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br Conflict of interest br
2021-09-14
Conflict of interest Funding Acknowledgements Introduction to SLC6 transporters The solute carrier (SLC) 6 family of membrane proteins perform the Na+-coupled symport of amino acids and amino brincidofovir receptor derivatives into cells throughout the body. Disrupting neurotransmitter
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With the aim to identify potential novel targets in
2021-09-13
With the aim to identify potential novel targets in CVD, we applied proteome analyses on vascular tissue of these frequently used mouse models of atherosclerotic disease in the presence and/or absence of diabetes. Potential targets for intervention identified with this approach were validated in hum
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Among the HER mutations reported
2021-09-13
Among the HER2 mutations reported in this study, the JMD mutant R678Q is the third most recurrent HER2 mutation. Basic residues (such as arginine) play an important role in anchoring TMD helices of single transmembrane proteins to the bilayer (Gleason et al., 2013, Hristova and Wimley, 2011, Kim et
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The HCV Ag immunoassay has been shown from
2021-09-13
The HCV-Ag immunoassay has been shown from previous studies to be an adequate alternative to the two-stage diagnostic process [6], [9], [16]. Kesli et al. reported a high correlation coefficient of 0.864 when comparing HCV core antigen levels with HCV RNA levels (detected using Qiagen HCV RNA test;
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Three additional Type I CDK
2021-09-13
Three additional Type I CDK8 and CDK19 kinase inhibitors have also been recently reported. Orally available 3-benzylindazole 12 was discovered by optimization of compounds with HSP90 affinity to yield potent and selective CDK8 inhibitors. Compound 12 showed strong binding activity for CDK8 with an I
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These to date remain the only two reports of mutations
2021-09-13
These to date remain the only two reports of mutations in GC-C found in humans. Perhaps this once again emphasized the critical requirement of the presence of an optimally functional GC-C in the intestine, since neither its loss, nor its hyperactivity, can be tolerated in humans without severe conse
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Although it has been observed in numerous studies and by
2021-09-13
Although it has been observed in numerous studies and by many investigators that intraplatelet cGMP elevation results in platelet inhibition, there are a few papers which proposed a platelet stimulatory role for cGMP when elevated in response to NO donors or PDE5 inhibitors in mouse and human platel
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We also demonstrated that inhibition of NAAG
2021-09-13
We also demonstrated that inhibition of NAAG hydrolysis to suppress glutamate production through a GCPII inhibitor is a viable target for cancer therapy. GCPII is also known as N-acetyl-L-aspartyl-L-glutamate peptidase I (NAALADase I) or NAAG peptidase (Pinto et al., 1996), and its increased express
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PBI is an agonist of GPR and
2021-09-13
PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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The main aim of our study was
2021-09-13
The main aim of our study was to identify whether glucokinase and Irs2 were required for beta cell replication induced by short-term HF diet feeding. Glucokinase plays a critical role in regulating blood glucose levels by catalysing the rate-limiting biochemical reaction of glycolysis [26,27]. In pa
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In type diabetic subjects with mean baseline glycated hemogl
2021-09-13
In type-2 diabetic subjects with mean baseline glycated hemoglobin A (HbA) of 8.4%, q.d. administration of MK-0893 for 12weeks as a monotherapy resulted in dose-dependent decreases in HbA and FPG. Administration of MK-0893 q.d. at doses of 20, 40, 60, and 80mg led to observed reductions in HbA of 0.
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adenosine receptor agonist Attempting to further elucidate t
2021-09-13
Attempting to further elucidate the role of adenosine receptor agonist and activation of the Gcgr without the influence of GLP-1, we used DT-Gcg mice with acute knockdown of all proglucagon products. This mouse model has previously been shown previously to have a normal total islet area as well as
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The first GSM was identified from the discovery of
2021-09-13
The first GSM was identified from the discovery of non-steroidal anti-inflammatory drugs (NSAIDs). An amyloid reducing GSM that also suppresses inflammation is desirable. Inflammatory response is an invariable characteristic of AD pathogenesis, in part triggered by Aβ. During AD onset and progressio
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Following an endoproteolytic cleavage of C secretase trims
2021-09-13
Following an endoproteolytic cleavage of C99, γ-secretase trims the remaining fragment Aβ49 or Aβ48 in successive, mostly three-residue steps. Aβ49 typically gives rise to Aβ46, Aβ43, and Aβ40; whereas Aβ48 usually yields Aβ45 and Aβ42 [59]. The physical basis for this characteristic cleavage patter
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br Conclusion In the present study we
2021-09-13
Conclusion In the present study, we found that the majority of commercially available antibodies and antibody-based tools against galanin and its receptors that we tested do not meet validation requirements. Therefore, critical validation of these tools by the user is essential before being used
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