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To improve the preferential GalR binding we
2022-04-01

To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollenb
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Further insight in how exactly galanin might inhibit seizure
2022-04-01

Further insight in how exactly galanin might inhibit seizures was obtained from galanin transgenic mice. It occurred that the altered susceptibility to seizures was in direct correlation with glutamate release from hippocampal slices obtained from these animals (Fig. 2(b)). While no differences were
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br Material and methods br Results br Discussion Propofol
2022-04-01

Material and methods Results Discussion Propofol is commonly used in operation rooms or intensive care units (ICUs) for critically ill patients. Various clinical trials have demonstrated that the antioxidant, anti-inflammatory, and free-radical-scavenging properties of propofol can provide
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On the contrary the benzhydrol series
2022-04-01

On the contrary, the benzhydrol series showed modest activity with EC of two digit micromole. The bulkiness of the Atropine tail may be the reason for the low activity. Interestingly, introduction of H-bonding groups, such as OMe in and CF in , slightly improved the activity compared to the unsubs
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Several observations about structure activity
2022-04-01

Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic TASIN-1 class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage of
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Despite the two models for the
2022-04-01

Despite the two models for the HIV-1 IN-aptamer complexes appeared to be comparable, disintegration assays revealed that 93-del inhibited C– or N-terminally truncated enzyme at the same extent, [18] whereas, T30695 required N-terminal domain (NTD) of the enzyme to exert its integrase inhibitory acti
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AZ505 ditrifluoroacetate Hippo pathway proteins could synerg
2022-03-31

Hippo pathway proteins could synergistically regulate germ cell development with some specific receptors. Kassab et al. [27] found that epidermal growth factor (EGF) receptor was localized in testicular germ AZ505 ditrifluoroacetate and played important roles in bovine spermatogenesis. Likewise, ins
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Kinases belonging to the Thousand and one
2022-03-31

Kinases belonging to the Thousand and one (Tao) family are conserved throughout evolution. Three Tao proteins are encoded in the human genome (TAO1, TAO2, and TAO3), while D. melanogaster possesses a single ancestral Tao kinase (Tao-1). Like Hpo and GckIII, Tao kinases belong to the Sterile 20-like
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br Materials and methods br Results Heterologous
2022-03-31

Materials and methods Results Heterologous expression of P. locustae Hxk in methylotrophic yeast P. pastoris was not accompanied by nuclear localization of parasite protein (Fig. 1). The addition of leptomycin B, a specific inhibitor of nuclear export in fission yeast Schizosaccharomyces pombe
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br Conclusion The mitochondrial and glycolytic energy metabo
2022-03-31

Conclusion The mitochondrial and glycolytic energy metabolism of the brain is coordinated by HKI binding to MOM, although the molecular mechanism of such a regulation is not yet clear. The IT-901 australia for HKI in MOM are VDACs [[5], [6], [7]], mainly the VDAC1 isoform [8]. Using a computatio
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br Materials and methods br Author contributions br
2022-03-31

Materials and methods Author contributions Acknowledgments We thank members of the Skaar laboratory for critical evaluation of the manuscript. This work was supported by grants from the National Institutes of Health, R01AI069233 (EPS), and T32GM008554-21 (LJL). Introduction Pseudomonas
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According to literature RASs V
2022-03-31

According to literature, RASs V36M, T54S, Q80K and R155K are considered primary resistance mutations to different PIs. RASs V36M and R155K can reduce susceptibility to recently approved PIs simeprevir, paritaprevir and grazoprevir [18], [31], [32]. T54S is associated to resistance for first-wave tel
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PLP has been found to be effective
2022-03-31

PLP has been found to be effective inhibitor of many enzymes that have s1p receptor for phosphate-containing substrates or effectors, including RNA polymerase [14], [15], reverse transcriptase [16], and DNA polymerase [17], [18]. Oka et al. [19], [20] reported that vitamin B6 deficiency generally e
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Based on the role of
2022-03-31

Based on the role of NMDA receptors in initiation and propagation of epileptic seizures and on potentiation of NMDA function by glycine, it has been hypothesized that glycine will have proconvulsant activity (Foster and Kemp, 1989). Indeed, there is some evidence that human epileptogenic foci, remov
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GT cells were treated in two
2022-03-31

GT1-7 Barasertib were treated in two ways; specifically, they were either dosed or transfected with VP, reflecting the extracellular and intracellular actions of VP, respectively. A dose of 200 pg/ml VP in culture supernatants was effective in stimulating GnRH in the supernatant and cell extracts; t
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