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Numerous epidemiological studies document fewer cardiovascul
2023-12-20
Numerous epidemiological studies document fewer cardiovascular events and increased survival of non-CKD individuals treated with angiotensin-converting enzyme inhibitors/angiotensin receptor blockers (ACEI/ARBs) [8], [9]. By contrast, there are few studies of cardiovascular benefits of interruption
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br Introduction The development and plasticity of synapses
2023-12-20
Introduction The development and plasticity of synapses involve the timely recruitment of a plethora of proteins on both pre- and postsynaptic sides through ill-defined mechanisms. At excitatory synapses, two of the major proteins that are dynamically recruited postsynaptically are the Ca2+/calmo
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Gliomas and Aldehyde Dehydrogenase Aldehyde dehydrogenases A
2023-12-20
Gliomas and Aldehyde Dehydrogenase Aldehyde dehydrogenases (ALDHs) are key metabolic enzymes involved in regulation of glycolysis/gluconeogenesis pathways as well as in the detoxification of endogenous and exogenous aldehydes, regulating cell function and homeostasis. ALDHs play important roles in
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In the late s Solvay Pharmaceuticals discontinued
2023-12-20
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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PL for actin in vitro
2023-12-20
PL for GDC-0084 in vitro showed that its profiles, including particular peak and intensity, could determine the length and thickness of an actin filament. Furthermore, we investigated if the PL intensity peak at approximately 340 nm can also be originated from another cytoskeleton filament, such as
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br Discussion Here we focused on seven plant
2023-12-19
Discussion Here, we focused on seven plant alkaloids extracted from yokukansan. These alkaloids individually inhibited 5-HT-mediated 5-HT3A and 5-HT3AB receptor currents weakly. Simultaneous administration of these alkaloids, however, inhibited the 5-HT3A and 5-HT3AB receptor currents strongly. T
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The reductase activity in patients
2023-12-19
The 5α-reductase activity in patients with 21-OHD, as assessed by the 5α-THF to 5β-THF (ratio 3) and by the 5α-17HP to 17HP (ratio 4) ratios, showed a similar pattern of activities (Fig. 2A–C) and significant correlations (ratio 1 vs. ratio 3; rs=0.67; pmenin to the 5α-reducase activity, the activit
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Drug resistance development often involves structurally un r
2023-12-19
Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 265 3 australia are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream activator of ERK1/2, assoc
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br Materials and methods br Results
2023-12-19
Materials and methods Results Discussion Author contributions JH purified protein, performed vanadate inhibition experiments, crystallized, collected data, determined and refined the ATX-VO5 structure, analysed all the structures, prepared the displayed items and supervised ALHE; WJK con
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Pyrimidine is the important pharmacology core
2023-12-19
Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the (S)-(+)-Dimethindene ma
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There are two major isoforms
2023-12-19
There are two major isoforms of 12/15-LO in mammalian, 12 and 15- LO, with different cellular distributions. To determine the relative contributions of these isoforms towards glucose-induced monocyte-endothelial interactions, the distribution of these isoforms in the two cell types involved in leuko
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br Conclusions A large body of evidence indicates
2023-12-19
Conclusions A large body of evidence indicates that oxidative stress is involved in the pathogenesis of NDDs. Hence, reducing oxidative stress or suppressing its downstream pathways may be beneficial for the treatment of these diseases, especially such chronic diseases as AD or glaucoma. Here we
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To enhance the accuracy of SEs in eliminating cancer
2023-12-19
To enhance the accuracy of SEs in eliminating cancer cells, the mAb recognized by specific Akt Inhibitor IV on tumor cells were fused with SEs. Fab C215 or C242 fused with SEA promoted apoptosis in human colon carcinoma cells via Fas (Dohlsten et al., 1994, Litton et al., 1996). SEB-incorporated ex
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The importance of insulin in
2023-12-18
The importance of insulin in controlling lipolysis and fat mass is further emphasized by mouse models with alterations in the insulin signaling pathway of adipocytes. For example, mice with a tamoxifen-inducible knockout of the insulin receptor in mature adipocytes reveal a substantial decrease of a
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br Conclusion br Conflicts of
2023-12-18
Conclusion Conflicts of interest Introduction Enzymes are widely applied as biocatalysts in fields such as synthetic chemistry [1], pharmaceuticals [2], environmental treatment [3], and food technology [4] because they can catalyze chemical transformations in a highly selective manner under
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