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A range of inhibitors were
2019-12-06
A range of inhibitors were therefore synthesized containing either carboxylic Furegrelate sodium salt or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively
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In this study we have developed and investigated three
2019-12-06
In this study we have developed and investigated three NADPH-regenerating fusion partners with two different enzyme systems: a BVMO and an ADH. With the exception of one fusion construct (StGDH with LbADH), all fusion Methimazole resulted in good soluble expression as well as fully functional as se
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The role of ARA cyp
2019-12-06
The role of ARA-cyp450 metabolites in the liver is still unclear [44]. However, ARA-cyp450 genes metabolize other fatty acids such lauric and palmitic Ro3280 [45]. It was found that decreased cyp4a expression caused fatty livers through reduction of fatty acid metabolism [46]. In this study, we foun
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To study the role of DNA PK in
2019-12-05
To study the role of DNA–PK in the response to replication arrest, we used the DNA replication inhibitor aphidicolin (APH). APH, a mycotoxin isolated from Cephalosporium aphidicola, inhibits DNA replication by interacting with the replicating DNA polymerase α (pol α). APH specifically inhibits the a
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Taken together this study gives first insights into the
2019-12-05
Taken together, this study gives first insights into the complex effect of DNMT inhibition on pattern separation. Acute administration of RG108 enhanced pattern separation performance measured with the OPS task and increased Bdnf1 expression. However, this effect was only acute, and was not present
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br Anti inflammatory effects of MTX In
2019-12-05
Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph
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These data indicate that in
2019-12-05
These data indicate that, in the context of the N-terminal 42 amino acids of p53, threonine 18 is a substrate for phosphorylation by CK1 as mediated by prior phosphorylation of serine 15. To determine whether this is a property of full length p53, GST-p53 fusion proteins comprising the full length p
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The relatively low overall response rates
2019-12-05
The relatively low overall response rates suggest the need for better predictive markers for response. The patient demographics in the SARC trial did not reflect typical Ewing sarcoma demographics as the patients tended to be older and had primarily soft tissue tumors. In addition, although accrual
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br Introduction Phoenixin PNX is a recently discovered
2019-12-05
Introduction Phoenixin (PNX) is a recently discovered peptide produced mainly in hypothalamus by proteolytic cleavage of a small integral membrane protein 20 (Smim20) [1]. The most important endogenous active isoforms of PNX are amided peptides, composed of 14 and 20 JW 55 australia [2]. Previou
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Lately using receptor TM peptides
2019-12-05
Lately, using receptor TM peptides, BiFC and PLA experiments, we have also obtained experimental evidence for the tetrameric structure of A1R–D1R, which explains the canonical interaction on Gi and Gs, respectively (Fig. 2). We have demonstrated for the first time the presence of this heterotetramer
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A growing body of data
2019-12-04
A growing body of data indicates that endothelial NOS (eNOS) is a rate-limiting enzyme for the synthesis of nitric oxide (NO), its downstream auz sale molecule. High pathological concentrations of NO produced from inducible NO synthase (iNOS) induce apoptosis, whereas a reduction in the concentratio
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br Acknowledgments The authors thank Dr Tai Sheng Cheng Yu
2019-12-04
Acknowledgments The authors thank Dr. Tai-Sheng Cheng, Yu-Wen Huang and Ting-Wei Gau for technical assistance. This work was supported by the National Science Council of TaiwanNSC 98-2320-B-024-002-MY3 and National University of TainanAB102-216. This information is available free of charge via th
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The inhibition of mRFP Ub E
2019-12-04
The inhibition of mRFP-Ub–E1 formation by ginsenosides Re was not in time-dependent in vitro (Fig. 4B). Fifty micrometres ginsenoside Rg1 decreased E1 activity to 0.24- to 0.36-fold over 30min. This finding suggests that ginsenoside Rg1 may irreversibly inhibit mRFP-Ub–E1 formation or a tight-bindin
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br Effect of DPP Inhibitors on the Clinical Course
2019-12-04
Effect of DPP-4 Inhibitors on the Clinical Course of Heart Failure Four large-scale cardiovascular outcomes trials with DPP-4 inhibitors have been completed, and their findings have been published (Table 1) 31, 32, 33, 34. In 2 studies (with saxagliptin and alogliptin), DPP-4 inhibition was accom
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Approximately of the etamicastat dose was recovered
2019-12-04
Approximately 50% of the etamicastat dose was recovered in urine, 30% in the form of etamicastat and 20% in the form of BIA 5-961. These data agree with those from a study with [14C]-labeled etamicastat in healthy subjects, which showed that approximately 95% of the administered radioactivity had be
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