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We also demonstrated that inhibition
2022-04-11

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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Ketamine has recently been found to exert rapid and
2022-04-09

Ketamine has recently been found to exert rapid and sustained antidepressant effect. Single dose ketamine can have an efficacy of up to 1 week [20]. Furthermore, ketamine is an effective drug against refractory depression [21,22]. The antidepressant mechanism of ketamine is still unclear. Whether CO
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br Methods br Results br Discussion The measurement
2022-04-09

Methods Results Discussion The measurement of intraocular pressure was made with a commercially available rebound tonometer, the Tonovet®. In our studies, Tonovet® underestimated the intraocular pressure in both animal models, being this effect more pronounced in the rat. To study the effe
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Emodepside The presented results speak for the direct effect
2022-04-09

The presented results speak for the direct effects of ghrelin on rat spermatozoa, which are accomplished by the activation of the GHSR-1a receptor. Thus, the results seem to be of physiological significance in vivo since ghrelin, the natural ligand of GHSR-1a, was found to be present in the seminal
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In order to facilitate the
2022-04-09

In order to facilitate the preparation of 2-aminothiazoles containing novel D-ring substitutions, a convergent synthetic route was selected which requires the synthesis of common precursor . Straightforward aromatic substitution of 3,4-difluoroacetophenone using 4-methylimidazole provided access to
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The gene structures of cGalR and
2022-04-09

The gene structures of cGalR2 and cGalR2-L were determined by in silico comparison with the chicken genomic DNA sequences retrieved from the Ensembl database. Both cGalR2 and cGalR2-L genes are composed of two coding exons, separated by single introns of 0.9kb (cGalR2) or 3kb (cGalR2-L) locating wit
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In this study we have investigated the expression of FXR
2022-04-09

In this study, we have investigated the expression of FXR and TGR5 in CCA tissues in two independent cohorts of patients and determined their association with tumor clinicopathological parameters. The expression of both BA receptors was also evaluated in CCA human cells and normal human cholangiocyt
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In addition several other considerations were made for the
2022-04-09

In addition, several other considerations were made for the optimization exercise. While the structural features of the endogenous ligands for long-chain fatty Rhapontigenin receptors suggest obtaining orthosteric agonists with drug-like properties may be challenging, the optimization efforts were
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br Acknowledgements We thank Kathy Spindler for helpful revi
2022-04-09

Acknowledgements We thank Kathy Spindler for helpful review of the manuscript. Expert technical assistance from Joel Whitfield in the University of Michigan Cancer Center Immunology Core is greatly appreciated. This research was supported by the American Heart Association (16GRNT30250013) and by
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Chi square tests with significance set to p were used
2022-04-09

Chi-square tests with significance set to p Results There were 4090 hip fracture patients included in the study. 2326 of these received enoxaparin, 929 received XaI, and 835 received warfarin. The mean CCI for each group was 3 (Table 2). There were some significant differences in demographics betw
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Senger et al performed a retrospective
2022-04-09

Senger et al. performed a retrospective review of 17 patients with ICH on dabigatran or rivaroxaban who received 4F-PCC. Eight patients had a traumatic K02288 injury (TBI) and nine patients had a spontaneous ICH. Nine patients had a devastating outcome, including severe neurologic deficits, comatose
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The mechanism study demonstrated that BDNF
2022-04-09

The mechanism study demonstrated that BDNF is one of the fundamental mechanisms underlying JMJD2A effects during neuropathic pain. BDNF is a neurotrophin with essential functions in neuronal development and neuroplasticity. Accumulating evidence suggests that alterations in BDNF expression levels un
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br Conclusion Our data allow pharmacological discrimination
2022-04-09

Conclusion Our data allow pharmacological discrimination of diverse of H3 4EGI-1 receptor antagonists that can be linked to their differential efficacy in preclinical and clinical disease settings (Fig. 6). Moreover, we identify the sigma-1 receptor as a common “off target” for H3 antagonists, a
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The CRY protein contains a
2022-04-09

The CRY1 protein contains a conserved photolyase homology region crucially involved in repression of CLOCK/BMAL1; a C-terminal helix also known as the predicted coiled coil (CC), which interacts with PER2 and FBXL3 in a mutually exclusive manner; and a C-terminal extension also referred to as the “t
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Mitochondrial binding by HK prevents mortality by
2022-04-09

Mitochondrial binding by HK prevents mortality by inhibiting pro-apoptotic factor (Bcl-2 family)-mediated opening of the mitochondrial permeability transition pore (mPTP) (Arora and Pedersen, 1988, Calmettes et al., 2016, Kodde et al., 2007, Pedersen et al., 2002, Rosano, 2011, Schindler and Foley,
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