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br Experimental section br Acknowledgments br Introduction A
2024-01-03

Experimental section Acknowledgments Introduction Adipose is a major endocrine organ which releases a range of bioactive agents [1]. Selected adipose depots have been established as sites of sex steroid metabolism [1]. Subcutaneous and visceral adipose express high levels of aromatase, cap
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To further investigate the role
2024-01-03

To further investigate the role of cholesterol in the Rh2-induced cytotoxicity, we then focused on the U937 cell line, which is cholesterol auxotroph and considered as a valuable model to study the importance of cholesterol in membrane structure and function (Billheimer et al., 1987), and used the e
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To further address the mechanism of Didox s suppressive
2024-01-03

To further address the mechanism of Didox’s suppressive effects on mast cell activation, FceRI receptor ekb mg and downstream transcription factor induction were assessed. We found that Didox had no effect on FceRI surface expression, and thus concluded that Didox effects must be occurring downstre
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Perhaps the first evidence of AMPKs
2024-01-03

Perhaps the first evidence of AMPKs therapeutic ability in DM1 came from Thomas Cooper’s laboratory where they demonstrated that insulin-independent glucose uptake was unaffected in human DM1 muscle γ-Linolenic Acid methyl ester treated with MET, an AMPK activator and first-line therapy for type 2 d
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Several enzymes in serine and
2024-01-03

Several enzymes in serine and glycine metabolism have been proposed as biomarkers for cancer stage and prognosis. Phosphoglycerate dehydrogenase (PHGDH), phosphoserine phosphatase (PSPH), and serine hydroxymethyltransferase (SHMT) levels are high in TNBC and low in luminal-A breast cancers (Kim et a
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endothelin receptor antagonist Aldose reductase ALR EC the f
2024-01-03

Aldose reductase (ALR2, EC1.1.1.21), the first enzyme in the polyol pathway, is a monomeric oxidoreductase that catalyses the NADPH-dependent reduction of a wide variety of carbonyl compounds, especially glucose. In this metabolism pathway, glucose is firstly reduced to sorbitol catalyzed by ALR2 wi
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For the first series we decided
2024-01-03

For the first series we decided to verify the effects induced, on the ALR2 inhibitory properties, of an additional steric hindrance on the carbon in α position with respect to the carboxylic group, by introducing a methyl group (R2=Me). Therefore, we synthesized a series of new α-alanine derivatives
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br Introduction Nausea and vomiting are
2024-01-03

Introduction Nausea and vomiting are among the most distressing side effects associated with chemotherapy in cancer patients (Billio et al., 2010). Severe emesis can negatively affect a patient's nutritional state, ability to work and motivation, which can, in turn, interfere with the clinical co
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The assay performance was estimated using
2024-01-03

The assay performance was estimated using Z′-factors (plotted in Fig. 2A) according to Zhang et al. calculated for each plate comparing positive (in the absence of an inhibitor) and negative controls (in the presence of an AdK inhibitor). The mean Z′-factor±SD was determined to be 0.7±0.1, indicativ
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Previously we described that cadmium induces a more pronounc
2024-01-03

Previously, we described that cadmium induces a more pronounced, but not selective, cell death on primary cholinergic neurons from basal forebrain (Del Pino et al., 2014). Degeneration of septal cholinergic neurons from basal forebrain, as happens in AD, results in memory deficits (Scheiderer et al.
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AXL is a member of the TAM Tyro
2024-01-02

AXL is a member of the TAM (Tyro3, Axl, Mer) family of receptor tyrosine kinases (RTKs) [4]. Elevated AXL expression could promote oncogenic processes such as cell growth, migration, invasion, and epithelial-to-mesenchymal transition (EMT), which substantially contribute to tumor progression and poo
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Skeletal pain associated with bone fracture is another
2024-01-02

Skeletal pain associated with bone fracture is another area of critical need for a novel pain medication. NSAIDs and opiates are the two major therapies currently used to manage bone fracture pain. However, both of these therapies lead to significant unwanted side effects. Using the osteotomy model
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IC values were obtained for
2024-01-02

IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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In this study we have
2024-01-02

In this study, we have isolated 5(S),6(R)-7-trihydroxymethyl Heptanoate that encode ACL from G. zeae through random mutagenesis by restriction enzyme-mediated integration (REMI). The mutant Z39P186 where the ACL gene had been disrupted showed defects in vegetative growth, asexual and sexual develop
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br Regulatory mechanisms of ASK activity br
2024-01-02

Regulatory mechanisms of ASK1 activity The functions of ASK1 in disease ASK1 inhibitor As mentioned above, ASK1 plays a pivotal role in the pathogenesis of various diseases; hence, an ASK1 inhibitor has therapeutic potential. Although inhibitors of the ASK1 downstream kinases p38 and JNK ar
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