptide isoforms (called α-2 and β-2). The mouse predicted amino acid sequences are
compared with published rat and human sequences. For completion of this comparison, cDNA encoding the rat β-1 carboxy terminus
was cloned by PCR. The carboxy terminal region containing MARCKS homology, calmodulin-binding region-2, and spectrin-actin-binding
site, is conserved among α-1, β-1, and γ-1 isoforms in mouse, rat, and humans. We also report here the localization of the
gene encoding γ adducin (Add3) to murine Chr 19, in a region that shows conserved synteny with human Chr 10.
Received: 1 June 1999 / Accepted: 25 August 1999 相似文献
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A human hepatocellular carcinoma-derived cell line, PLC/PRF/5, was examined for its ability to respond to epidermal growth factor (EGF) exposure with increased phosphatidylinositol 4,5-bisphosphate hydrolysis. Upon addition of EGF (25 ng/ml), a rapid (10-15 s) but transient increase in Ins(1,4,5)P3 levels and large, prolonged (2 min) increases in Ins(1,3,4,5)P4 and Ins(1,3,4)P3 levels were detected. Increases in cytosolic Ca2+ were observed after a 10 to 20 s lag, reaching peak value at 1 min, and remaining elevated for 10 min. The initial burst of cytosolic Ca2+ occurred in the absence of extracellular Ca2+ and probably reflects mobilization of intracellular Ca2+ stores. In cells pretreated with EGTA, the sustained component of the Ca2+ response was not observed. Comparison of the inositol phosphate and Ca2+ responses of PLC/PRF/5 cells to responses reported in other cell types indicates that this cell line is a good model for EGF action in liver. 相似文献
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Y N Sinha T A Gilligan 《Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.)》1985,178(4):505-514
Peptide mapping of individual pituitary proteins within the gel after separation by electrophoresis in NaDodSO4-polyacrylamide gels has revealed a high-molecular-weight (mol wt) protein whose fingerprint is similar to that of prolactin (PRL). This protein is approximately 4000 greater in mol wt than the traditional pituitary PRL, but does not appear to be the latter's prohormone. Its concentration ranged from 3 to 15% of the major PRL protein in the pituitary glands of several species examined. The protein isolated from sheep pituitary glands partly cross-reacted with a polyclonal antibody raised against the main PRL, but the material from mouse pituitary glands was completely noncross-reactive. The substance eluted from denaturing gels failed to significantly stimulate mucosal growth in the crop sac of the pigeons, a commonly used test for PRL's bioactivity. Its biological activities remain to be characterized. 相似文献
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