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Until recently the first line treatment
2020-11-10
Until recently, the first line treatment of RLS was the administration of low dose of three dopaminergic drugs, which has been approved by the US Food and Drug Administration and the European Medicines Agency for the treatment of moderate to severe RLS. These compounds are pramipexole (Mirapex), rop
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In this contribution herein we
2020-11-10
In this contribution, herein we report our newly devised molecular probes with a triazole linked benzimidazole-indole-thiazolium mixed heterocyclic framework as depicted in Scheme 1. Their architecture was designed to achieve the advancement in selectivity and specificity toward DNA matrix over RNA
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SBI-0206965 receptor Considering the divergence of multiple
2020-11-10
Considering the divergence of multiple DGAT isoforms, we examined whether MiDGAT1 and MiDGAT2s utilized different fatty acids as the substrate to synthesize TAGs. GC-MS analysis indicated that C16:0 and C18:0 were the major components of TAGs in yeast cells, and all three MiDGATs displayed the same
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As shown in Fig there are two
2020-11-10
As shown in Fig. 9, there are two mechanisms for the removal of the Va-acyl group from PC to make it available for incorporation into TAG with DGATs' acting at the final acylation step. ①: Transfer of Va from PC to the acyl-CoA pool. This process can be driven by the reverse action of acyl- CoA:lyso
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Collectively the results presented here provide new insights
2020-11-10
Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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Our recent discovery M P
2020-11-10
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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We next examined the effects of substituents
2020-11-09
We next examined the effects of substituents around the carboxylic WZ4003 moiety on CRTH2 binding (Table 4). The carboxylic acid moiety shared by the representative CRTH2 antagonists and is essential for the CRTH2 activity. Germinal dimethylation of the methylene moiety next to the carboxylic acid
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The significant CRF increase in the DS and
2020-11-09
The significant CRF increase in the DS and the overall changes in the CRF system observed in the VM and DS during the development of sensitization suggest that this neuropeptide (and possibly urocortin) contributes to the specific molecular alterations occurring in the mesolimbic pathway that suppor
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br Acknowledgments br Introduction Understanding
2020-11-09
Acknowledgments Introduction Understanding the characteristics of the Amazonian Dark soils “Terras Pretas de Índio” (TPIs) is of ecological importance, because the TPI soils represent a residue-based model for tropical sustainable agriculture (Sombroek et al., 2003, Neves et al., 2003, Cohen-O
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br Conclusion br Introduction The morphological variability
2020-11-09
Conclusion Introduction The morphological variability of aquatic plants is well documented, and in some cases has seriously constrained taxonomic resolution (Sculthorpe, 1967, Santamaría, 2002). Many of these variations are caused by the extensive phenotypic plasticity of aquatic plants, but t
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br Materials and methods br Results br
2020-11-09
Materials and methods Results Discussion In this study, we uncovered a female-specific haplotype-MDD vulnerability association, by which a two-marker haplotype TG of rs4633-rs4680 may link to enhanced MDD risk in females. Female haplotype TG carriers were estimated to have a 9.17-fold incre
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Next our exploration shifted to modifications at the lateral
2020-11-09
Next, our exploration shifted to modifications at the lateral chain of the benzoquinone nucleus (SAR 2). Considering that the CK2 inhibitory activity is favoured by the presence of the -Ph-4-NO2 (SAR 1), the subsequent analogues were investigated with this moiety retained. The influence of the side
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In summary we demonstrated the high potency of fluxametamide
2020-11-09
In summary, we demonstrated the high potency of fluxametamide against M. domestica, L. striatellus, and T. urticae GABACls, which leads to high acaricidal/insecticidal effects on these arthropod pests. In contrast to its high potencies against the GABACls of arthropod pests, fluxametamide exhibited
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In patients with CTEPH ET levels
2020-11-09
In patients with CTEPH, ET-1 levels are raised and have been shown to fall after PEA surgery [24]. After an acute pulmonary embolism there is obstruction of the pulmonary chemicals library by acute thrombus and elevated levels of ET-1 [28], [30]. Elevated levels of ET-1 have also been observed in a
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Nevertheless because of the preclinical work and the interfe
2020-11-09
Nevertheless, because of the preclinical work and the interference with EWS–FLI1 transcriptional activity, we believe that there may be a role for ET-743 in Ewing sarcoma. An analysis of the pharmacokinetic data published in the phase II clinical trial shows that at most the drug spent 5 to 6days ou
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