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In conclusion we have demonstrated that diaryl pyrazolo pyri
2024-09-18
In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi
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The bovine Ack is called Ack bAck and has
2024-09-18
The bovine Ack is called Ack2 (bAck2) and has been suggested to act as a clathrin-assembly protein regulated by the small GTPase Cdc42 [17]. bAck2 lacks some of the C-terminal parts when compared to hAck1 and mAck1. Both Ack1 and Ack2 have been demonstrated to interact with sorting nexin 9 (SNX9 or
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br Methods br Transparency document
2024-09-18
Methods Transparency document Introduction Epinephrine (EP) is a critical hormone and catecholamine neurotransmitter in nervous system of mammals.1, 2, 3 It has been known to accelerate and regulate heartbeat, blood pressure, bronchodilation, mydriasis, blood sugar and lipolysis, and can he
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Macrophage polarization is linked to activation of the ligan
2024-09-18
Macrophage polarization is linked to activation of the ligand-dependent transcription factor PPARγ. Recently, Odegaard et al. demonstrated with a macrophage-specific deletion of PPARγ in mice that alternative macrophage activation is impaired [14]. We provided evidence that contact to apoptotic cno
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br Materials and methods br Results and discussion In our
2024-09-18
Materials and methods Results and discussion In our previous studies (Matarneh et al., 2017), mitochondria were mechanically disrupted and separated into supernatant and pellet fractions by centrifugation. The causative agent for enhnced glycolytic flux was shown to be a protein that resides i
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In liver the essential organ of lipoprotein synthesis
2024-09-18
In liver, the essential organ of lipoprotein synthesis, ACL plays a fundamental role in lipogenesis and steroidogenesis by supplying cytosolic NSC 74859 to both pathways. By using a tricarboxylic acid cycle intermediate (citrate) to produce acetyl CoA, ACL can be seen as an important bridge between
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In clinical studies BA has
2024-09-18
In clinical studies, BA has been reported to promote dose-dependent LDL-C lowering effects of up to 30% as monotherapy, and up to an additional 24% when added in combination with stable statin therapy, or approximately 50% when combined with ezetimibe 109, 110, 111, 112. These effects were accompani
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br Apelin Discovered in apelin was initially identified as
2024-09-14
Apelin Discovered in 1998, apelin was initially identified as the sole endogenous ligand for the APJ receptor (Tatemoto et al., 1998). Apelin-77 (pre-pro-apelin) is the precursor for various pharmacologically active apelin isoforms (e.g. apelin-12, -13, -17 and 36), and it shares 75–95% sequence
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We subsequently performed immunohistochemistry on
2024-09-14
We subsequently performed immunohistochemistry on sections obtained from mice at 16 weeks after surgery. Type II collagen expression was detected in all articular cartilage zones, but was weak in the upper zone in the vehicle-treated group. MMP-13 and type X collagen expression were increased in the
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The Irbesartan Diabetic Nephropathy Trial
2024-09-14
The Irbesartan Diabetic Nephropathy Trial enrolled patients with type 2 diabetes, proteinuria of at least 0.9 g/24 h, BP >135/85 mmHg and moderate kidney impairment (creatinine 88 to 265 µmol/L in women or 106 to 265 µmol/L in men). Patients were randomized to receive irbesartan (titrated from 75 to
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The findings from our previous
2024-09-14
The findings from our previous study indicate that mitochondrial biogenesis of astrocytes is increased under experimental septic condition [25]. Recent studies have shown that IL-6 can activate AMPK by increasing the concentration of AMP [26], while AMPK regulates mitochondrial biogenesis and autoph
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br Discussion In a series
2024-09-14
Discussion In a series of linear mixed effects models of longitudinal neuroanatomical change, we have identified genetic risk variants associated with an increase in chk1 inhibitor shape asymmetry in AD. The closest genes associated with significant SNPs include BIN1 (rs6733839), CD2AP (rs1094836
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The PAS domains of AHR consist of two
2024-09-14
The PAS domains of AHR consist of two regions, PAS-A and PAS-B, which function as interfaces for dimerization with ARNT and for ligand binding, respectively [14]. Although both the bHLH and the PAS-A domains have been shown to be involved in dimerization with ARNT, a recent report suggests that only
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Altogether the situations described above clearly
2024-09-13
Altogether, the situations described above clearly impede the critical steps of drug discovery and development and the scientific process in general [14]. In conclusion, it is the opinion of these authors that many exciting lines of drug discovery (which includes those devoted to nAChR ligands) have
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In most industrial areas which are in need of treatment
2024-09-13
In most industrial areas which are in need of treatment, there are mixtures of different contaminants at different concentrations in soil, underground water or wastewater. These hazardous wastes include a variety of salts, organic matter, heavy metals, trace elements and radioactive compounds [5].Si
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