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ap1 The absolute requirement for substrate prephosphorylatio
2022-05-20
The absolute requirement for substrate prephosphorylation raised the possibility that short phosphorylated peptides might serve as selective substrate competitive inhibitors. A set of phosphorylated peptides patterned after known GSK-3 substrates was generated and shown to inhibit GSK-3 in vitro in
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GDC-0152 The endocannabinoid system ECS consists of cannabin
2022-05-20
The endocannabinoid system (ECS) consists of cannabinoid (CB)1 and CB2 receptors, their endogenous ligands anandamide and 2-arachidonylglycerol, and the synthesizing and degrading enzymes for these ligands. Cannabinoids and the ECS are involved in the regulation of GI motility in physiological and p
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Previously we reported that the inhibition of
2022-05-20
Previously, we reported that the inhibition of PKC-ζ and PKC-ε activity in hypertrophic adipocytes had deleterious effects on EPA-induced GPR120-mediated VEGF-A production [12]. However, the activation of PKC-θ, -ζ and -λ can also enhance the phosphorylation of IKK and p65, and facilitate the transl
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As well as the above
2022-05-20
As well as the above studies, Meier and coworkers used TUG-891, alongside omega-3 fatty acids, to show a potential role for FFA4 in inhibiting proliferation of DU145 prostate cancer cells [68]. Given that these cells express both FFA4 and FFA1 and the current view that TUG-891 may not be sufficientl
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All HFD fed groups in our study
2022-05-20
All HFD fed groups in our study, having significantly higher levels of EE (heat production) is consistent with previous studies [91], where a significant increase in EE was observed within just one week of HFD feeding [81]. It is hypothesized that this phenomenon is due to the increased body mass an
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Sepsis was defined as a systemic inflammatory response syndr
2022-05-19
Sepsis was defined as a systemic inflammatory response syndrome (SIRS) associated with severe infection in 1992 [9]. However, in the Third International Consensus Definitions for Sepsis and Septic Shock [10], it was redefined as life-threatening organ dysfunction provoked by a dysregulated host resp
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dpat br Methods and materials br Results
2022-05-19
Methods and materials Results To examine the fear conditioning effects of the pre-exposure, drug, and sex factors in the total latency time, a 2 × 3 × 2 three-way ANOVA indicated that dpat significant differences occurred in the drug (F2109 = 14.44, p 0.05) and pre-exposure × sex (F1109 = 0.
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Tail group SAR of the
2022-05-19
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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GKRP binds to the inactive super open conformation of
2022-05-19
GKRP binds to the inactive, super-open conformation of GCK, acting as a competitive inhibitor of glucose association with the enzyme (Fig. 3) [45]. Upon formation of the inhibitory complex with GKRP, GCK is sequestered into the hepatocyte nucleus [48]. The detailed mechanism by which GKRP mediates t
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Analysis of the GHSR screening
2022-05-19
Analysis of the GHSR screening data for inactive library members indicated that the prolinol-derived secondary amine and α-substituted phenoxyacetamide moieties described in were critical for activity. As a result, we initiated the synthesis of follow-up libraries utilizing the solid-phase chemistry
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br Concluding remarks br Introduction The hair cells
2022-05-19
Concluding remarks Introduction The hair KPT-276 of vestibular organs detect linear and rotational head movements, providing sensory information that is essential for normal postural and visual reflexes. Most vestibular hair cells are produced during embryonic development, but they can be los
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In perimenstrual catamenial epilepsy there is emerging
2022-05-19
In perimenstrual catamenial epilepsy, there is emerging evidence to suggest that P withdrawal plays a key role in seizure exacerbations occurring around the time of menstruation (Backstrom et al., 1984, Bonuccelli et al., 1989, Scharfman and MacLusky, 2006). The mechanisms underlying ovarian cycle-r
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br Acknowledgements This study was supported by National
2022-05-19
Acknowledgements This study was supported by National Institutes of Health grant (R01GM104037), VA grant (BX002741), and Rutgers Busch grant. Nuclear receptor FXR is the master regulator of bile acids homeostasis The farnesoid X receptor (FXR) belongs to a family of proteins known as nuclear
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br Redox cancer therapy The understandin
2022-05-19
Redox cancer therapy The understanding of ROS mechanisms supported the development of two parallel anticancer strategies based on ROS modulation, the use of antioxidants for cancer prevention and the use of ROS inducers to exacerbate oxidative stress to lead cancer K-115 to death [27], [133]. Th
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br Conclusion br Acknowledgements This study was supported
2022-05-19
Conclusion Acknowledgements This study was supported by the China Postdoctoral Science Foundation (No.2015M581817), the National Research Council of Science and Technology Support Program (2015BAD03B05-06), and the Priority Academic Program Development of Jiangsu Higher Education Institutions
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