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It has long been known that native BChE is a
2020-11-17

It has long been known that native BChE is a major factor in the inactivation of cocaine, an ester-type drug of abuse [190]. But recently some researchers conceived the idea that BChE mutations could improve that function to a point that would favorably impact cocaine overdose. Rapid progress was ma
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In summary we demonstrated the high potency of fluxametamide
2020-11-17

In summary, we demonstrated the high potency of fluxametamide against M. domestica, L. striatellus, and T. urticae GABACls, which leads to high acaricidal/insecticidal effects on these arthropod pests. In contrast to its high potencies against the GABACls of arthropod pests, fluxametamide exhibited
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In ER group Histopathological examination followed by Fluore
2020-11-17

In ER + group, Histopathological examination followed by Fluorescence in situ hybridization (FISH) had revealed the absence of HER2 receptors. Co-targeting of ER and HER2 appears to provide benefit without a significant increase in toxicity although formal trials have not been carried out [18]. Adop
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There is a considerable molecular genetic heterogeneity with
2020-11-17

There is a considerable molecular genetic heterogeneity within ES/PNET. As mentioned above, either or can rearrange with in these gene fusions. Furthermore, for either gene fusion, additional heterogeneity stems from the location of the genomic breakpoints of the translocation, resulting in differen
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Previously we have shown that the overexpression of ERR
2020-11-17

Previously, we have shown that the overexpression of ERRγ induces exercise-like oxidative muscle remodeling without engaging changes in the expression level or activity of PGC1α (Narkar et al., 2011). In this study, overexpression of ERRγ in PKO muscle reveals that ERRγ-activated target genes can ac
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br Experimental procedures br Results Fluorescence attributa
2020-11-17

Experimental procedures Results Fluorescence attributable to GnRH-eGFP neurons was observed through the diagonal band of Broca, to the POA of the hypothalamus in GnRH-eGFP transgenic rats for all groups as described previously (Kato et al., 2003, Tada et al., 2013). Discussion The mEPSCs w
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Based upon these findings on portions
2020-11-17

Based upon these findings on portions A and B, novel scaffolds of EP4 antagonist, and (R & R=()-Me; =Cl; R=H), shown in , were identified. We next focused on optimizing portion C of these scaffolds. We utilized for an alternative synthesis of nicotinamide scaffold , which is quite effective for der
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br Conclusions When the authors joined the field
2020-11-16

Conclusions When the authors joined the field of oxysterol analysis around the turn of the century, oxysterols and cholestenoic acids were mostly considered as uninteresting intermediates of cholesterol metabolism. Some oxysterols had been shown to have biological activity, but the most studied o
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br Results br Discussion Many studies have shown that
2020-11-16

Results Discussion Many studies have shown that intrinsic properties of the E2 enzyme govern the nature of the Ub modification, including both the multiplicity of the Ub modification and the specific lactacystin type in the case of polyubiquitin chains [3], [4], [9], [14]. Whereas previous st
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Ubiquitination is a reversible posttranslational modificatio
2020-11-16

Ubiquitination is a reversible posttranslational modification. The removal of Ub is carried out by enzymes known as deubiquitinases (DUBs). The antagonistic role played by these enzymes in the Ub pathway regulates the function of the ubiquitinated proteins, while maintaining the free Ub pool in euka
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These data from developing brain are in contrast to
2020-11-16

These data from developing mmp endocrinology synthesis are in contrast to noradrenergic receptor regulation in the adult brain. In adult animals, a persistent increase in the α2-AR high affinity state is elicited as a result of DSP-4 lesion or reserpinization, as measured by [3H]clonidine binding t
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br Results br Discussion Prostate cancer dissemination
2020-11-16

Results Discussion Prostate cancer dissemination and skeletal metastases represent major therapeutic challenges. Once the skeletal metastasis occurs, the incurable patient could just be symptomatically treated to alleviate the pain. Therefore it is of great necessity to disclose the molecular
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We have previously reported DAPK inhibitors discovered throu
2020-11-16

We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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Instead of receptor interaction or
2020-11-16

Instead of receptor interaction or GT activity, we focused on the CPD and autoprocessing. The CPDs from the 2 toxins are highly homologous: each cysteine protease targets an intramolecular substrate and mediates InsP6-induced autoprocessing to release the GTD into host cytosol.40, 41 However, TcdB i
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In a previous study we reported
2020-11-16

In a previous study we reported that the systemic administration of the α1-adrenergic receptor antagonist prazosin attenuates the deficit in SR 1555 hydrochloride synthesis reward function associated with precipitated nicotine withdrawal (Bruijnzeel et al., 2010). One of the aims of the present expe
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