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Herein in continuation of our
2021-06-22
Herein, in continuation of our interest in designing new DNA photocleavage agents [18], we report the synthesis, characterization and DNA binding and cleaving properties of a novel compound: trans-N,N-dimethyl-10,11-di(pyridin-4-ium)-10,11-dihydro-9,12-dioxobenzo[e]phenanthrene tetrafluoroborate (1)
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br Development of the double strand break repair model
2021-06-22
Development of the double strand break repair model for meiotic recombination Meiotic recombination was first described by Frans Alfons Janssens using namely in the salamander Batracoseps attenuatus in 1909 [21] and then further elaborated at the genetic level in Drosophila by Thomas H. Morgan [
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Compound was synthesized by the
2021-06-22
Compound () was synthesized by the directed -metallation procedure (DOM) at the stage of the amide using butyl lithium and dry ice as CO source for the introduction of the carboxylic group. Thiophene amides were prepared from commercial 3-thiophenecarboxylic opiate receptors by conversion into th
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The first example of a
2021-06-22
The first example of a broadly-acting antiviral drug is ribavirin, a nucleoside analogue that was proposed to act directly at the level of the viral polymerase, although an indirect effect via inhibition of the host-cell IMP dehydrogenase and depletion of the GTP pool seems more plausible [9]. Anoth
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Our previous studies have demonstrated that the
2021-06-22
Our previous studies have demonstrated that the DDR2 discoidin domain fully contains the binding site(s) for the fibrillar collagens I and II (Leitinger, 2003, Leitinger et al., 2004). The binding site for collagen I was mapped to three spatially adjacent surface loops within the DDR2 discoidin doma
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2-APB The lungs dissected from week
2021-06-22
The lungs dissected from 4–5-week mice were cut into small pieces and then immersed in Dulbecco's modified Eagle's medium (Invitrogen, Carlsbad, CA) containing collagenase II (2 mg/ml), trypsin (2.5 mg/ml), Dnase I (2 mg/ml), penicillin (100 U/ml), and streptomycin (100 μg/ml) for 12 hours at 37 °C
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br Results br Discussion The structures presented here were
2021-06-22
Results Discussion The structures presented here were solved at high KT 5823 mg and show in detail how DDR1 achieves high affinity for imatinib and ponatinib, respectively. Both type II inhibitors bind in their more potent extended conformations to the inactive DFG-out conformation of the kina
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Regarding the mechanism of action of CRF several studies
2021-06-22
Regarding the mechanism of action of CRF, several studies have shown that low doses of CRF may preferentially activate CRF1 receptors in glutamatergic projection neurons, serotoninergic neurons or glutamatergic collaterals in the medial prefrontal cortex (Vertes, 2004). Indeed, prosencephalic inacti
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Compound A and Compound B Fig
2021-06-22
Compound A and Compound B (Fig. 4) were found in our in vitro screening assays and have similar CRF1 receptor in vitro profiles (Table 1). When binding was investigated using [125I]-CRF in ex vivo assay, Compound A inhibited binding of [125I]-CRF both in the frontal cortex and the pituitary; however
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To the best of our knowledge this study was the
2021-06-22
To the best of our knowledge, this study was the first to demonstrate in vitro and in vivo that the lipolytic effect of kinsenoside results from coordination between PKA and AMPK pathways. We validated the lipolytic effect of kinsenoside in vivo and the effect of PKA activation on the modulating AMP
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In general up to date no study has considered
2021-06-22
In general, up to date, no study has considered thermodynamic modeling to estimate the corticosterone of SO2 by different DESs. Since experimental measurements are time consuming and expensive, general and accurate theoretical models are vital to estimate SO2 solubilities in different DESs over wid
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In conclusion the present study demonstrates that E s
2021-06-22
In conclusion, the present study demonstrates that E2's antiapoptotic effects are significantly reduced by coadministration of progestogens. The combination of E2 and progestogens resulted in diverging effects on the expressions of ERs and PRs, which induced different effects on the cell growth of M
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Targeting the MAPK pathway has attracted significant interes
2021-06-22
Targeting the MAPK pathway has attracted significant interest in cancer therapy. Efforts directly targeting RAS protein are believed to be very challenging in spite of the promise shown by a few RAS inhibitors in the early development stage. Clinical benefits achieved by BRAF and MEK inhibitors have
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br Target enzyme attributes and substrate peptide selection
2021-06-21
Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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In principle in vitro techniques
2021-06-21
In principle, in vitro techniques for assessing enzyme induction might include the use of cultured hepatocytes, precision-cut liver slices, immortalized Methyllycaconitine citrate lines (such as those derived from hepatomas) and reporter gene constructs (where appropriate cells are transfected with
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