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Accessibility and physico chemical features
2022-07-12
Accessibility and physico-chemical features of cysteine residues define their redox-reactivity and the 3-dimensional structure of GSNOR allows to identifying such surface-exposed, redox-sensitive cysteine residues. GSNOR crystal structures are available from human (Protein Data Bank code: 1MP0), tom
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PF-03814735 receptor In this study we explore different math
2022-07-12
In this study, we explore different mathematical models for describing the IVIVC of a preclinical dataset of 12 different dual GPR109A/GPR81 agonists. The objective is to establish a predictive model of in vivo lipolysis suppression in the rat based on in vitro potency data. First, a nonlinear mixed
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Na K ATPase adenosine triphosphate ATP and astrocytic glutam
2022-07-11
Na+/K+-ATPase, Etomoxir receptor and astrocytic glutamate transporters act together to maintain sodium and potassium gradients and the proper activities of EAAT1 and EAAT2 (Rose et al., 2009; Sheean et al., 2013); nevertheless, in present study, Na+/K+-ATPase activity was shown to be increased as f
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Through the analysis of various synthetic GPR agonists
2022-07-11
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic 94 8 motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering TAK-875,
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To confirm that these were bona fide
2022-07-11
To confirm that these were bona fide interactions, we investigated whether the potassium channel subunits or Tmem263 formed complexes with GLT-1 or DAT after immunoprecipitation. Lysates of HEK-293 cells previously cotransfected with HA-GLT-1 or HA-DAT, and either YFP-Kv7.3, YFP-Kv7.2 or YFP-Kv7.5 w
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Several studies have indicated MUC to
2022-07-11
Several studies have indicated MUC1 to be an effective marker for identifying various malignant tumors, such as gastric, breast, pancreatic, ovarian, gallbladder, uterus, lung, and prostate cancers, as well as for prognostic outcomes [16], [17], [18], [19], [20], [21], [22], [23]. Studies by Kaira e
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br Acknowledgements This work was supported
2022-07-11
Acknowledgements This work was supported by the grants from National key Basic Research Program of China (2012CB124702), 948 Program (2015-Z33), National Natural Science Foundation of China (31172093, 31301947), the National Science Foundation for Fostering Talents in Basic Research (J1103510), S
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br A myriad of receptors in
2022-07-11
A myriad of receptors in WM To complicate the picture, WM glia express numerous non-glutamatergic neurotransmitter receptors, a fact that is often underappreciated when considering pathophysiology. When examined in isolated optic nerve, a central WM tract completely devoid of neuronal synapses, r
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br Conflicts of interest br Acknowledgments This
2022-07-11
Conflicts of interest Acknowledgments This work was supported by the following funds: National Natural Science Foundation of China (81502222); Natural Science Foundation of Hubei Province (2013CFB370); Training program for Wuhan young and middle-aged medical backbone personnel (2017–51). In
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SNL in rats led to upregulated Panx mRNA and protein
2022-07-11
SNL in rats led to upregulated Panx1 mRNA and protein level in DRG but not in spinal cord, and immunostaining revealed increased Panx1 in DRG neurons [50]. Although it was not emphasized, Panx1 labeling in SGCs was also increased in this pain model. Intrathecal injection of Panx1 blockers or Panx1-s
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Because of its role in the cleavage
2022-07-11
Because of its role in the cleavage of Aβ and the fact that many genetic forms of AD are caused by mutations in the enzyme, GS has long been a target for drug development, though previous clinical trials of Semagacestat, a GS inhibitor, have failed due to an increase in skin cancer, and a decrease i
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In the course of our
2022-07-11
In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric MRS 2365 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 process
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The NGS of six Southern
2022-07-11
The NGS of six Southern Brazil patients revealed three different variants: c.472C > T (p.Arg158Trp); c.958G>A (p.Gly320Arg) and c.986T>C (p.Leu329Pro) (Table 2). The amino acids involved in these substitutions were evolutionarily conserved in different species (Fig. 1B). The amino HG-9-91-01 austral
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br Conflicts of interest br Acknowledgments This
2022-07-08
Conflicts of interest Acknowledgments This work was supported by the Project of Huzhou Municipal Science and Technology Bureau of Zhejiang Province (No. 2016GY45 to YGC) and he Project of Zhejiang Basic Public Benefit research of Zhejiang Province (No. LGF18H160005 to YGC) Introduction Wi
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The H R couples to G i o proteins and
2022-07-08
The H3R couples to Gαi/o proteins, and hence its stimulation leads to inhibition of adenyalate cyclases, diminishing the level of cyclic AMP (cAMP) with the subsequent reduction in downstream signaling pathways such as protein kinase A (PKA) activation and cAMP-responsive element binding protein (CR
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