The present invention relates to pharmaceutical compositions comprising one or more phosphodiesterase type IV ("PDE-IV") inhibitors, and at least one other active ingredient selected from muscarinic receptor antagonists (MRA), <225> 2 -agonists, p38 MAP Kinase inhibitors, and corticosteroids, and, ...
可以看到,除了典型的type II比如imatinib等,以及几个allosteric,其余皆归类于type I,尽管有点简单,但也没有争议。 而有的文章提的type I 1/2 B、type IIB,尽管是因为激酶构象不是“纯正”的active构象,而被额外分出来,但谁又规定type I inhibitor不能结合inactive构象? 比如erlotinib结合EGFR的例子,蛋白处于active...
MacKenzie SJ, Houslay MD 2000 Action of rolipram on specific PDE4 cAMP phosphodiesterase isoforms and on the phosphorylation of cAMP-response-element-binding protein (CREB) and p38 mitogen-activated protein (MAP) kinase in U937 monocytic cells. Biochem J 347: 571–578 Article CAS Google Scholar ...
We evaluated the anti-fibrotic therapeutic potential of a small-molecule inhibitor of TGF-β type I receptor kinase, EW-7197, on HIF1α-derived TGF-β signaling in cholestatic liver fibrosis. We used a bile duct ligation (BDL)-operated rat model to characterize the role of HIF1α-derived ...
type I, type II and type III IFN loci, which are linked with 3-hydroxyacyl-CoA dehydratase 4 (HACD4)/rho GTPase activating protein 27 (ARHGAP27), dual specificity tyrosine phosphorylation regulated kinase 2 (DYRK2) and syncollin (SYCN)/SPT5 homolog (SUPT5H), respectively (Fig.5b, c,...
type I, type II and type III IFN loci, which are linked with 3-hydroxyacyl-CoA dehydratase 4 (HACD4)/rho GTPase activating protein 27 (ARHGAP27), dual specificity tyrosine phosphorylation regulated kinase 2 (DYRK2) and syncollin (SYCN)/SPT5 homolog (SUPT5H), respectively (Fig.5b, c,...
McArdle's disease (type V glycogen storage disease) is caused by deficiency of the phosphorylase kinase gene in the liver and muscle (McGrane, 2013). It is presented in adulthood and it is characterized by progressive muscle weakness and glycogen accumulation. This disease causes exercise intol...
55 SU5416 was the first tyrosine kinase inhibitor with known activity against FLT3 used in clinical trials of AML. Additional compounds that inhibit FLT3, from several companies, are now entering clinical development.21, 56, 57 These trials have been specifically designed to study the effects of ...
Ligand binding and ectodomain shedding are hypothesized to promote C-terminal intracellular domain interactions with multiple signaling pathway molecules including extracellular signal-regulated kinases 1/2 (ERK) and protein kinase C-alpha (PKC-α), and through a PDZ binding motif. The intracellular ...
The surfaces of many bacteria are decorated with long, exquisitely thin appendages called type IV pili (T4P), dynamic filaments that are rapidly polymerized and depolymerized from a pool of pilin subunits. Cycles of pilus extension, binding and retractio