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br Results and discussion Compounds were
2021-01-29
Results and discussion Compounds were tested for their binding affinity to human CRTH2 in a radioligand binding assay (3H-PGD2) using CHO cells stably transfected with human CRTH2. In addition, these compounds were assessed for their functional activity in PGD2 driven Ca2+ flux in KB8 cells expre
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Social interaction is known to be the
2021-01-29
Social interaction is known to be the main source of stress in human beings (Dickerson and Kemeny, 2004, Tamashiro et al., 2005). An animal model of social stress should closely mimic real-life situations in human life (Neisewander et al., 2012); in this context, social defeat in an agonistic encoun
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Telbivudine receptor Activating GSK signaling to inhibit PK
2021-01-29
Activating GSK3β signaling to inhibit PK signaling during ischemia/reperfusion (I/R) is protective of WM ischemic injury. Glycogen synthase kinase (GSK3), which was the first substrate identified for AKT [44], is inhibited by AKT phosphorylation at positions S9 and S21 [45]. When GSK3β is active, it
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The quantification and monitoring of ChEs enzymatic activiti
2021-01-29
The quantification and monitoring of ChEs enzymatic activities have traditionally been associated to environmental studies in order to diagnose the exposure of non-target organisms to specific anti-cholinesterasic agents (Nunes, 2011). The importance of these enzymes as biomarkers of environmental c
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Endothelins ETs are peptides expressed in both
2021-01-29
Endothelins (ETs) are peptides expressed in both the peripheral and the central nervous systems, which can contribute to sensory changes seen in animal models of inflammatory, cancer and neuropathic pain [10], [11]. All three mammalian isoforms (ET-1, ET-2 and ET-3) activate specific G protein-coupl
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Initially studies of GPCRs predominantly assessed
2021-01-29
Initially, studies of GPCRs predominantly assessed the signalling pathways downstream of receptors on the cell surface. There is now an understanding that GPCRs can localize to and signal from various intracellular compartments, such as the nucleus (reviewed in [40]). These intracellular pools of re
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The imaging and biochemical data presented here
2021-01-29
The imaging and biochemical data presented here demonstrated that in T cells, AEP played a specific function in cleaving Foxp3 but not Tbet. These results are in accordance with previous AEP studies where it has been shown that AEP substrates in part are not amenable to other protease activity. In a
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br Results and discussion br
2021-01-29
Results and discussion Conclusion Recent studies showed that EGFR signaling is involved in inflammatory response in several inflammatory conditions. The normal inflammatory macrophage BGP-15 receptor show EGFR-dependent production of inflammatory mediators. Nevertheless, the development of EG
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Crystallographic and NMR based analyses have revealed that
2021-01-29
Crystallographic and NMR-based analyses have revealed that RINGs and U-boxes have a common mode of interaction with E2s (Fig. 2A). The key structural elements are two loop-like regions, which, in the case of RINGs, coordinate Zn. The loops surround a shallow groove formed by the central α-helix. Tog
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Spectinomycin hydrochloride hydrate The current study provid
2021-01-29
The current study provides evidence for a previously unknown role for DHODH as a growth/survival factor in KRAS mutant tumors. While many aspects of the link between DHODH inhibition and survival of KRAS mutant cells remain to be established, de novo pyrimidine biosynthesis appears to be a crucial p
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Some mechanistic experiments performed in
2021-01-29
Some mechanistic experiments performed in the early 2000s by Ongusaha et al. [78], suggest that DDR1 induction protects T-5224 from apoptosis in a p53-dependent manner, and that impairment of DDR1 expression or function leads to a pronounced increase of DNA damage-induced apoptosis. This evidence su
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br Materials and methods br Results br
2021-01-28
Materials and methods Results Discussion CDK and their regulatory cyclins form a family of heterodimeric kinases that are particularly important for regulation of GSK621 progression and transcription in tumor cells. These kinases therefore constitute biomarkers of proliferation and attract
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The pharmacokinetics properties of compound were evaluated i
2021-01-28
The pharmacokinetics properties of compound were evaluated in male Sprague Dawley rats following IV (0.7mg/kg) and oral (2.0mg/kg) dosing. The total body clearance and the terminal half-life were 0.73 L/h/kg and 5.1h, respectively. After oral administration the compound showed good bioavailability
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Under optimized assay conditions very low concentrations pM
2021-01-28
Under optimized assay conditions, very low concentrations (20pM) of [125I]YP20 bound to hCRF1-CHO KPT-8602 membranes with high specificity (>95% inhibited by 1μM astressin) and in a membrane protein-dependent manner. Specific binding was selective vs. the hCRF2α subtype because little specific bind
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br Experimental methods br Results and discussion
2021-01-28
Experimental methods Results and discussion Conclusions Here we describe the first reported method for high-yield 1,4-DPCA australia of active and soluble mature CPG2 (in the absence of the leader peptide) and its individual catalytic and dimerization domains in E. coli. Such a method is o
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