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Activation of Src family kinases by colony stimulating factor-1, and their association with its receptor. 总被引:32,自引:4,他引:28
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S A Courtneidge R Dhand D Pilat G M Twamley M D Waterfield M F Roussel 《The EMBO journal》1993,12(3):943-950
The receptor for the macrophage colony stimulating factor-1 (CSF-1R) is a transmembrane glycoprotein with intrinsic tyrosine kinase activity. CSF-1 stimulation promotes the growth of cells of the macrophage lineage and of fibroblasts engineered to express CSF-1R. We show that CSF-1 stimulation resulted in activation of three Src family kinases, Src, Fyn and Yes. Concomitant with their activation, all three Src family kinases were found to associate with the ligand-activated CSF-1 receptor. These interactions were also demonstrated in SF9 insect cells co-infected with viruses encoding the CSF-1 receptor and Fyn, and the isolated SH2 domain of Fyn was capable of binding the CSF-1R in vitro. Analysis of mutant CSF-1Rs revealed that the 'kinase insert' (KI) domain of CSF-1R was not required for interactions with Src family kinases, but that mutation of one of the receptor autophosphorylation sites, Tyr809, reduced both their binding and enzymatic activation. Because fibroblasts expressing this receptor mutant are unable to form colonies in semi-solid medium or to grow in chemically defined medium in the presence of CSF-1, the Src family kinases may play a physiological role in the mitogenic response to CSF-1. 相似文献
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Xiang-Yang Ye Stephanie Chen Hao Zhang Kenneth T. Locke Kevin O’Malley Litao Zhang Raijit Srivastava Bowman Miao Daniel Meyers Hossain Monshizadegan Debra Search Denise Grimm Rongan Zhang Jonathan Lippy Celeste Twamley Jodi K. Muckelbauer Chiehying Chang Yongmi An Vinayak Hosagrahara Lisa Zhang Joseph A. Tino 《Bioorganic & medicinal chemistry letters》2010,20(9):2933-2937
The synthesis and follow-up SAR studies of our development candidate 1 by incorporating 2-aryl-4-oxazolylmethoxy and 2-aryl-4-thiazolylmethoxy moieties into the oxybenzylglycine framework of the PPARα/γ dual agonist muraglitazar is described. SAR studies indicate that different substituents on the aryloxazole/thiazole moieties as well as the choice of carbamate substituent on the glycine moiety can significantly modulate the selectivity of PPARα versus PPARγ. Potent, highly selective PPARα activators 2a and 2l, as well as PPARα activators with significant PPARγ activity, such as 2s, were identified. The in vivo pharmacology of these compounds in preclinical animal models as well as their ADME profiles are discussed. 相似文献
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The single crystal structure of LaPS4, (1), is reported. The space group is tetragonal, I4(1)/acd. Unit cell dimensions are a = 10.9641(3) Å and c = 19.4828(9) Å. The far infrared absorption and Raman spectra (100-600 cm−1) are consistent with the groups being in a distorted tetrahedral geometry. The room temperature emission spectrum of LaPS4 doped with Er3+ is also presented. Emission peaks at 529, 534, 549, and 554 nm were observed when the sample was excited at 492 nm. The compound reported here is isomorphous and isostructural to several other lanthanide orthothiophosphates. 相似文献
4.
Ahmed Muhib Ward Sinead McCann Malachy Kavanagh Kevin Heaney Frances Devereux Michael Twamley Brendan Rooney Denise 《Biometals》2022,35(1):173-185
BioMetals - A series of phenanthroline-oxazine ligands were formed by a cyclisation reaction between L-tyrosine amino acid esters and 1,10-phenanthroline-5,6-dione (phendione). The methyl... 相似文献
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Ye XY Li YX Farrelly D Flynn N Gu L Locke KT Lippy J O'Malley K Twamley C Zhang L Ryono DE Zahler R Hariharan N Cheng PT 《Bioorganic & medicinal chemistry letters》2008,18(12):3545-3550
Several series of substituted dehydropiperidine and piperidine-4-carboxylic acid analogs have been designed and synthesized as novel, potent dual PPARalpha/gamma agonists. The SAR of these series of analogs is discussed. A rare double bond migration occurred during the basic hydrolysis of the alpha,beta-unsaturated dehydropiperidine esters 12, and the structures of the migration products were confirmed through a series of 2D NMR experiments. 相似文献
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