• br Materials and methods br Results and

  2022-02-07

  

  Materials and methods Results and discussion Conclusions Notes Declaration of interest statement Acknowledgment This work was supported by the National Natural Science Foundation of China (No. 21775132, 21505112), Scientific Research Foundation of Hunan Provincial Education Departm

• In the light of the

  2022-02-07

  

  In the light of the above-mentioned considerations, it is interesting to note that the FPR-related research with regards to bias agonism did not prosper during considerably during the last decade (possible exceptions are [[8], [9], [10], [11]]. However, with new insights in receptor chemistry and fu

• br Clinical development of FGFR inhibitors in

  2022-02-07

  

  Clinical development of FGFR inhibitors in breast cancer The rationale to explore the role of FGFR inhibitors in patients with breast cancer comes from a variety of sources. These include genomic aberrations frequently identified in the FGF/FGFR pathway in breast cancer, the increased sensitivity

• Another lever to efficiently eradicate tumors

  2022-02-07

  

  Another lever to efficiently eradicate tumors including ovarian cancer might rely on their high addiction to iron [34]. In fact, ultrasmall silica-based nanoparticles, functionalized with melanoma-targeting peptide, efficiently triggered ferroptosis not only in cell culture but also in tumor bearing

• Aberrant activity of PRC as a result of

  2022-02-05

  

  Aberrant activity of PRC2 as a result of over expressed EZH2, has been frequently seen in a wide range of human cancers including breast and prostate tumors [10]. However, leukemia-associated epigenetic aberrations are not fully understood [7]. Herein, we will overview the current knowledge of epige

• br Introduction Atherosclerosis is a chronic inflammatory

  2022-02-05

  

  Introduction Atherosclerosis is a chronic inflammatory disease characterized by lipid and leukocyte accumulation within the arterial wall. Homocysteine (Hcy) is a thiol-containing amino PFI 3 derivative derived from the metabolism of dietary methionine. Epidemiological studies have shown that el

• Throughout our studies we used CBD

  2022-02-05

  

  Throughout our studies we used CBD under the assumption that it binds to the GPR55 receptor and has antagonist properties at the GPR55 receptor, as previously suggested (Whyte et al., 2009). To clarify whether the GPR55 receptor is involved in the O-1602-mediated effects on GI motility, we performed

• Continuing studies of endocannabinoid ligands

  2022-02-05

  

  Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort

• br Materials and methods br Results

  2022-02-04

  

  Materials and methods Results Discussion To the best of our knowledge, the current study presented the first evidence that GPR40, also named FFAR1, played an essential role in bone formation and mediated tlr4 receptor induced osteogenic effect via Wnt/β-catenin signaling. We found that dos

• Given the proposed importance of conformational

  2022-02-03

  

  Given the proposed importance of conformational dynamics to GCK's allosteric regulation, a number of biophysical methods have been utilized to probe the enzyme's dynamic structural landscape. Investigations into the mechanism of Decanoyl-RVKR-CMK binding, using changes in the enzyme's intrinsic flu

• Two excellent GSMs with clear pharmacological effect across

  2022-02-03

  

  Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas

• We reveal that the four well

  2022-02-01

  

  We reveal that the four well known vertebrate families of KAT enzymes (GNAT, MYST, P300/CBP, Basal transcription factor/nuclear receptor co-activator) seem to be conserved (Karmodiya et al., 2014; Roth et al., 2001; Sheikh & Akhtar, 2018) in the mangrove rivulus, together with Camello, a potential n

• Introduction Histamine Imidazolyl ethylamine is an important

  2022-02-01

  

  Introduction Histamine [2-(4-Imidazolyl)-ethylamine] is an important mediator of many physiological and pathological processes including inflammation, gastric Cy5 EGFP mRNA secretion, neuromodulation, regulation of immune function, cell proliferation and differentiation, among others. Histamine ex

• In addition to redox stress nutritional intake plays a

  2022-02-01

  

  In addition to redox stress, nutritional intake plays a key role in modulating energy metabolism. DIO animal models are commonly used to study altered metabolic changes consequential to fat storage within various fat pads. In general, diets containing >40% high-fat lard, milk, and butter promote exc

• In summary activated A AR exacerbated the reverse transport

  2022-02-01

  

  In summary, activated A2AR exacerbated the reverse transport function of endothelial EAATs through a direct or indirect pathway depending on PKA and glutamate levels in response to OGD in vitro, but A2AR inhibition quickly restored the normal transport function. Moreover, the key mechanisms by which

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