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These mutations induce the gene auto activation
2025-02-19
These mutations induce the gene auto-activation in 10–40% of adenocarcinomas, triggering the EGFR-signaling pathway in the absence of ligand. That leads to an uncontrolled acceleration of cell proliferation, survival and anti-apoptotic signals (Couraud et al., 2012). The frequency of these mutations
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To guide our attempts at achieving AKT potency and
2025-02-19
To guide our attempts at achieving AKT potency and selectivity against p70S6K and other kinases from (p70 S6K IC: 0.004 μM) and , we took advantage of exploiting the subtle sequence differences in the active sites of the AGC family kinases, we utilized the information around crystal structure of AK
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Our studies suggest that AdipoR and AdipoR genes
2025-02-19
Our studies suggest that AdipoR1 and AdipoR2 genes are expressed in multiple tissues in the chicken wherein both receptors are likely to mediate the physiological effects of adiponectin. We determined the relative expression of AdipoR1 and AdipoR2 mRNA in various tissues and found that skeletal musc
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Introduction Adenosine monophosphate cAMP is a general purpo
2025-02-19
Introduction Adenosine 3′,5′-monophosphate (cAMP) is a general-purpose signaling molecule present in most branches of life. Intracellular cAMP levels control diverse cellular functions. In bacteria, cAMP regulates metabolism by activation of the catabolite activator protein (CAP), also known as cAM
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br Materials and methods br Results br
2025-02-19
Materials and methods Results Discussions Diabetes is mainly divided into Type 1 diabetes and Type 2 diabetes [16]. Type 2 diabetes, featured by insulin resistance, results from environmental factors and poor eating habits [2]. Type 2 diabetes accounts for more than 95% of the diabetic pat
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br Conflicts of interest br Introduction Phosphatidic acid p
2025-02-18
Conflicts of interest Introduction Phosphatidic ace inhibitors phosphatase (PAP) enzymes are responsible for catalyzing the reaction that dephosphorylates phosphatidic acid (PA), which in turn produces diacylglycerol (DAG) and a phosphate group during phospholipid regulation (Fig. 1A) [1]. Su
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Enhanced GFP mRNA Protein phosphorylation is an important po
2025-02-18
Protein phosphorylation is an important posttranslational mechanism for the regulation of distribution, trafficking, and function of modified proteins (Wang et al., 2014). GluA1 phosphorylation at S845 also has functional consequences (Lu and Roche, 2012). For instance, S845 phosphorylation drove tr
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A third motif involves the
2025-02-18
A third motif involves the toggle switch and consists of the conserved FxxCWxP sequence in TM6 of class A GPCRs (Hofmann et al., 2009, Rosenbaum et al., 2009). Rotamerization of Trp in combination with a kink caused by Pro facilitates the outward movement of TM6 upon activation (Hofmann et al., 2009
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Sorafenib was the first small RTK inhibitor drug to be
2025-02-18
Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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The specific mechanism and neurotoxic
2025-02-18
The specific mechanism and neurotoxic Aβ Cytidine 5-triphosphate are yet to be elucidated, however recent studies have provided significant evidence for the amyloid channel hypothesis. These reports have established that relatively small oligomers ( Conflict of interest Acknowledgements This wo
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EGFR L858R mutation br Material and methods br Results br Di
2025-02-18
Material and methods Results Discussion Nimodipine administration inhibited the level of AMP-activated protein kinase (AMPK) phosphorylation, a sensor of cellular energy status that directs metabolic EGFR L858R mutation to support cellular growth and survival. CCH influences the oxygen and
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VRT752271 br Conflict of interest statement br Introduction
2025-02-18
Conflict of interest statement Introduction Tanshinone IIA (Tan IIA) is a major active component of Salvia miltiorrhiza (S. miltiorrhiza), a well-known Chinese traditional medicine that is used for the treatment of cardiovascular and cerebrovascular diseases [1]. Tan IIA exhibits diverse pharm
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The glutamate receptors are important
2025-02-18
The glutamate receptors are important to the glioma RN 1734 mg from escaping the excitotoxicity under physiological conditions. There are three subtypes of ionotropic glutamate receptors, including NMDA, kainate, and AMPA receptors, which are relating to diverse Ca2+ permeability. Glioma cells also
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Previous studies have demonstrated that synaptic AMPARs
2025-02-18
Previous studies have demonstrated that synaptic AMPARs can differ greatly in their mobility; some rapidly and constitutively S1RA receptor in and out of the synaptic membrane, while others remain somewhat stable in the synaptic membrane (Luscher et al., 1999, Luthi et al., 1999). We find that mGluR
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br Conclusion We have identified three non competitive inhib
2025-02-18
Conclusion We have identified three non-competitive inhibitors of the human and porcine APN with Ki values in the μM range, by combining virtual screening and kinetic assays. Molecular docking simulations suggest these novel inhibitors block APN activity by an alternative mechanism to Zn coordina
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