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Meropenem The benzimidazole group seems to be a key feature
2023-12-18
The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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br Clinical realities br Commentary on uses of
2023-12-18
Clinical realities Commentary on uses of selective 17,20 lyase inhibitors If continued monitoring of these same parameters along with tracking of circulating ACTH in human trials confirms these new drugs are the long sought after 17,20 lyase inhibitors, then we may for the first time be able t
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br The embryological and physiological roles of ATX
2023-12-18
The embryological and physiological roles of ATX ATX is a vital enzyme that is needed for early embryological development. ATX knockout (KO) (ENPP2−/−) embryos die in utero on average at day 9.5 with vascular and neural tube defects [30], [73], [74], [75]. In these mice, malformations in the alla
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Further analysis sought to understand the
2023-12-18
Further analysis sought to understand the mechanism associated with the autotaxin-mediated increase of miR-489-3p in circulation. Based upon sequence complementarity, DIANA TarBase predicted miR-489-3p targets MAPK2K1, or MEK1, an oncogene widely dysregulated in cancer (Fig. 4A). To test this relati
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3-Chlorotyrosine sale Phosphoinositide kinase PI K Akt has
2023-12-18
Phosphoinositide 3-kinase (PI3K)/Akt has been well demonstrated in the protection of myocardial cell against IR injury via increasing cardiomyocyte survival, inhibiting excessive autophagy, et al. (Kong et al., 2016). The 3-Chlorotyrosine sale of ERK1/2 also involves in the regulation of cardiac myo
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Fmoc-Gly-OPfp receptor Having demonstrated that Gq coupled m
2023-12-18
Having demonstrated that Gq-coupled mGluR1a was necessary for estradiol-induced enhancement of CREB phosphorylation, we hypothesized that activation of a separate G-protein signaling pathway could explain the effect of estradiol on L-type calcium channel signaling (Boulware et al., 2005). Indeed, in
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The mitogen activated protein kinase MAPK plays
2023-12-18
The mitogen-activated protein kinase (MAPK) plays an important role in a variety of cell processes by controlling transcriptional or translational regulation [14]. There are three major MAPK family members that have been well characterized: extracellular signal-regulated kinase (ERK), c-Jun N-termin
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In glucose stimulated pancreatic cells B Raf activity is inc
2023-12-18
In glucose-stimulated pancreatic β-cells, B-Raf activity is increased, while Raf-1 activity is under the detection limit (Duan and Cobb, 2010). Thus, B-Raf is the primary protein kinase involved in the rapid activation of ERK1/2 in glucose-treated pancreatic β-cells. Expression of a dominant-negativ
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semagacestat Previous studies demonstrate that chiral bioint
2023-12-18
Previous studies demonstrate that chiral biointerface has great influence on cells adhesion and proteins adsorption [39], [40], [41], [42], [43], which inspired us to further develop antimicrobial materials or surfaces by taking advantage of the “chiral taste” of microbes. L-borneol is a hydrophobic
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br Angiogenesis as a critical event
2023-12-18
Angiogenesis as a critical event in diabetic retinopathy Angiogenesis refers to the abnormal proliferation of blood vessels during various pathological conditions. It acquires the stature of being one of the most detrimental events responsible for the progression of diabetic retinopathy. Angiogen
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br Introduction Clinical manifestations of Alzheimer s disea
2023-12-16
Introduction Clinical manifestations of Alzheimer's disease (AD) are mainly characterized by progressive intellectual deterioration, memory impairment, cognitive impairment, and psychiatric symptoms. The pathogenesis of AD remains unclear, mainly containing genetic factors, neurotransmitter disor
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LY364947 br Perspectives and challenges Previously the
2023-12-16
Perspectives and challenges Previously, the main focus of development of adenosine targets for pain was on A1Rs, due to prominent antinociception in multiple preclinical models and preliminary observations in human trials. However, delivery of agonists can be limited by other (e.g. cardiovascular
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To date more than different
2023-12-16
To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su
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Brain damage diseases such as cerebral ischemia
2023-12-16
Brain damage diseases, such as cerebral ischemia, brain trauma and infection are characterized by the increase in oxygen free radicals. Therefore, deeper understanding of the character and mechanism of free radical damage in the brain is important to ultimately relieve diseases and promote recovery
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The take home message here is that although Aurora
2023-12-16
The take-home message here is that, although Aurora A phosphorylated on T288 is the activated isoform of Aurora A, measuring the level of phosphorylation of T288 does not reflect Aurora A kinase activity (Figure 5). What would be the most appropriate readout for an in vivo Aurora A kinase activity
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