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As described above we designed
2020-06-29

As described above, we designed and synthesized a new 1,4-di-substituted isoquinoline lead compound, and was identified as a ligand with moderate potency for the CRTH2 receptor. We initially we examined the effects of the steric factor of R group on the CRTH2 binding potency (). When the methyl gro
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Taken together our results demonstrate that
2020-06-29

Taken together, our results demonstrate that the changes of striatal dopamine release and locomotor activity observed following chronic nicotine treatment and consequent acute withdrawal are mediated by CRF1, but not CRF2. Previous studies have already indicated that blocking CRF1 would prevent some
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Some of the psychoactive actions of nicotine are
2020-06-29

Some of the psychoactive actions of nicotine are mediated by the nigrostriatal and mesolimbic pathways (Di Chiara, 2000, Di Chiara et al., 2004). The nigrostriatal pathway originates in the dopaminergic neurons located in the substantia nigra and terminates in the putamen and nucleus caudatus which
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In this study we characterized the metabolic function
2020-06-29

In this study, we characterized the metabolic function of tra2 in the Drosophila fat body. Similar to the 9G8 phenotype, decreasing tra2 levels in the Drosophila fat body using RNAi resulted in increased starvation resistance and a large increase in triglycerides. This increased storage of triglycer
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Coumarins also known as benzopyran ones are a
2020-06-29

Coumarins also known as benzopyran-2-ones are a family of nature-occurring lactones first isolated from Tonka beans in 1820. They are an important class of oxygen containing heterocycles widely found in nature, so much so that they have been routinely employed as herbal remedies since early days. Ov
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br Experimental br Declaration of interest
2020-06-29

Experimental Declaration of interest Introduction Material and methods Results and discussion Conclusion By screening the NMR β(1,3)-d-glucan synthase library an initial hit was found for an inhibitor of the PPI between the α-β subunits of CK2 with an IC50 of 900 μM. This compound
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endothelin receptor antagonist br Iterative design approach
2020-06-29

Iterative design approach overview An iterative design strategy is used to identify a peptidase-resistant reporter that acts as an efficient substrate for kinases in cell lysates as well as intact cells (Fig. 1). In this process, small-scale, rationally designed libraries are used to screen pepti
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Just as Dorin et al
2020-06-29

Just as Dorin et al. [2] and Nguyen et al. [3] write in regard to their models, our static model can be used to estimate the affinities of Deoxynivalenol to albumin and CBG. Dorin et al. [2] estimates the K, but not K, since they find that their model is not particular sensitive towards changes in
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The chemical structures of I
2020-06-29

The chemical structures of I3C, 3MOI, and 3MI and the allopurinol zyloprim australia responsible for 3MI metabolism in rainbow trout and carp are shown in Fig. 4. Discussion To determine the individual CYP450 isoforms involved in 3MI metabolism, we used specific inhibitors for CYP1A, CYP3A and
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The findings of Qiu et al
2020-06-29

The findings of Qiu et al. (2016) represent the first instance of a Ub-specific mono-ADP-ribosyltransferase, as well as the first documentation of E1/E2 independent ubiquitination. Post-translational modification of Ub certainly adds layers of complexity to our understanding of the Ub signal and sho
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Several functions of FAT have been suggested It
2020-06-29

Several functions of FAT10 have been suggested. It has been shown that FAT10 binds noncovalently to the mitotic spindle checkpoint protein MAD2 and that this binding might cause chromosome instability in the cancer Cilengitide overexpressing FAT10 (Liu et al., 1999, Ren et al., 2006). In other stud
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Ginsenoside Re lysine mixture had increased
2020-06-29

Ginsenoside Re-lysine mixture had increased anticancer effects upon heat processing by regulating Bcl-2 and Bax (Yamabe et al., 2013). Ginsenoside Re (20mg/kg) inhibited NF-κB activation by inhibiting LPS binding to TLR4 on macrophages in TNBS-treated mice (Lee, Hyam, Jang, Han, & Kim, 2012). The ch
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br A brief introduction to DUBs The reversal of
2020-06-29

A brief introduction to DUBs The reversal of ubiquitin conjugation of targeted proteins relies on deubiquitinating G-36 australia (DUBs), which catalytically cleave single Ub or poly-ubiquitin chains from proteins. The human genome encodes approximately 100 potential DUBs which can be classified
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2 deoxyglucose Over the past decade targeting DNA repair pro
2020-06-29

Over the past decade, targeting DNA repair proteins has emerged as an effective tool to enhance chemosensitivity of malignant cells [9]. However, identification and selection of the proper target of DNA repair pathways is critical to increase cytotoxic activity of chemotherapeutic agents in cancer c
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br Introduction In mammals there are ten known isoforms
2020-06-29

Introduction In mammals there are ten known isoforms of the enzyme diacylglycerol kinase (DGK), as well as gene splice variants. Enzymes of this family all have a homologous active site but differ widely in their molecular mass, mechanisms of activation and biological function (Shulga et al., 201
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