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A high throughput screening campaign led
2024-09-10
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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Receptor Subtypes and Their Function
2024-09-10
Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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The enzyme Arginase ARG plays a
2024-09-10
The enzyme Arginase 1 (ARG1) plays a role in the hepatic urea cycle by hydrolyzing L-arginine to L-ornithine and urea [13]. In the context of macrophages and MDSCs, ARG1 expression redirects L-arginine metabolism to abolish cytotoxic nitric oxide production [14], suppress T-cell function [15], [16],
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Finally terbinafine is generally associated
2024-09-10
Finally, terbinafine is generally associated with a low index of toxicity and few adverse effects. In humans, only mild GI toxicity and hepatobiliary dysfunction are reported. In red-tailed hawks, oral administration of a high dose of terbinafine (120 mg/kg BW) was furthermore demonstrated to induce
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Glu Gln Asp and Asn the main amino acids presented
2024-09-10
Glu, Gln, Asp, and Asn, the main ctp cytidine triphosphate presented in the present study, are involved in nitrogen assimilation and transport processes within the plants. Furthermore, they are used to build up reserves during periods of nitrogen availability for subsequent use in growth, defense, a
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br Brain cell reactions Brain
2024-09-10
Brain cell reactions Brain cells in common with all metabolic cells must contain chemically active primary compounds which spontaneously initiate and continue cell reactions under normal conditions of temperature and pressure (NTP). These compounds have been identified as monophosphoric and polyp
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Mechanisms implicated in antinociception by A R
2024-09-09
Mechanisms implicated in antinociception by A3R agonists in neuropathic pain are summarized in Box 3. Cellular transduction mechanisms for A3Rs include inhibition of cyclic AMP, PKA via Gαi, interactions with PLC/IP3/DAG and signaling via Gαi and Gαq, and interactions with PI3K/MEK/ERK via βγ subuni
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In terms of the ring B C position while C
2024-09-09
In terms of the ring B C5′ position, while C5′-F (compound ) was tolerated, C5′-Me (compound ) and C5′-Cl (compound ) substitutions resulted in a loss in potency. However, the C5′-OMe substitution (compound ) resulted in a ∼3-fold increase in potency compared to . Modeling suggested a pseudo hydroge
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We have expressed the ECDs of the human and AChR
2024-09-09
We have expressed the ECDs of the human α1, β1, γ and ɛ AChR subunits in the past using the methylotropic yeast Pichia pastoris as soluble glycosylated proteins [15], [16]. Further work with the γ subunit ECD revealed a marked improvement of the solubility and yield following the mutation of hydroph
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In these experiments recordings were performed continuously
2024-09-09
In these experiments, recordings were performed continuously in the homecage and during the first 5 days of training on a randomized forced alternation T-maze working memory task (Figures 1A, 1B, 3A, and 3B) (Kucewicz et al., 2011). Sleep and wake states were determined by simultaneous recording of
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br In our experience br History of
2024-09-09
In our experience History of ER and ACh tests As shown in Table 1, Stein et al. first reported the usefulness of intravenous injection of ER in diagnosing coronary insufficiency in 1949 [16]. In 1972, the first ER spasm provocation test was employed at the Cleveland Clinic during cardiac cathe
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Toremifene receptor It has been recognized for decades that
2024-09-09
It has been recognized for decades that neurons in the mammalian central nervous system may release both a fast-acting, typically amino acid derived neurotransmitter such as glutamate or GABA, and a second peptidergic neuromodulatory molecule such as neuropeptide Y, substance P, or cholecystokinin.
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The present work has implications
2024-09-09
The present work has implications for our thinking about the effects of antidepressant (e.g. SSRIs) use on maternal care in depressed mothers which consist of approximately 10–20% of all mothers (Gjerdingen and Yawn, 2007, Susser et al., 2016), and more than 40% of depressed mothers are prescribed w
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NOXA a member of the pro apoptotic
2024-09-09
NOXA, a member of the pro-apoptotic B-cell lymphoma 2 (BCL-2) family, plays a vital role in regulating mitochondrial or inherent apoptotic pathways [7,8]. NOXA binds to MCL-1 with high affinity and interacts with A1 (known as BCL2A1), resulting in BIM release to trigger subsequent apoptosis [9]. In
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In this study we observed the ATPase activity of
2024-09-09
In this study, we observed the ATPase activity of RaGroEL at various temperatures and metal ions conditions and the role of GroES in the ATPase activity of RaGroEL. Furthermore, we quantified the expression of groEL genes under different abiotic stresses, including temperature, pH, salt and oxygen s
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