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br Materials and method br Result
2024-07-04
Materials and method Result and discussion Conclusion Acknowledgments This work is partly supported by the University Research Committee (URC) of the Senate of The Federal University of Technology, Akure. The authors thanked IFS for the funds (F/4449 1F and F/4449-2F) used to purchase th
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br Actin cytoskeleton in protrusion Pushing force
2024-07-04
Actin cytoskeleton in protrusion Pushing force driving membrane protrusion is generated by polymerizing Annexin V-Cy5 Apoptosis Kit mg filaments organized either into branched networks or parallel bundles. Branched networks are assembled through Arp2/3 complex-dependent actin nucleation and drive
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Conclusion Twenty compounds with dinitrobenzoate
2024-07-04
Conclusion Twenty compounds with 3,5-dinitrobenzoate scaffold were synthesized and evaluated using cell-free and HWB assays for their 5-LOX inhibition activities. Compared to the parent compound, six compounds show significantly increased enzyme inhibition activities. The best compound, 3-tolyl 3,5
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The srd a isoforms showed unique expression profiles in earl
2024-07-04
The srd5a isoforms showed unique expression profiles in early FHM development (Fig. 2). Similar to amphibian embryos, there was a high abundance of both srd5a1 and srd5a3 at 1dpf in FHMs, suggesting that mRNA for these enzymes may be maternally deposited and that these enzymes may play a key role in
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LPA binds to six specific
2024-07-04
LPA binds to six specific cell surface GPCR receptors. The receptors LPA1 (lysophosphatidic receptor 1, formerly, Edg2), LPA2 (Edg4) and LPA3 (Edg7) belong to the endothelial differentiation gene family (EDG) and share sequence homology (50–60% amino N1-Methylguanosine-5'-Triphosphate homology) An
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Pyrimidine is the important pharmacology core in many Aurora
2024-07-03
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 nor-Binaltorphimine dih
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Phagosomes acquire some hydrolases early during their journe
2024-07-03
Phagosomes acquire some hydrolases early during their journey from the cell surface to lysosomes. An example for such hydrolase is cathepsin H which is most concentrated in the early phagosome at a pH of approximately 6.3 (Claus et al., 1998), the pH optimum of enzyme activity (Schwartz and Barrett,
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Crystal structures were obtained of sulfonamide and
2024-07-03
Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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It has been well established that shortly after systemic inf
2024-07-03
It has been well established that shortly after systemic inflammation, NADPH oxidase and iNOS activity were increased in the DC260126 and lead to overproduction of reactive oxygen species (ROS) and NO [66]. Moreover, previous studies indicated that Ang II induced an increased level of NADPH oxidase
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Recent studies revealed that certain plant
2024-07-03
Recent studies revealed that certain plant-derived compounds can also interfere with AR function. One way of such an interference is by modulating its expression levels. This is the case for the two flavonoids quercetin and luteolin that have been reported to repress the function of AR by inhibiting
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Although several ARIs have reached various phases of
2024-07-03
Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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A large number of aldose reductase
2024-07-03
A large number of aldose reductase inhibitors have been prepared synthetically, and a limited number of them are therapeutically used. However, none of them is satisfactory. Here, Cannabis extracts with high content of non-psychotropic phytocannabinoids CBD/CBDA or CBG/CBGA showed statistically sign
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Pituitary adenylate cyclase activating polypeptide PACAP is
2024-07-02
Pituitary adenylate cyclase-activating polypeptide (PACAP) is a member of the secretin/growth hormone-releasing hormone (GHRH)/vasoactive intestinal peptide (VIP) family, with potent anti-inflammatory and potent cytoprotective properties [[6], [7], [8], [9], [10], [11], [12], [13]]. PACAP exists as
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In the late s Solvay Pharmaceuticals discontinued
2024-07-02
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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PRIMA-1 sale Renal fibrosis is regarded as the final common
2024-07-02
Renal fibrosis is regarded as the final common pathway for most forms of progressive renal disease, and mouse UUO is a widely accepted experimental model of renal injury leading to extreme fibrosis localized to the interstitial compartment. A-306989 attenuated the mRNA expression levels of several k
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