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The G R mutation is located at the solvent front
2025-02-05
The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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Introduction Aldose reductase ALR is the
2025-02-05
Introduction Aldose reductase (ALR2) is the first enzyme of the polyol pathway that catalyzes the reduction of glucose to sorbitol utilizing NADPH as a cofactor. The intracellular accumulation of sorbitol, due to increased aldose reductase activity at high blood glucose levels, such as those occurr
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Adiponectin also suppresses inflammatory stimuli induced NF
2025-02-05
Adiponectin also suppresses inflammatory stimuli-induced NF-kappaB activation, which may significantly contribute to the anti-diabetic and anti-atherogenic effects of adiponectin (Ouchi et al., 2000). The downstream mediators of AdipoR1 and AdipoR2, RPPAR and AMPK increase inflammatory responses by
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At present the role of autophagy
2025-02-03
At present, the role of autophagy in neurons remains controversial. Autophagy has homeostatic and waste-recycling functions and plays a protective role in neurodegeneration diseases. Moreover, it has been thought as a programmed cell death participating in the occurrence and development of various d
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The activity of an enzyme may
2025-02-03
The activity of an enzyme may be regulated allosterically as well as transcriptionally. We have consistently studied REMS deprivation (REMSD) associated NA mediated allosteric regulation of Na-K ATPase activity in neurons and glia in vivo and in vitro (Amar and Mallick, 2015; Amar et al., 2016; Bask
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exemplifies three of the compounds
2025-02-03
exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC Coumarin receptor as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degradation prod
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For the derivatives a c another likely explanation for antif
2025-02-03
For the derivatives 3a–3c, another likely explanation for antifungal properties is that polymers bearing primary amine groups and secondary phosphoryl groups formed, enhancing complexation with the phosphate groups, and the complexes are amphiphilic (Palermo, Lee, Ramamoorthy, & Kuroda, 2011). The a
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The mechanisms that control Ahr transcription are poorly und
2025-02-01
The mechanisms that control Ahr transcription are poorly understood, especially when considering cell type-specific regulation. A recent report suggested that the Ahr transcription might be directly promoted by RORγt [retinoic estriol receptor (RAR)-related orphan receptor γt] based on ChIP-Seq anal
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There is a growing literature
2025-02-01
There is a growing literature on ABCA2 expression in human biopsies, where it has been described as a potential biomarker of leukemias. In childhood T-cell acute lymphoblastic leukemia, ABCA2 and ABCA3 were expressed at high levels, which upon treatment with methotrexate, vinblastine and doxorubicin
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br Materials and methods br Results
2025-02-01
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 pati
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For comprehensive understanding of actin myosin XI
2025-02-01
For comprehensive understanding of actin-myosin XI as a control network, it will be necessary to determine the functions of all the myosin XI and inhibitor of apoptosis isoforms. However, it is difficult to reveal the function of individual myosin XI isoforms because most myosin XI single knockouts
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Metabotropic glutamate receptor 5 blocker The AChR is compos
2025-02-01
The AChR is composed of five homologous, membrane-spanning subunits. AChRs containing two α, one β, one δ and one γ subunit (AChRγ) predominate during embryonic development and mice lacking AChRγ die at birth (Takahashi et al., 2002). After birth, the AChRγs are replaced during the first 2 postnata
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egfr inhibitor In this study an in vitro AChE inhibition ass
2025-02-01
In this study, an in vitro AChE inhibition assay combined with UF-HPLC-ESI-Q-TOF/MS method was developed for rapid screening and identification of AChEI from the roots of C. chinensis Franch. Five compounds was found with AChE inhibitory activity and identified by the on-line DAD-ESI-Q-TOF/MS compar
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Osteocytes the most abundant cells in an
2025-02-01
Osteocytes, the most abundant cells in an adult skeleton, are essentially mature osteoblasts that are surrounded by the products they secreted (Noble and Reeve, 2000). Osteocytes serve as mechanosensors that direct bone remodeling and that regulate the activities of osteoblasts and osteoclasts (Bone
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To test the compounds metabolic stability
2025-02-01
To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structural i
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