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Introduction Diabetic nephropathy is a rapidly
2024-06-03
Introduction Diabetic nephropathy is a rapidly growing cause of end-stage renal disease [1]. Glomerular, tubular and vascular toxicity resulting from hyperglycemia (glucotoxicity) have been evaluated extensively at the molecular level as contributing factors for diabetic nephropathy [[1], [2], [3]]
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We further analyzed selected hit
2024-06-03
We further analyzed selected hit compounds for their ability to inhibit human AdK in intact cells. Human 1321N1 astrocytoma leptomycin b were utilized which were found to express AdK. The whole cell assay was performed using a 96-well format. The standard AdK inhibitor 5-iodotubercidin was employed
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br Discussion One binding site MB Fig is
2024-06-03
Discussion One binding site, MB327-1 (Fig. 4) is located in the extracellular domain between the γ and α subunits. MB327 adopts an extended conformation in the MB327-1 site and is oriented parallel to the channel. The second putative binding site, MB327-2 (Fig. 4) is situated deep inside the chan
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br Methods br Results br Discussion br
2024-06-03
Methods Results Discussion Acknowledgements This work was supported by the National Institutes of Health [Grant R21 NS081429], a Pilot Grant from the Vanderbilt Conte Center supported by the National Institutes of Health [Grant P50 M096972], and by the Department of Anesthesiology at V
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HT modulates cortical and hippocampal pyramidal cell
2024-06-03
5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal Swainsonine australia as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leise
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The synthetic route for the aminobenzoxazole scaffold with a
2024-06-03
The synthetic route for the aminobenzoxazole scaffold with a solvent accessible moiety is described in . Nitration of methoxyphenol and subsequent hydrogenation of the resulting nitro sesamin receptor afforded compound . Aminobenzoxazole was formed by the reaction of compound with BrCN in EtOH. T
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Matthew et al synthesized and carried out SAR
2024-06-03
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that E3330 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pHH3), EC50
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Expression subcellular localization transcriptional activity
2024-06-03
Expression, subcellular localization, transcriptional activity and protein stability of Foxo are regulated by proteins such as STAT3, PKB, JNK and AMPK (Sun et al., 2017; Zhang et al., 2011). STAT3 is a member of the signal transducer and activator of transcription (STAT) protein family that plays c
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br Implementation of sacubitril valsartan into clinical
2024-05-31
Implementation of sacubitril/valsartan into clinical practice Following on from the results of PARADIGM-HF, sacubitril/valsartan was given regulatory approval for use in patients who conform to the main inclusion criteria of the trial; NYHA functional class II–IV, reduced left ventricular ejectio
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The molecular mechanisms that mediate the
2024-05-31
The molecular mechanisms that mediate the plasticity of the NMJ are not well understood. PGC-1α is a master regulator of the NMJ gene expression program 23, 24, and thus AMPK might indirectly regulate the NMJ via its broad influence on the coactivator. Cerveró et al.[6] recently provided more direct
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We found that decreased Ng levels
2024-05-31
We found that decreased Ng levels lead to a lower threshold for LTD induction at L4–L2/3 synapses. Previous studies in hippocampal slice culture have shown that LTD at individual synapses induces spine elimination at both the targeted synapse and selective neighboring synapses when spines are monito
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br Possible complementarity of trimming pathways Determining
2024-05-31
Possible complementarity of trimming pathways Determining the exact pathway for the generation or destruction of MHCI peptide ligands by ERAP1 is important for our understanding of the shaping of the immunopeptidome and for designing inhibitors that can manipulate it. It is also possible however
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The literature suggests that adiponectin has a steroidogenic
2024-05-31
The literature suggests that adiponectin has a steroidogenic effect on ovarian function. In pigs, in vitro studies have shown that adiponectin reduced basal testosterone secretion in internal theca cells; in granulosa cells, it increased secretion of estradiol and, in combination with insulin, incre
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br Acknowledgments br Introduction Hypospadias is a
2024-05-31
Acknowledgments Introduction Hypospadias is a common congenital malformation in males, in which the urethral orifice is found on the ventral side of the penis as a result of incomplete fusion of urethral folds. The mean prevalence in per 10,000 live births from 1910 to 2013 were: Europe 19.9,
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Taken together BRP represents a novel chemotype of LT
2024-05-31
Taken together, BRP-187 represents a novel chemotype of LT biosynthesis inhibitors with outstanding potency in human PMNL and monocytes activated under pathophysiological relevant conditions and with effectiveness in vivo. Using the PLA that visualizes the in situ interaction between 5-LO and FLAP i
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