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Several layers of regulation for
2021-11-01
Several layers of regulation for this canonical activation of the HH pathway exist. First, the protein kinase A (PKA), the casein kinase 1α (CK1α) and GSK3β can phosphorylate and mark for proteosomal degradation the GLI transcription factors. [36] Second, Suppressor of Fused (SUFU) binds to GLI and
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Lactate as administered in these
2021-10-29
Lactate as administered in these models is metabolized rapidly and it appears that transient engagement of GPR81 with lactate serum concentrations in the range of moderate exercise physiology, as measured here at 3–4 mmol/L, are sufficient to suppress tissue macrophage NF-κB activation in our models
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ESI-09 It appears that not all GPR agonists
2021-10-29
It appears that not all GPR119 agonists require a high dose to elicit acceptable ESI-09 control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved by 30mg/kg sitaglipt
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In addition to gonadotropes GnRHRs have also
2021-10-29
In addition to gonadotropes, GnRHRs have also been detected on somatotropes, lactotropes, thyrotropes, melanotropes, somatolactin (SL) cells, and/or corticotropes using immunohistochemical, radioligand-binding, or mRNA expression approaches across species; including fishes, rats, and humans (La Rosa
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DCG IV The fact that KNDy neurons activity is sensitive
2021-10-29
The fact that KNDy neurons activity is sensitive for circulating hormones related with control of DCG IV homeostasis was demonstrated in other studies (Cejudo Roman et al., 2012; Navarro et al., 2011). It is well documented that leptin plays an important role in the regulation of the gonadotrophic a
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Petrat et al could show that even a low
2021-10-29
Petrat et al. could show, that even a low dosage of 10-mg/kg glycine (133 μmol/kg) has a beneficial effect on the small intestine after I/R. In regard to glycine, β-alanine has a clearly higher EC50 to the GlyR and activates the receptor with an efficiency of only 34.6%.16, 17 Therefore, it can be c
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br Introduction Most organisms require
2021-10-29
Introduction Most organisms require glucose as a key metabolite, and it is critical that mammalian cells regulate glucose levels properly to maintain bioenergetic homeostasis. The major transporters responsible for the uptake of glucose from systemic circulation into cells are the GLUTs, members
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Injury to oligodendrocyte progenitors caused in part by glut
2021-10-29
Injury to oligodendrocyte progenitors caused in part by glutamate contributes to the pathogenesis of myelination disturbances in PVL [5]. In the immature human brain, the susceptibility of developing oligodendrocytes to hypoxia-ischemia correlates with their expression of glutamate receptors of the
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br Galanin in depression A major
2021-10-29
Galanin in depression A major impediment in depression research is the lack of validated animals´ models. Animals not only lack consciousness of self, self-reflection and consideration of others but also hallmarks of the disorder such as depressed mood, low self-esteem or suicidal intent are hard
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In the course of our ongoing attempts
2021-10-29
In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric Cobimetinib type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise the proce
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br Author contributions br Conflict of interests br Acknowle
2021-10-29
Author contributions Conflict of interests Acknowledgements This work was supported by NIH grant DK098730 to NHM. Free fatty acids play important roles in biological processes contributing to both health and disease. As essential nutritional components, free fatty acids are utilized as b
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Prior models suggest that the terminal ends
2021-10-29
Prior models suggest that the terminal ends of the endocrine FGFs individually determine FGFR and KLB recognition, with little or no cross-talk. Our results confirm that short C-terminal sequences are necessary and sufficient to bind KLB and, supportive of a common mechanism, the underlying structur
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br Results br Discussion Our
2021-10-29
Results Discussion Our studies highlight MUFAs as key lipid modulators of both non-apoptotic and apoptotic cell death. Recent studies show that a more mesenchymal phenotype, de-differentiation, and acquired resistance to targeted inhibitors, can all promote a ferroptosis-sensitive cell state (
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Reparixin L-lysine salt synthesis Introduction Ventilator in
2021-10-29
Introduction Ventilator-induced lung injury(VILI) is the most common complication in the mechanical ventilation in clinic. Repetitive opening and closing of Reparixin L-lysine salt synthesis at high pressures during artificial ventilation would generate shear stress and then lead to the damage of c
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Multi targeting agents are of major
2021-10-29
Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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