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G-15 Recently accumulated evidence has revealed a close
2021-11-26

Recently, accumulated evidence has revealed a close link of FXR to gluconeogenesis. For example, activation of FXR by its agonist GW4064 improved hyperglycemia in db/db mice by repressing gluconeogenesis [15], and FXR agonist CDCA decreased transactivation activity of key gluconeogenic genes by indu
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br Conclusions Osteoclcastogenesis is regulated
2021-11-26

Conclusions Osteoclcastogenesis is regulated by multiple signal transduction pathways. To maintain bone homeostasis, osteoclast cells must achieve a balance regulation of formation, function, and trafficking of its precursors. Here, we proposed a model in which crosstalk between Fas and S1P/S1P1
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br Conclusion Discovery of an ideal orally active
2021-11-26

Conclusion Discovery of an ideal orally active antithrombotic drug has remained elusive till date. Research efforts in this direction led to the discovery of numerous coagulation enzyme inhibitors including various thrombin and FXa inhibitors. Several preclinical studies have highlighted the impo
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br Methods br Results We have
2021-11-26

Methods Results We have previously used ß-hex assays in HeLa nor-Binaltorphimine dihydrochloride to study the role of lysosomal exocytosis on transition metal clearance and the effects of transition metals on lysosomal exocytosis [26], [29], [40]. ß-hex is a lysosomal enzyme, the delivery of w
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Syt itself does not catalyze lipid mixing and membrane
2021-11-26

Syt1 itself does not catalyze lipid mixing and membrane fusion. Rather, the pairing of vesicular and target membrane SNAREs into complexes serves to pull bilayers together to drive fusion; Ca•syt1 accelerates these fusion reactions so that they occur on rapid timescales in a manner that is precisel
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In conclusion we have demonstrated
2021-11-26

In conclusion, we have demonstrated that the ejection of structural zinc ions from G9a and GLP in the presence of selenium-, and sulfur-containing electrophilic small BRL 37344, sodium salt leads to inhibition of these two biomedically important epigenetic enzymes. Our work demonstrates that clinic
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Here we investigate the structural and
2021-11-26

Here we investigate the structural and biochemical properties of the N-GTPase domain of p190RhoGAP-A. We determine the crystal structure and find that N-GTPase adopts an extended GTPase-like fold with six unique inserts that seem to preclude its ability to bind typical GAP, GEF, or Gemcitabine mole
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Pharmacologic approaches of inhibiting GSNOR activity
2021-11-26

Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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Difopein receptor Introduction Non alcoholic hepatic steatos
2021-11-26

Introduction Non-alcoholic hepatic steatosis is characterized by the presence of steatosis in hepatocytes [1], which leads to the development of fatty liver [2]. It is strongly associated with obesity, insulin resistance, and type II diabetes [3]. They are major risk factors of non-alcoholic hepati
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Niacin nicotinic acid is widely used to regulate abnormaliti
2021-11-26

Niacin (nicotinic acid) is widely used to regulate abnormalities in plasma lipid and lipoprotein metabolism, as evidenced by its potential for reducing atherosclerotic cardiovascular disease risks (Guyton, 1998), due to its ability to reduce circulating triglycerides and apolipoprotein-B containing
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br Material and methods br Results br Discussion Organisms h
2021-11-25

Material and methods Results Discussion Organisms have developed a variety of anti-glycation defense mechanisms. In amiodarone hcl sale to the aldose-reductase-pathway or 2-oxoaldehyde dehydrogenase-pathway, the glyoxalase system is the only mechanism, which is not restricted to liver [19]
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The glycine receptor is an ionotropic neurotransmitter recep
2021-11-25

The glycine receptor is an ionotropic neurotransmitter receptor coupled to a chloride ion channel. Glycine receptors are typically described as inhibitory and distributed in the spinal cord and brainstem, though mRNA transcription labelling studies in rats show expression in the hippocampus, cingula
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In order to elucidate the reasons of
2021-11-25

In order to elucidate the reasons of high efficacy of , we evaluated the BOC group itself and the linkage between the BOC group and the benzene ring of A-part. Urea moiety (), the replacement of an oxygen CCG 203971 of the BOC group to a nitrogen atom, decreased the activity (EC = 0.12 μM), while th
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5 03 Ghrelin readily crosses the blood
2021-11-25

Ghrelin readily crosses the blood 5 03 barrier (Banks et al., 2002, Banks et al., 2008), and recent studies have identified central nervous system sites of action for ghrelin-mediated appetite and hyperphagia (Alvarez-Crespo et al., 2012, King et al., 2011, Schele et al., 2016, Skibicka et al., 201
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br Materials and methods br Results and discussion br Conclu
2021-11-25

Materials and methods Results and discussion Conclusions Acknowledgements This study was supported by the Portuguese Foundation for Science and Technology (FCT) under the scope of the strategic funding of UID/BIO/04469/2013 unit and COMPETE 2020 (POCI-01-0145-FEDER-006684), and also by t
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