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br Acknowledgments This work was
2021-10-12
Acknowledgments This work was financially supported by the National Natural Science Foundation of China (No. 81703451) and the China Postdoctoral Science Foundation Grant (No. 2017M611269). Introduction According to the International League Against Epilepsy (ILAE), epilepsy is generally defin
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Tail group SAR of the imidazole
2021-10-12
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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k j and d were then submitted to metabolic stability
2021-10-12
15k, 15j and 14d, were then submitted to metabolic stability studies in human and mouse liver microsomes and permeability test with Caco-2 cells (Table 7). 15k, 15j and 14d all retained excellent permeability (Papp value greater than 15.2 × 10−6 cm/s) and displayed modestly improved metabolic stabil
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The developed method was used to
2021-10-12
The developed method was used to quantify RBC membrane transport of the anomers of three monofluorinated analogs of glucose in a modified medium designed to provide stable metabolic properties of the cells over the lifetime of the experiment. This allowed us to evaluate the specific interaction (spe
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Pefloxacin GCK MODY is the most common
2021-10-11
GCK-MODY is the most common form of MODY diabetes in many populations (Chevre et al., 1998; Massa et al., 2001; Barrio et al., 2002; Estalella et al., 2007; Pruhova et al., 2010; Capuano et al., 2012; Giuffrida et al., 2017). However, data about GCK-MODY among North African populations are very rare
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Corresponding to the different insulinotropic signaling the
2021-10-11
Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct SecinH3 on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site for full agonists
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Remarkably most of these molecules are
2021-10-11
Remarkably, most of these molecules are also quite effective in interfering with the proliferation of the drug-resistant cancer cell lines, with IC50 values ranging from 0.59 to 2.93 μM against MCF-7/ADR cells, and from 0.160 to 1.17 μM against NSCLC-resistant H1975 cells. Among these molecules, com
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In addition to the regulation of SV exo
2021-10-11
In addition to the regulation of SV exo- and Capreomycin Sulfate by Ca2+ influx retrieval of SV membranes depends on the exocytic insertion of SV components into the presynaptic membrane: If exocytic SV fusion in neurons is abrogated by genetic inactivation of the core release machinery (e.g. knock
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br Methods br Results br Discussion In
2021-10-11
Methods Results Discussion In the general population BNP has been established as a marker for GSK 2837808A failure diagnosis. Moreover, there is growing evidence that elevated levels of natriuretic-peptides may improve CV risk prediction in the general population above traditional risk fac
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One limitation of our study was that all control
2021-10-11
One limitation of our study was that all control dogs had histologic evidence of mild GI inflammation according to established WSAVA guidelines (Washabau et al., 2010), despite being apparently healthy purpose-bred research dogs housed in a controlled environment with no history of vomiting, diarrhe
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Anti apoptotic Bcl proteins have become
2021-10-11
Anti-apoptotic Bcl-2 proteins have become attractive targets for anti-cancer agents development, because they are associated with progression of a wide variety of human cancers., , The small-molecular Bcl-2 inhibitor venetoclax (ABT-199) () has been approved recently for the treatment of patients w
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br Soluble guanylyl cyclase nitric
2021-10-11
Soluble guanylyl cyclase, nitric oxide and nitric oxide synthase The primary and best-studied endogenous activator of soluble guanylyl cyclase (sGC) is nitric oxide (NO), which was originally describe as endothelium-derived relaxing factor for its potent ability to relax blood vessels in response
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To determine the functional consequences of HIV gp
2021-10-11
To determine the functional consequences of HIV gp120 binding to vaginal epithelial cells, an annotation clustering of the differentially expressed genes was performed. The top enriched biological processes included an inflammatory immune response, defense response and the pathways included the SODD
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GPR A a G protein coupled receptor located
2021-10-11
GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic pkc inhibitors [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to Gi-med
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Taken together specific antibodies and SR SIM used
2021-10-11
Taken together, specific p2y receptor and SR-SIM used in the study helped uniquely visualize the distribution of lymphocytes and macrophages with their molecular expression in human cochleae. Using SR-SIM, we verified that resident IBA1-positive macrophages are widely distributed in human cochlea (
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