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A number of GCK activators for treating T
2021-09-23
A number of GCK activators for treating T2D have been developed and tested but not progressed successfully from clinical trials into therapy [45]. Our observations suggest that increased risk of hypoglycemia might be possible, particularly if drugs penetrate into brain. A further possibility is that
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br Indirect GLI antagonists br Direct GLI
2021-09-23
Indirect GLI antagonists Direct GLI antagonists Concluding remarks Targeting GLI effectors represents a promising therapeutic strategy for cancer treatment. This is particularly relevant for certain tumors, such as MB, since, although classified into four distinct molecular groups (Hh- or W
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In summary our findings provide the evidence and
2021-09-23
In summary, our findings provide the evidence and the mechanistic understanding of the protective effects of GIP receptor agonist, D-Ala2GIP, in the MPTP-induced neurotoxicity in mice. The observed protective effects are potentially due to reduced oxidative stress and attenuation of dopamine loss in
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br Conflict of interest statement
2021-09-23
Conflict of interest statement Acknowledgements Introduction Galanin is a multi-functional neuropeptide that is widely distributed in the neuroendocrine system and peripheral tissues of various species. This 29-amino-acid peptide (30 in humans) is proteolytically processed from its precurso
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In our study the changes in the and subunit
2021-09-23
In our study, the changes in the α4 and δ subunit expression were accompanied by a significant increase in γ2 subunit expression in almost all analysed hippocampal structures in the fully kindled animals. In contrast, an acute injection of PTZ at a convulsive dose (55mg/kg) evoked a potent decrease
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We next investigated whether pharmaceutical
2021-09-22
We next investigated whether pharmaceutical inhibition of the PI3K pathway was synergistic with FGFR inhibition using BKM120, a pan-PI3K inhibitor with modest antitumor activity in cancer patients, as a single agent. We found that RT112 (- translocation) and JMSU1 ( amplification) were not signifi
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It was then found that TAZ a YAP
2021-09-22
It was then found that TAZ, a YAP holomog, binds heteromeric SMAD2/3–4 complexes in a TGF-ß-dependent fashion, and is recruited to TGFβ response elements (Varelas et al., 2008). Knockdown experiments identified TAZ as critical for nuclear accumulation of SMAD2/3/4 complexes in response to TGF-ß, and
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Molecular modeling of the sGC H NOX domain has
2021-09-22
Molecular modeling of the sGC H-NOX domain has placed the β1-domain Cys, β1-C78 and β1-C122, close to the heme binding pocket; specifically, the β1-C78 is placed diametrically opposite to β1-H105, the residue responsible for coordinating the heme iron [42,43]. β1-C78 is enclosed in a highly PF-47086
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There is no doubt that GPR is
2021-09-22
There is no doubt that GPR55 is a LPI receptor; however, we should re-consider whether or not GPR55 is in fact another cannabinoid receptor. The pharmacologies of the GPR55 and CB1 receptors are complicated; CB1 inverse agonist/antagonists SR141716A (rimonabant) and AM251 were shown to be potent ago
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br Amino acid usage in cancer br
2021-09-22
Amino Trimidox usage in cancer Perspective High glucose consumption is a common feature of several types of tumor cells. Therefore, so far, in vivo positron emission tomography (PET) imaging with the glucose analog 18F-fluorodeoxyglucose (18F-FDG) has been used to detect various tumors. Howev
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br Materials and methods br Results
2021-09-22
Materials and methods Results Discussion In this study, we demonstrated that zaprinast (a cGMP-PDE inhibitor) induced the intracellular calcium mobilization in the glycosylase inhibitor coexpressing GPR35 and Gqi5, Gqo5, or Gα16. Induction of intracellular calcium mobilization by zaprinast
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A number of synthetic GPR agonists have been reported
2021-09-22
A number of synthetic GPR119 agonists have been reported to date, several of which have advanced into clinical trials. Reported GPR119 agonists are often composed of three parts as depicted in : a piperidine or a piperazine ring -substituted with a carbamate or a heteroaryl group at the right side,
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br Material and methods br Result br Discussion The
2021-09-22
Material and methods Result Discussion The female with well-differentiated endometrial cancer, especially those in the reproductive age have a strong desire to preserve fertility. Therefore, conservative medical treatment with progestin is widely used in the clinic. However, up to 30% of pa
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Recent research reveals that human alkyladenine
2021-09-22
Recent research reveals that human alkyladenine DNA glycosylase (hAAG) is an important protein enzyme which can specifically recognize and excise a variety of alkylated purines and deoxyinosine from DNA [12]. hAAG plays pivotal roles in maintaining genomic integrity, and it is involved in spectinomy
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br Materials and methods br Results and discussion br
2021-09-22
Materials and methods Results and discussion Conclusions In summary, the Au@SiO2 based lateral flow sandwich immunoassay for fast detection of EBN-specific glycoprotein has been firstly established by using nanocomposites as signaling-labels and synthesized EBN-specific apr 246 as recognit
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