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br Results and discussion br Conclusions
2021-12-30

Results and discussion Conclusions In summary, we generated analogues of the hit compounds 1–3, studied their structure–activity relationships, and created a series of highly potent GPR55 agonists. The most potent agonists among the series were 17a-b, 17e, 17g and 17l with EC50 values below 10
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In summary through medicinal chemistry
2021-12-30

In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on
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br A selective inhibitor of mammalian histone deacetylase tr
2021-12-30

A selective inhibitor of mammalian histone deacetylase, trichostatin A, reduces GnRH mRNA expression Epigenetic mechanisms controlling GnRH expression have been reported, and these mechanisms may be involved in the development and maturation of GnRH neurons in the brain (Gan et al., 2012, Kurian
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br Introduction L Glutamate is one of
2021-12-30

Introduction L-Glutamate is one of the most prevalent excitatory signaling molecules in the central nervous system (CNS) (Salazar et al., 2016) and plays a crucial role in a variety of BTL-104 functions such as memory and learning (Danbolt, 2001, Nedergaard et al., 2002). At elevated concentratio
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In the present study a significant
2021-12-30

In the present study, a significant increase in liver glut4 mRNA levels as well as an increase in liver glycogen content was observed in the dogfish in response to glucose-loading, although we did not observe any changes in liver glycogen content or glut mRNA levels following insulin administration
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Insulin de sensitization has been observed in the brains of
2021-12-30

Insulin de-sensitization has been observed in the brains of people with AD [51], [52], [53] and we previously demonstrated that the GLP-1 analogue liraglutide was able to reverse this [54]. Importantly, SANT-1 insulin de-sensitization correlates well with cognitive decline [15], [55] and with tau p
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Recently some researchers working in China Pharmaceutical Un
2021-12-29

Recently, some researchers working in China Pharmaceutical University developed novel FFA1 agonists some of which were found to be efficacious in the management of type 2 diabetes and with low toxicity. For instance, Zheng et al. [48] in their in vivo study using experimental animals, reported that
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The inhibitory activities of the compounds
2021-12-29

The inhibitory activities of the compounds with the modification of the amino group against human liver FBPase are summarized in . Replacement of the amino group of with hydrophobic substituent such as a methyl group () led to a substantial loss of activity (IC=995nM). Similarly, replacement with h
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EZH can also interact with
2021-12-29

EZH2 can also interact with Ten-Eleven Translocation gene family members (TET1, TET2, and TET3), which convert 5-methylcytosine (5 mC) to 5-hydroxymethylcytosine (5hmC), to cause changes in patterns of histone methylation and DNA methylation [52]. Huang et al. found that the expression levels of all
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The replenishment time course of
2021-12-29

The replenishment time course of already-tethered vesicle to became release ready, was examined by TIRFM imaging combined with calcium uncaging. By UV-flash photolysis of caged calcium, intracellular calcium concentration raises rapidly and homogenously throughout the cell (Ellis-Davies, 2008). Upon
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We have expanded these studies by doing EEG recording in
2021-12-29

We have expanded these studies by doing EEG recording in the ET-1 model. Using this technique, we demonstrated that activation of either the ETA how to make dilutions or the ETB receptor induces electrical seizures. ET-1 induced electrical seizures occurred in the presence of either the ETA recepto
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As for hMOF inhibitor s study Dekker and
2021-12-29

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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In Arabidopsis GCN containing protein complexes are found to
2021-12-29

In Arabidopsis, GCN5-containing protein complexes are found to be involved in cell differentiation, leaf and floral organogenesis [[8], [9], [10]]. AtHAC1 has involvement with root elongation, flowering, fertility and de novo shoot regeneration [11,12]. AtHAM1 and AtHAM2 control flowering time by ep
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Human immunodeficiency virus type HIV is responsible for the
2021-12-29

Human immunodeficiency virus type 1 (HIV-1) is responsible for the TCEP pandemic; notification is compulsory in Brazilian blood banks since 1988. From 1980 to 2016, the Brazilian MH reported 882,810 HIV/AIDS cases, with 52.3% in the southeast region. HIV/HCV co-infection has been associated with p
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br Transparency declaration br Acknowledgements br Hepatitis
2021-12-29

Transparency declaration Acknowledgements Hepatitis C Virus (HCV) infection represents a disease of significant global impact that afflicts around 170 million people worldwide., A small proportion of infected people clear the virus naturally, whilst the majority develop chronic hepatitis C (
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