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Despite these data implicating Kdm b as a positive
2021-10-12
Despite these data implicating Kdm6b as a positive regulator of neuronal differentiation, and surprisingly, given the evidence that germline knockouts die perinatally due to an inability to breathe, the brains of Kdm6b knockout mice are remarkably normal in gross morphology [26,]. Interestingly, Kdm
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br Acknowledgements This work was supported by grants
2021-10-12
Acknowledgements This work was supported by grants from the Agencia Nacional de Promoción Científica y Tecnológica (PICT2013-0495, PICT2016-1821), and from CONICET (PIP 2013-562), as well as from Fundación René Barón and Fundación Williams. Introduction Histamine poisoning, also known as scom
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En el caso de la foliculitis decalvante FD se ha
2021-10-12
En el caso de la foliculitis decalvante (FD), se ha publicado un estudio multicéntrico español de 82 pacientes en el que se concluye que el tratamiento que consigue una mayor efectividad (mejora en 15/15 pacientes tratados) y un mayor periodo de remisión postratamiento (7,2 meses) es la combinación
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The synthesis of nitropyrimidine analogs was outlined
2021-10-12
The synthesis of 5-nitropyrimidine analogs – was outlined in . 4,6-Dichloro-5-nitropyrimidine, 4-methylsulfonylaniline and 2-fluoro-4-methylsulfonylaniline were prepared according to previously reported procedures., , Reaction of 4,6-dichloro-5-nitropyrimidine and substituted aniline in DMF yielded
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In summary we discovered azaindole substituted
2021-10-12
In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that
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We next compared the enhancing effects
2021-10-12
We next compared the enhancing effects of 100nM zinc on currents produced by a low concentration of glycine with zinc effects on the same currents produced by the partial agonist taurine. In this experiment, zinc was co-applied with concentrations of glycine or taurine producing 5–10% of the maximal
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br NMDA receptor LBDs The study of GluA
2021-10-12
NMDA receptor LBDs The study of GluA2 was later expanded to include NMDA receptors [22]. NMDA receptors are obligate heterotetramers that are composed of two glutamate-binding subunits and two glycine-, or d-serine-, binding subunits. In this study, crystal structures of the NMDA receptor glycine
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Next we asked how a common
2021-10-11
Next, we asked how a common activation marker of fibroblasts, Acta2, defined gene expression signatures in alveolar airspaces by using Acta2-mKO1 reporter mice (Fig. 2A). In the lungs of Acta2-mKO1 mice, mKO1 was expressed in smooth muscle cells and mesenchymal cells in betaxolol (Fig. 2B). By sort
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In Gallus gallus four FGFRs FGFR have been
2021-10-11
In Gallus gallus, four FGFRs (FGFR1-4) have been identified, along with 13 FGFs (FGF1–4, 8–10, 12, 13, 16, 18–20) (Thisse and Thisse, 2005). FGFRs are tyrosine kinase receptors that contain an extracellular ligand binding domain, a transmembrane domain and an intracellular tyrosine kinase domain. Th
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The suboptimal trypsin selectivity profile
2021-10-11
The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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Octreotide acetate KDM D also known as
2021-10-11
KDM5D (also known as JARID1D or SMCY) is encoded on the Y chromosome and until now it has been implicated in prostate cancer invasion and metastasis [42], spermatogenesis [43], and sex-specific tissue transplantation rejection [44]. KDM5D acts as a direct epigenetic modulator, and as one of the four
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In cancer cells HIF upregulates HK II expression by
2021-10-11
In cancer cells, HIF-1α upregulates HK-II expression by binding to the hypoxia-responsive element in the HK-II promoter region to adapt to hypoxic conditions [20]. In the present study, we observed that mangiferin transiently increased HIF-1α expression in endothelial cells, suggesting another possi
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On the basis of the structure of
2021-10-11
On the basis of the structure of the Rab35/ACAP2 complex, the authors identified Thr76 in switch II of Rab35 as one key specificity determinant (Lin et al., 2019). The crystal structure shows that the hydroxyl group of Thr76 forms a angiotensin 1 with Asp756 in ACAP2, while the methyl group is a par
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Various inhibitors have been developed to target
2021-10-11
Various inhibitors have been developed to target molecules present in these pathways. They include both man-made monoclonal Arecaidine but-2-ynyl ester tosylate as well as small molecule membrane permeable inhibitors that often target kinases or phosphatases [5], [338], [348], [364]. In summary, th
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Lipid sensing GPCRs as therapeutic targets G
2021-10-11
Lipid-sensing GPCRs as therapeutic targets G-protein-coupled receptors (GPCRs) comprise a family of cell-surface receptors that respond to various extracellular stimuli such as light, odorants, neurotransmitters and hormones, and trigger a cascade of intracellular signaling. There are approximately
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