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Through the analysis of various
2021-09-11

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic Walrycin B mg motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discoverin
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In the GLUT family glucose
2021-09-11

In the GLUT family, glucose transporter 1(GLUT1) is primarily responsible for basal glucose uptake and maintenance of glucose basal metabolism in cells (Olson and Pessin, 1996). High GLUT1 expression occurred in various types of human cancers, like brain tumor, lung cancer and esophageal cancer (Nis
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microcystin lr GK allosteric activators validate the importa
2021-09-11

GK allosteric activators validate the importance of GK from a therapeutic perspective, but the nature of allosteric activation of GK remains unclear. The GK allosteric activator site, the pocket where GKAs bind, is ~20 Å remote from the active site (Fig. 1A). The allosteric site is the locus of man
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Work in the Ruiz i Altaba lab was funded
2021-09-11

Work in the Ruiz i Altaba lab was funded by grants from the Swiss National Science Foundation, the Ligue Suisse Contre le Cancer, the European FP7 Marie-Curie Initial Training Network HEALING, a James McDonnell Foundation 21st Century Science Initiative in Brain Cancer-Research Award and funds from
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Experiments show that CSD propagation
2021-09-11

Experiments show that CSD propagation can be slowed or interrupted by pre-existing lesions or areas of high astrocytic density (Chen et al., 2006), and reduced expression of astrocytic gap junctions significantly increases the size of ischemic infarcts (Nakase et al., 2003). By decreasing the gap ju
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Chlormezanone As for hMOF inhibitor s study Dekker and Zheng
2021-09-10

As for hMOF inhibitor's study, Dekker and Zheng et al. synthesized MG149 (Fig. 1) as an inhibitor of Tip60 and MOF which has an IC50 value of 74 ± 20 μM and 47 ± 14 μM [31]. However, MG149 has no experimental data on hMOF in cell or in vivo. The lack of hMOF inhibitor limits the function study of hM
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This crosstalk may be responsible
2021-09-10

This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on Lomustine pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation of high-dose raniti
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These agents can be divided into three
2021-09-10

These agents can be divided into three categories based upon the therapeutic agent conjugated to the antibody; the most frequently explored are ADCs using a cytotoxic agent to be delivered directly to the tumor site. The second class has not been broadly used and consists of radionucleotides (Wong e
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In addition to understanding the
2021-09-10

In addition to understanding the GEF-GAP cycle regulating Rho-family GTPases, studies have continued to address the role of the Rho-GDIs, which binds to the geranylgeranyl tail to sequester Rho-family GTPases from interacting with lipid membranes, preventing their activation. Whilst it would be temp
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br Introduction Atherosclerosis is a
2021-09-10

Introduction Atherosclerosis is a chronic inflammatory disease characterized by lipid and leukocyte accumulation within the arterial wall. Homocysteine (Hcy) is a thiol-containing amino AG957 derivative derived from the metabolism of dietary methionine. Epidemiological studies have shown that el
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Another important question is what
2021-09-10

Another important question is what ligand(s) bind to GPR84 in vivo? Previous studies have identified medium-chain FFAs of 9 to 14 carbons in length and two other organic molecules (6-n-octylaminouracil and 3,3′-diindolylmethane) as agonists of GPR84 in vitro (Wang et al., 2006, Suzuki et al., 2013).
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Abn CBD induced changes reduced microglial cell
2021-09-10

Abn-CBD induced changes (reduced microglial cell density, Cy5 TSA Fluorescence System Kit sale size and a lower density of ramification) in the microglial morphology that could be compatible with a blockade of the neuroinflammation provoked by MPTPp. The absence of GPR55 transcripts in microglial c
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Our synthetic approach to GPR antagonists was designed
2021-09-10

Our synthetic approach to GPR55 antagonists was designed so that many different structures could be accessed to rapidly explore initial SAR, along with validating or modifying our current model (). The synthesis begins with the coupling of a carboxylic u73122 to 4-piperidone by first forming the aci
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br Materials and methods br Results br
2021-09-10

Materials and methods Results Discussion In this study, we demonstrated that zaprinast (a cGMP-PDE inhibitor) induced the intracellular calcium mobilization in the Iohexol coexpressing GPR35 and Gqi5, Gqo5, or Gα16. Induction of intracellular calcium mobilization by zaprinast in the GPR35-e
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Some studies show that testosterone
2021-09-10

Some studies show that testosterone may be involved in regulating cell proliferation and its stimulating effect has been proved in castrated rats (Wainwright et al., 2011), but not in mice and meadow voles (Ormerod and Galea, 2003; Benice and Raber, 2010). However, the seasonal difference in cell pr
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