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MK-571 sodium salt hydrate The ACC receptor family appear to
2020-09-26
The ACC receptor family appear to be attractive targets for the development of novel anthelmintics. With this in mind we also tested the activity of the anthelmintics levamisole and pyrantel which activate the nematode nAChR (Martin and Robertson, 2007). We found both molecules were partial agonists
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During the past decade it became increasingly clear
2020-09-25
During the past decade, it became increasingly clear that the affinity and efficacy of small agonists acting on the orthosteric binding site of a GPCR can be modulated by ligands that bind to a topographically distinct (allosteric) binding site on the same GPCR molecule 33, 39, 40, 41, 42. This allo
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In rodent models the loss of estrogens through ovariectomy h
2020-09-25
In rodent models, the loss of estrogens through ovariectomy has been shown to promote the development of intracranial aneurysms. Conversely, the administration of an Fulvestrant receptor beta agonist restores its protective effect, but is abolished with the introduction of a nitric oxide synthase i
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UNC1999 br Diverse functions of ERK pathway
2020-09-25
Diverse functions of ERK pathway Same as the other MAPK cascades, the ERK pathway is activated by several extracellular stimuli and different internal routes. ERK vitally tunes the function of various substrates in all cellular components; the nucleus, cytoplasm, membranes and the cytoskeleton. E
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The interferences between thapsigargin and forskolin induced
2020-09-25
The interferences between thapsigargin- and forskolin-induced Ca release indicate that these drugs deplete the same intracellular stores in RASMC. In fact, after partial depletion of thapsigargin-sensitive stores, the forskolin-induced increases in [Ca]c were significantly reduced. Similarly, a prev
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ML130 Treatment with AAV EP also improved aspects of adverse
2020-09-25
Treatment with AAV9-EP4 also improved aspects of adverse cardiac remodeling. The increased collagen deposition noted in the peri infarct and remote zone after MI was substantially attenuated by use of AAV9-EP4 and there were significant reductions in the number of macrophages and T ML130 infiltrati
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As illustrated in Table monocyclic acid analogs were
2020-09-25
As illustrated in Table 3, monocyclic vasopressin receptor antagonist analogs were synthesized and evaluated. 2-Oxido-3H-1,2,3,5-oxathiadiazol analog 8 showed 15-fold less potent EP1 receptor affinity relative to 2b, while it showed 2.2-fold more potent antagonist activity. Oxadiazole-5-one analog
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From an industrial perspective the low
2020-09-25
From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo
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If the effects described here are
2020-09-25
If the effects described here are present in catalysis, their empirical confirmation poses many challenges. Cat state correlations are fragile outside an environment especially suited for their preservation. As present day observational techniques whether in vivo or in vitro were not designed bearin
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br Materials and methods br Results br
2020-09-25
Materials and methods Results Discussion and conclusion The cardiac hypertrophy model can be established by two methods: drug induction and operation. The drug induction method is simple, while the operation method is closer to the real development of the disease. In this experiment, accord
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It was demonstrated that ET signaling is the
2020-09-25
It was demonstrated that ET-1 signaling is the primary axon guidance mechanism that accounts for sympathetic innervation of the sinoatrial node and myocardium in the developing mouse heart [11]. In this article, we will review the findings relating to the basic profiles; i.e. molecular features of
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br Results br Discussion br Materials and Methods br Acknowl
2020-09-25
Results Discussion Materials and Methods Acknowledgment This work was funded by the Collaborative Research Centre (SFB) 807 of the German Research Foundation (DFG) and supported by the state of Hessen (Center for Biomolecular Magnetic Resonance) and the German Research Foundation (DO545/
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In some cases more than one CYP enzyme
2020-09-25
In some cases, more than one CYP450 enzyme may be involved in the metabolism of a drug, and an Eadie–Hofstee plot is usually more reliable for assessing the involvement of multiple Aurora Kinase Inhibitor III (Bu, 2006). Therefore, we first plotted the Eadie–Hofstee curves and observed their shape t
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HOIP s ability to build linear
2020-09-25
HOIP\'s ability to build linear Ub chains arises from a unique domain that follows directly after the RING2 domain, the linear ubiquitin chain-determining domain (LDD) (Fig. 1). Structures have revealed that the LDD is structurally integrated into RING2, creating a single RING2–LDD unit (Fig. 2D) [4
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br Discussion The regulation of intracellular
2020-09-25
Discussion The regulation of intracellular cholesterol levels is a biological process of vital importance for cellular function and integrity, and involves robust transcriptional and post-transcriptional mechanisms that are sensitive to metabolic feedback control. Amongst post-transcriptional mec
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