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A high throughput screening campaign led
2023-11-14

A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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As the experimental procedure used could reflect agonist
2023-11-14

As the experimental procedure used could reflect agonist-stimulation of both anterograde and retrograde APJ trafficking, as has been described for the δ-opioid peptide receptor (Zhang et al., 2006b, Zhang et al., 2006a), receptor internalization was more directly monitored by loading cell surface HA
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br Experimental procedures br Results br Discussion br
2023-11-14

Experimental procedures Results Discussion Acknowledgments SRE and EBL contributed equally to this EPZ004777 work. SRE, EBL, and MJT designed experiments, SRE, EBL, MCH, and AEI conducted experiments, SRE and EBL analyzed data, and EBL and MJT wrote the manuscript. We would like to than
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br The lipoxygenase pathway and
2023-11-14

The 12/15-lipoxygenase pathway and microvascular complications of diabetes The 12/15-lipoxygenase pathway in adipose tissue Only recently has adipose tissue been recognized as a highly metabolically active endocrine organ imparting profound local and systemic inflammatory effects. Adipose tiss
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Glycerol dehydratase GDHt EC is a key enzyme for
2023-11-14

Glycerol dehydratase (GDHt, EC 4.2.1.30) is a key enzyme for the bioconversion of glycerol into the value-added chemicals and thereby has recently attracted a great deal of attention as an essential component for metabolic engineering . GDHt carries out a radical-mediated turnover of glycerol into 3
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Active SI behavior was dose dependently
2023-11-13

Active SI behavior was dose-dependently affected by PACAP treatment (F3,25 = 14.42, p 69 8 1 week later (F3,20 = 8.93, p hypothesis that PACAP causes disruptions in posterror adjustments that are similar to disruptions seen in humans with depression.
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STF-118804 receptor It is worth mentioning that cordycepin
2023-11-13

It is worth mentioning that cordycepin, as an adenosine analogue, is structurally similar to adenosine. A previous study has shown that the anti-apoptotic effects of cordycepin are partially dependent on the activation of A1R [16], and cordycepin increases theta waves power density via nonspecific a
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br AMPK structure and mechanism of action AMPK is
2023-11-13

AMPK: structure and mechanism of action AMPK is a metabolic master switch that regulates downstream signals based on shifts in the surrounding energy reservoir [6]. It is expressed in a number of tissues, including the kidney, the liver, the skeletal muscle, the adipose tissue, and the hypothalam
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Ultraviolet UV spectroscopy is commonly used for screening p
2023-11-13

Ultraviolet (UV) spectroscopy is commonly used for screening potential ADA inhibitors [15]. In the UV method, the ADA reaction is calculated by measuring the decrease in absorbance of the substrate at 265 nm or increase in absorbance of the product at 248 nm. However, AD and inosine share a very clo
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Whereas more research is needed
2023-11-13

Whereas more research is needed to identify the precise mechanism by which FIN exerts its antidyskinetic effect, the Micafungin synthesis that it can negatively modulate dopaminergic transmission is also supported by our previous findings. Indeed, we have previously shown that FIN completely reverse
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The first rationally designed dual mPGES LO inhibitor was
2023-11-13

The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic BAY 80-6946 - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synthe
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The mechanism by which Gas prevents inflammation has been
2023-11-13

The mechanism by which Gas6 prevents inflammation has been reported to be via inhibition of Toll-Like receptors (TLRs) signaling (Cui et al., 2016). After injury, TLRs become stimulated, leading to downstream activation of TRAF3 and TRAF6 and translocation of several transcription factors, such as I
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If the lack of specificity and the high pleiotropy
2023-11-13

If the lack of specificity and the high pleiotropy may represent a problem in view of the potential chemotherapeutic features of autophagy-inducing agents, it Pirfenidone may switch into an advantage in the case of chemopreventive strategies. In fact, as non-pharmacologic interventions such as limi
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Since primitive societies plants herbs and seeds rich in phy
2023-11-13

Since primitive societies, plants, herbs and seeds, rich in phytochemicals, were used due to their benefits in human health. These molecules were shown to present a diverse array of action mechanisms, including antioxidant activity, enzyme stimulation, hormones mimicking and by interfering with DNA
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br Brain Angiotensin II receptors The information above leav
2023-11-13

Brain Angiotensin II receptors The information above leaves Angiotensin II receptors as the only RAAS components for which localization, regulation of expression and function in the SAR-302503 has been convincingly demonstrated, with the use of quantitative film and emulsion autoradiography to s
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