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A high throughput screening campaign
2025-01-22
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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The compounds containing beryllium act as
2025-01-22
The compounds containing beryllium act as strong Lewis acids because of electron deficiency of the Be Garcinol []. Interactions of X-Be-Y compounds with different Lewis bases have been studied by Yanez and co-workers [], extensively. Recently, they proposed a class of extremely strong bidentate Be-
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It has been well established
2025-01-21
It has been well established that shortly after systemic inflammation, NADPH oxidase and iNOS activity were increased in the MC 1568 receptor and lead to overproduction of reactive oxygen species (ROS) and NO [66]. Moreover, previous studies indicated that Ang II induced an increased level of NADPH
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Immunohistochemistry in tissue samples showed the expression
2025-01-21
Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of BI-D1870 tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-activator also resulted in si
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Second the phosphorylation events e
2025-01-21
Second, the phosphorylation events (e.g., α-Thr172 and β-Ser108) needed for AMPK activation by small molecules binding at the ADaM or other sites remains unclear. Within the β-GBD, phosphorylation of β1-Ser108 was shown to be required for the activation by small molecules binding in the ADaM site, s
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br Effects of BCAAs on
2025-01-21
Effects of BCAAs on glucose metabolism Insulin plays an exclusive role in regulation of glucose metabolism, and obesity and type 2 diabetes induce hyperinsulinemia due to insulin resistance. Plasma BCAA concentrations are increased by 14–20% in patients with hyperinsulinemia under overnight fasti
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Our results add to previously published data
2025-01-21
Our results add to previously published data on the contribution of ALDH3A1 to the optical properties of the cornea. Specifically, the study by Nees et al. (2002) was among the first to examine whether ALDH3A1 serves as a structural component in the cornea and similarly to lens crystallins. Their ex
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However there are a lot of external
2025-01-21
However, there are a lot of external magnetic field disturbances in urban environments, for example when the AHRS is close to a ferrous or magnetic object, which will disturb the output of magnetometer, then the observational errors cannot satisfy the assumption of Kalman filtering, and so, the atti
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Ketogenic diets are more effective
2025-01-21
Ketogenic diets are more effective in promoting weight loss than conventional caloric restriction [26] however, their effect on hepatic glucose and lipid metabolism remains inconclusive. Blood glucose homeostasis is tightly regulated. In both mice and humans consuming KD, baseline blood glucose decr
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Circulating adrenal derived stress hormones epinephrine
2025-01-21
Circulating adrenal-derived stress hormones, epinephrine and corticosterone mediate their tissue effects through adrenergic (AR; α and β) and glucocorticoid (GR) receptors. AR are widely distributed throughout the body and although epinephrine is a prototypical agonist for all types of AR, the selec
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Rising depolarization was observed during and decaying depol
2025-01-21
Rising depolarization was observed during and decaying depolarization after the photostimulation (Fig. 1D). The slow decrease of the firing rate after photostimulation is also a remarkable characteristic of the striatal neuron (Figs. 1E, 2 and 3), since the cortex pyramidal neurons (data not shown)
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Nexturastat A br Adiponectin receptors in colorectal cancer
2025-01-21
Adiponectin receptors in colorectal cancer development APN receptors expressed in CRC tissue may mediate its effects on cell expansion and cell death (Byeon et al., 2010). It was observed that the expression of AdipoR1 and 2 is higher in CRC tissue than in counterpart healthy tissues (Williams et
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The second evidence comes from the results obtained
2025-01-21
The second evidence comes from the results obtained by patch-clamp recordings carried out at the endplate region of isolated mouse FDB fibers, where adenosine and the P1R agonist NECA significantly affected the NPo, the open frequency and the time constant τ of the adult nAChR channels. It is genera
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br Materials and methods br Functional demonstrations of ACh
2025-01-21
Materials and methods Functional demonstrations of ACh/GABA cotransmission The cotransmission of GABA and ACh has been best characterized in starburst amacrine cells (SACs) of the retina. SACs are a subtype of amacrine cell, a diverse set of retinal interneurons that are crucial for processing
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However although in vitro studies in heterologous systems
2025-01-21
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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