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Natural product based drug discovery can be
2022-02-18

Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in melanotropin binding assays, we used molecular modeling to predict how well these compound
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A few previous studies have examined Factor
2022-02-18

A few previous studies have examined Factor Xa inhibitors for VTE prophylaxis in hip fracture patients. In a 2001 paper, Eriksson et al. studied 1250 patients with hip fractures that had been randomized to either postoperative Factor Xa inhibitor or enoxaparin [13]. Each patient received bilateral v
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In conclusion the present study shows that the
2022-02-18

In conclusion, the present study shows that the endothelin system is of importance in the cardiopulmonary vascular pathophysiology of porcine endotoxin shock. In this model, combination of a selective endothelin ETA and a selective endothelin ETB receptor antagonist markedly improved pulmonary circu
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Chicoric acid CA is a di acylated
2022-02-18

Chicoric Cy5 NHS ester (non-sulfonated) (CA) is a di-acylated hydroxycinnamoyl tartaric acid ester [12] found in a variety of plant species, especially within the Astereceae family [13]. Of interest for this study, Sonchus oleraceus and Bidens pilosa plants, from Astereceae family, were used. Both
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br Significance Cellular heterogeneity for
2022-02-18

Significance Cellular heterogeneity for phenotypic features is a key mechanism underlying disease progression and therapeutic resistance, yet its regulation is poorly understood at the molecular level. Our findings demonstrate that endocrine resistance is associated with higher transcriptomic het
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Another important outcome of reducing hypothalamic HIF
2022-02-18

Another important outcome of reducing hypothalamic HIF in DIO was the increase in gliosis and hypothalamic inflammation. Both experimental and human studies have shown that hypothalamic inflammation plays an important role in obesity by inducing resistance to anorexigenic signals, such as insulin a
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VDAC interacts with hexokinase and is implicated
2022-02-17

VDAC interacts with hexokinase and is implicated in NLRP3 activation in response to noxious stimuli including monosodium urate, silica, and alum (Zhou et al., 2011). Hexokinase dissociation may allow VDAC to carry out this role. It will be informative to block or silence VDAC to explore its function
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GSTs have been originally named ligandins
2022-02-17

GSTs have been originally named ‘ligandins’ because of their capacity to bind large ligand molecules (of molecular weight >400 Da) (Oakley et al., 1999). At least three separate Y-27632 have been reported for xenobiotics within the H-site; only one is for CDNB (Ralat and Colman, 2004). Usually, the
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Compared to previously reported atypical N glycosites that
2022-02-17

Compared to previously reported atypical N-glycosites that were identified based on the deamidation of asparagine residues after PNGase F treatment [106], [107], these two studies further validated the identified atypical motif glycosites by directly identifying their intact glycopeptides. Since the
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Herein we report the discovery
2022-02-17

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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Axons are the largest component of WM by
2022-02-17

Axons are the largest component of WM by volume and are a significant repository of intracellular glutamate that can be releases under ischemic conditions [1,3,4,29,117]. We have recently shown that the principle route by which mature myelinated MK0752 release glutamate during acute ischemia is via
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br Results br Discussion Postsynaptic trafficking of
2022-02-17

Results Discussion Postsynaptic trafficking of AMPA receptors, a process responsible for maintaining the steady-state level of AMPA receptor synaptic transmission, is believed to also actively partake in glutamatergic synaptic plasticity in principal neurons, such the hippocampal CA1 cells. He
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br Materials and methods br Results In order to address
2022-02-17

Materials and methods Results In order to address the role played by the catalytic and the anticodon-binding domains of E. coli GluRS in cognate and non-cognate aminoacylation, the two domains (NGluRS: 1–314; CGluRS: 318–471) of E. coli were expressed and purified (Fig. 1b). Prior to assessing
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Some of the key aspects of the myofibroblasts biology includ
2022-02-17

Some of the key aspects of the myofibroblasts’ biology, including their signaling sensitivity and residual regenerative potential, are shaped by their origin. In this respect, lineage studies on myofibroblast precursors are critical for increasing our understanding of the natural history of fibrosis
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In an effort to more fully explore the
2022-02-16

In an effort to more fully explore the structure–activity relationships of the ALLINIs and potentially attenuate resistance to known mutants, the central scaffold of these compounds was identified as a potential site for structural manipulation. Specifically, we wished to examine whether a scaffold
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