• A group of small molecule with a more promising therapeutic

  2021-10-26

  

  A group of small molecule with a more promising therapeutic mechanism are known as γ-secretase modulators (GSMs), which modulate the cleavage activity of γ-secretase (and likely a host of other substrates) and specifically reduce the levels of the fibrillogenic Aβ42 peptide without altering the ε-si

• Emerging evidence has shown that pharmacological FXR

  2021-10-25

  

  Emerging evidence has shown that pharmacological FXR agonism attenuates chronic alcohol treatment-induced liver injury and steatosis [18], [19], while whole-body FXR knockout worsens alcohol-induced liver injury [19]. This suggests that FXR plays an important role in ALD development. However, defici

• By measuring the accumulation of unprenylated Rap a as a

  2021-10-25

  

  By measuring the accumulation of unprenylated Rap1a as a surrogate marker for the inhibition of FPPS [8], [9], [10], [11], we found that upregulation of FPPS expression in Hela cells reduced the accumulation of unprenylated Rap1a in response to 24h' treatment with 0–50μM ZOL. As expected, cells cult

• Hypoxia HIF and Inflammation Cellular responses to hypoxia a

  2021-10-25

  

  Hypoxia, HIF, and Inflammation Cellular responses to hypoxia are essential for life and are now recognized to be dysregulated in a wide range of disease processes. The key players in these pathways are a family of transcription factors, the hypoxia-inducible factors (HIFs; see Glossary), as well as

• Sugar gliders and hedgehogs are insectivores and

  2021-10-25

  

  Sugar gliders and hedgehogs are insectivores and actively seek arthropods in nightly forays. It is suspected that Triatoma were not feeding on the sugar gliders and hedgehogs, but rather were being eaten. The oral route of infection is often nonfatal and induces a carrier state in South American did

• how to calculate dilution In our previous study we designed

  2021-10-25

  

  In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic how to calculate dilution (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and i

• br General aspects of HDACs br General aspects of

  2021-10-25

  

  General aspects of HDACs General aspects of HDAC inhibitors Based on the previous elements, inhibitors designed for HDAC have in common a well-admitted pharmacophore model (Fig. 7A). This model is composed of a zinc binding group (ZBG), attached to a linker chain mimicking the lysine side chai

• Having identified initial leads and further lead optimizatio

  2021-10-25

  

  Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic b-raf inhibitors derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl, ch

• Various inhibitors have been developed to target

  2021-10-25

  

  Various inhibitors have been developed to target molecules present in these pathways. They include both man-made monoclonal phospholipase a2 inhibitor as well as small molecule membrane permeable inhibitors that often target kinases or phosphatases [5], [338], [348], [364]. In summary, these pathwa

• The compounds described in this paper were prepared

  2021-10-25

  

  The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m

• br Introduction High dose niacin

  2021-10-25

  

  Introduction High dose niacin, or nicotinic acid, has been used as an athero-protective drug for more than 50 years (Carlson, 2005, Offermanns, 2006). When taken in pharmacological doses (>1g/day), the nicotinic protein kinase inhibitor form of niacin modulates plasma lipid profiles including dec

• br Results and discussion br

  2021-10-25

  

  Results and discussion Conclusions Introduction There is no effective treatment for HIV-associated neurocognitive disorder (HAND) which affects about half of the over 36 million people infected (Saylor et al., 2016). HIV can remain in the CI 976 during combination antiretroviral therapy (E

• Young et al described the role of adenine monophosphate acti

  2021-10-25

  

  Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c

• br Introduction As a fundamental metal

  2021-10-23

  

  Introduction As a fundamental metal-dependent hydrolytic enzyme, inorganic pyrophosphatase (PPase) exhibits a specific catalytic ability, in which one molecule of inorganic pyrophosphate (PPi) can be transformed into two orthophosphate (Pi) ions [1,2]. The process of transformation is extremely e

• The deduced amino acid sequences of all scIPPSs

  2021-10-23

  

  The deduced amino gdc-0980 synthesis sequences of all scIPPSs display high similarity, and sequence alignments reveal seven conserved regions [2]. Regions II and VI contain the substrate-binding regions, with two characteristic aspartate-rich motifs (DDx(xx)xD; where x represents any amino acid res

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