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The CRTH inhibitory activities of the synthesized compounds
2020-07-08

The CRTH2 inhibitory activities of the synthesized compounds are listed in , . At first we introduced halogen or other substituents at the 4,4′-position of phenyl rings in the benzhydryl moiety in order to obtain SAR and to improve the metabolic stability at this moiety (–). It is well-known that in
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Unexpectedly CRF receptor agonist and antagonist evoked simi
2020-07-08

Unexpectedly, CRF2 receptor agonist and antagonist evoked similar effects in the fall in tail skin temperature caused by restraint. However, Ucn3 reduced basal values of tail skin temperature, thus indicating that some degree of basal vasoconstriction caused by BNST treatment with Ucn3 may have cont
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Many studies have also demonstrated that CK inhibition profo
2020-07-08

Many studies have also demonstrated that CK2 inhibition profoundly affects the PI3K/AKT pathway in different cancer models; promising results have been obtained in hematological malignancies (Buontempo et al., 2014, Borgo et al., 2013, Piazza et al., 2012, Cheong et al., 2010, Gowda et al., 2016), a
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The oxidation of the lipid fraction of meat
2020-07-08

The oxidation of the lipid fraction of meat is an extremely complex process because of the high sensitivity of oxidation products to decomposition, their reactions with other components, the complex effect of catalysts and the presence of antioxidants. These changes are the main cause of limited she
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br Discussion The use of carp primary cell
2020-07-08

Discussion The use of carp primary cell cultures proved to be a valuable approach to evaluate the piscine immune response. A. hydrophila was a more potent stimulator of NO formation by carp leukocytes compared to commercial LPS often used for leukocyte stimulation (Mustafa and Olson, 1998, Chao e
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We hypothesize that both IGF dependent kinase activation
2020-07-08

We hypothesize that both IGF-1-dependent kinase activation and locally synthesized neuroestrogens interactively regulate estrogen receptor activity in neuronal Fmoc-Cl synthesis in the absence of exogenously applied estradiol. The Neuro-2A cell line was chosen as the model system for these studies
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br Acknowledgments We are thankful to the University of Guil
2020-07-08

Acknowledgments We are thankful to the University of Guilan Research Council for partial support of this work. Introduction It is significant to predict the mass, number and velocity distribution of BAD generated by RHA subjected to penetration of EFP by the thickness of target and the impact
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Although MMP might be a downstream target of Src kinase
2020-07-08

Although MMP-9 might be a downstream target of Src kinase signaling (Liu and Sharp, 2011), a direct connection has not been established. We showed for the first time that, in the collagenase-induced ICH model, Src kinase signaling regulates MMP-9 activity and mediates EP1R toxicity. Consistent with
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br Material and methods br Results and discussion br Conclus
2020-07-08

Material and methods Results and discussion Conclusion The gene encoding the Bos taurus muscle enolase enzyme was successfully isolated and cloned in this study. Optimization of the cloning, gene Santacruzamate A and purification was performed and protein elution at 95% purity was achieved
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To develop antagonists selective for the mouse
2020-07-07

To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic loteprednol () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable aldehyde
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N Cyclopentylmethyl analog exhibited fold
2020-07-07

N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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The majority of serpins inhibit serine
2020-07-07

The majority of serpins inhibit serine proteases, but serpins that inhibit caspases or papain-like cysteine proteases have also been identified [4], [5]. Inhibitory serpins are ‘suicide’ or ‘single use’ inhibitors that use a unique conformational change to inhibit proteases. This conformational tran
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The synthesis of compounds a and b are outlined in
2020-07-07

The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of 99 0 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and 7b were obtain
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Elevation of plasma glucocorticoids as well
2020-07-07

Elevation of plasma glucocorticoids as well as a sympathetic activation are highly adaptive mechanisms allowing the individual to cope in various situations [39]. Novelty-induced increase in locomotor activity, characterizing the bold fish herein, accompanied by elevated glucocorticoids is a well-es
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br Experimental methods br Results and
2020-07-07

Experimental methods Results and discussion Conclusion Rational design of highly selective fluorescent probes to detect G-quadruplexes is of profound importance for basic research. On this basis, we designed and synthesized a series of N-alkylated styrylquinolinium dyes Ls-1, Ls-2 and Ls-3.
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