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br Acknowledgements br Introduction Resistant
2023-10-18
Acknowledgements Introduction Resistant hypertension (RH), is defined as blood pressure (BP) > 140/90 mm Hg despite three full doses antihypertensive drugs including a diuretic. Controlled hypertensive patients taking four kras-pdeδ inhibitor or more of antihypertensives are also considered re
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On another hand pyrazoles are widely found as the
2023-10-18
On another hand, pyrazoles, are widely found as the core structure in a large variety of compounds of great biological and pharmaceutical value exhibiting anti-HCV [11], antitumor [12], cytotoxic[13], and antioxidant activities [14]. Finally, 1,2,3-triazoles have attracted the interest of medicinal
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In this study in an effort to explore the possible
2023-10-18
In this study, in an effort to explore the possible role of 5-HT6 receptors in mediating the memory-enhancing effects of YL-0919, we first assessed the memory-enhancing effects of YL-0919 in the Morris water maze, object recognition test and step-down passive avoidance task. In addition, we then inv
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br Roles of apelin and APJ in cardiovascular
2023-10-18
Roles of apelin and APJ in cardiovascular diseases Therapeutic potential of apelin/APJ in cardiovascular diseases Since the apelin/APJ system plays a key role in the occurrence and development of cardiovascular diseases, it seems logical to presume that targeting this axis should be feasible a
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HMGN proteins are subject to extensive post translational mo
2023-10-17
HMGN proteins are subject to extensive post-translational modifications which influence both their mode of binding to Alda 1 and their functional activity. Like the other HMG protein families, HMGNs are substrates for many of the same enzymes that modify histone proteins (review in [175]). The hist
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Atovaquone br Results and discussion This paper reports the
2023-10-17
Results and discussion This paper reports the synthesis of methoxy and 4-thio derivatives of quercetin and luteolin, which includes two new derivatives (4 and 12) and explores how subtle variations in the chemical structure of flavonoids affect their biological activity, particularly in relation
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However in recent years advanced
2023-10-17
However, in recent years advanced experiments and findings are emerging to give us more detailed information on Aβ-membrane interactions. Several reviews have provided background on the fibrillation of Aβ and the Aβ-membrane interactions [[18], [19], [20], [21], [22]]. In this review, we mainly focu
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The relationship between AG and
2023-10-17
The relationship between AG and tau deposition in the presence of Aβ burden warrants more research in AD and in other primary tauopathies (not associated with accumulation of Aβ plaques). Our findings highlight the importance of measuring AG, as this relationship was not evident for total Plumbagin
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For the first series we decided to verify the
2023-10-17
For the first series we decided to verify the effects induced, on the ALR2 inhibitory properties, of an additional steric hindrance on the carbon in α position with respect to the carboxylic group, by introducing a methyl group (R2=Me). Therefore, we synthesized a series of new α-alanine derivatives
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br Author contributions br Acknowledgements We thank Dr Bob
2023-10-17
Author contributions Acknowledgements We thank Dr. Bob Hammer and the Transgenic Core Facility at UTSW for the generation of the transgenic lines, John Shelton and the Histology Core for assistance with histology and the UTSW Metabolic Core Unit for help in phenotyping. We acknowledge support
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br AMPK structure and mechanism of action AMPK
2023-10-17
AMPK: structure and mechanism of action AMPK is a metabolic master switch that regulates downstream signals based on shifts in the surrounding energy reservoir [6]. It is expressed in a number of tissues, including the kidney, the liver, the skeletal muscle, the adipose tissue, and the hypothalam
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In terms of the ring B C position while C
2023-10-17
In terms of the ring B C5′ position, while C5′-F (compound ) was tolerated, C5′-Me (compound ) and C5′-Cl (compound ) substitutions resulted in a loss in potency. However, the C5′-OMe substitution (compound ) resulted in a ∼3-fold increase in potency compared to . Modeling suggested a pseudo hydroge
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Here we show that the co activation of RTKs and
2023-10-17
Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC SGI-1027 and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhibitor TPX-0005
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The original Aurora kinase was identified during a phenotypi
2023-10-17
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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br Synthetic lethal approaches In addition to the potential
2023-10-17
Synthetic lethal approaches In addition to the potential utility of ATM and ATR as chemo- or radiosensitisers, recent studies suggest that such compounds may have single agent activity in certain subsets of patients through induction of synthetic lethality. Two genes are considered synthetically
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