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Matthew et al synthesized and carried
2023-12-13
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that peptide yy receptor 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3
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Expression subcellular localization transcriptional activity
2023-12-13
Expression, subcellular localization, transcriptional activity and protein stability of Foxo are regulated by proteins such as STAT3, PKB, JNK and AMPK (Sun et al., 2017; Zhang et al., 2011). STAT3 is a member of the signal transducer and activator of transcription (STAT) protein family that plays c
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Atglistatin br Materials and methods br Results and discussi
2023-12-13
Materials and methods Results and discussion Conclusion Funding This work was supported by the Canadian Institute of Health Research (CIHR) [grant number FDN-148413] to PS, the National Science and Engineering Research Council of Canada (NSERC) [grant number CRD-399680] to ÉM, and the FR
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The proinflammatory cytokines and chemokines including
2023-12-13
The proinflammatory cytokines and chemokines, including IL-1β, TNF-α and MCP-1, mediate acute and chronic inflammation and play a role in the development of hypertension [2, [51], [52], [53]], cardiovascular diseases [4, 54] and renal injury [55, 56] in animal models and humans. Concerning the possi
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In this study we have generated new FRET reporters to
2023-12-13
In this study, we have generated new FRET reporters to screen all submembrane domains of AT1R for interactions with CaM. We identified a new CaM-binding domain on the receptor’s SMD2 (a.a. 125 – 141), confirmed interactions at SMD4JM (a.a. 309 – 327) and characterized the full interacting domain in
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Although only Leu CysAP IRAP Herbest et al
2023-12-13
Although only Leu/CysAP (IRAP) (Herbest et al., 1997, Keller, 2004) and DPPIV (Alponti and Silveira, 2010, Kirino et al., 2009) had been identified and studied in adipocytes, our kinetic analysis suggested the highest physiological significance for AspAP (highest affinity) and APM and PSA (highest e
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We next developed a system for
2023-12-13
We next developed a system for staging severity. Our guiding principles were the following. Two types of information about the research participant are staged independently from each other: (1) grading disease severity using biomarkers and (2) grading the severity of cognitive impairment. Measures u
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OSU-03012 br Materials and methods br Results
2023-12-13
Materials and methods Results Discussion Knowledge of the molecular basis of an inherited genetic disease is crucial for understanding the disease pathology and, ultimately, for therapeutic design. Several recent reports have stressed the need for physical characterization of disease-associ
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Regarding the HT B receptors they act as terminal receptors
2023-12-13
Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT dur
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GSK2656157 For the NSCLC patients with EGFR activating mutat
2023-12-12
For the NSCLC patients with EGFR-activating mutations, EGFR-TKIs (gefitinib and erlotinib) are effective clinical therapies [21], [22]. However, approximately 10% of patients harboring EGFR-sensitizing mutations exhibit intrinsic resistance, and up to 40% do not attain a major response to treatment
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The original Aurora kinase was identified during a phenotypi
2023-12-12
The original Aurora kinase was identified during a phenotypic screen for defects in mitotic spindles in Drosophila mutants. Aurora mutants were so named because of the morphological defects at the mitotic spindle resembling the Aurora borealis, or the Northern light [4]. The structure of the Auroras
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Recent findings imply that proper Na
2023-12-12
Recent findings imply, that proper Na+/K+-ATPase function is crucial for unimpaired development of the vertebrate heart. Targeted knockout of Na+/K+-ATPase α1 in mice led to early embryonic lethality whereas heterozygous knockout mice displayed severe hypocontractile hearts [52]. Pharmacological inh
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dopamine beta hydroxylase ARG I is one of the most important
2023-12-12
ARG I is one of the most important mammalian enzymes responsible for nitrogen metabolism since it comprises the main route for the elimination of excess nitrogen resulting from amino dopamine beta hydroxylase and nucleotide metabolism [18]. ARG I deficiency leads to hyperargininemia, characterized b
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ccr2 antagonist br Implications for cancer ROS have a long
2023-12-12
Implications for cancer ROS have a long history of being involved in the development and progression of cancer and increased ROS level is considered as a hallmark of many tumors [76], [77]. Initially, it was thought that ROS would serve as chemical mutagens that would indiscriminately damage cell
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Limitations of this study include the use of HL cardiomyocyt
2023-12-12
Limitations of this study include the use of HL-1 cardiomyocytes, which show different characteristics than primary cardiomyocytes [56]. Furthermore, sustained TAC in Ampkα1-deficient mice did not favorably influence cardiac function [33]. It must be kept in mind that global Ampkα1-deficiency may af
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