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Ulimorelin also known as TPZ is a
2022-02-07

Ulimorelin, also known as TPZ101, is a macrocyclic molecule that is a potent agonist of the ghrelin receptor (Hoveyda et al., 2011). Due to its ability to stimulate gastrointestinal motility, ulimorelin has been evaluated as a possible treatment in gastroparesis (Ejskjaer et al., 2010), ileus (Frase
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AT9283 Recent studies have elucidated a profound role for
2022-02-07

Recent studies have elucidated a profound role for FFA4 in modulation of metabolism and energy utilization as well as endocrine and immune function, and as a consequence, have thrust FFA4 to the forefront of drug discovery efforts. For example, activation of FFA4 by fatty AT9283 or synthetic ligands
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EPZ004777 FPR ligands comprise structurally very diverse cla
2022-02-07

FPR ligands comprise structurally very diverse EPZ004777 of compounds, ranging from naturally occurring peptides/proteins or “danger signals” such as PAMPs and DAMPs (see 1.1), respectively, to endogenous lipids and even various synthetic non-peptides, such as benzimidazoles, pyrazolones, pyridazin
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Potential roles for S P in
2022-02-07

Potential roles for S1P in angiogenesis, cancer, and autoimmune diseases such as RA have been reported [73]. In RA synoviocytes, S1P has been shown to enhance expression of prostaglandin E2 (PGE2) and cyclooxygenase-2 (COX-2) in response to the pro-inflammatory cytokines, TNF-α and interleukin (IL)-
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Several observations about structure activity
2022-02-05

Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic HU 308 class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage of
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In this study we also
2022-02-05

In this study, we also investigated the role of GST TMPyP4 tosylate in relation to ASD. In univariable analyses, where the role of each GST gene (i.e., GSTM1, GSTT1, GSTP1) was individually assessed, we did not observe any significant associations between the GST genotypes and ASD. In contrast, a p
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After initial validation of the ability
2022-02-04

After initial validation of the ability of Ad5-Cre virus to express Cre recombinase protein in glial cells in vitro and in vivo, we employed this virus to induce site-specific deletion of our target GlyT1 in the thalamus, through injection of the cKO GlyT1 mice. This transgenic line was constructed
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br Author s contributions br Conflict
2022-02-04

Author's contributions Conflict of interest Acknowledgements This work was supported in part by a grant from Department of Biotechnology (DBT), Government of India (Sanction Order No.: BT/563/NE/U-Excel/2016). MC, PDG and SKM acknowledge the Ministry of Human Resource and Development (MHRD)
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No specific inhibitor of KCC has
2022-02-03

No specific inhibitor of KCC has progressed to clinical trials, however, although compounds like H74 were shown to specifically target KCC over the related Na+-K+-2Cl− cotransporter (NKCC) (Ellory et al., 1990). This molecule, or its related analogues, represent compounds of promise. Simple Mg suppl
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Emergent studies have recently shown that Sherpas
2022-02-03

Emergent studies have recently shown that Sherpas living at high altitude have adaptations that make life at high altitude more compatible. Sherpas are known to have blood Hb concentrations about the same as lowlanders and Han populations [30]. This is different from what happens to lowlanders, Han
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Nemonapride Compound and several additional FPR antagonists
2022-02-03

Compound 10 and several additional FPR1 antagonists identified here specifically blocked fMLF-induced responses mediated via FPR1 in FPR1-HL60 Nemonapride and human neutrophils, but not responses mediated via FPR2 or FPR3 (in human neutrophils and transfected HL60 cells) or Fpr1 (murine neutrophils
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There are many histone H K demethylases including JMJD A
2022-02-01

There are many histone H3K9 demethylases, including JMJD1 A, JMJD2 A, JMJD2B, and JMJD2C (Kooistra and Helin, 2012). Considering that EPO Dextran sulfate sodium salt synthesis is regulated by hypoxia, we further analyzed several hypoxia-induced H3K9 demethylases, such as JMJD1 A, JMJD2B and JMJD2C
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br Glycoengineering br The Omics perspective
2022-02-01

Glycoengineering The « Omics » perspective The publication of the CHO-K1 genome sequence in 2011, followed by the publication of two Chinese hamster and six CHO cell line genomes in 2013, bring new opportunities in developing and engineering CHO Fmoc-L-Arg(Aloc)2-OH for improved glycoprotein
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br Acknowledgements br Introduction Obesity is a
2022-02-01

Acknowledgements Introduction Obesity is a growing pandemic, which becomes a global public health problem. The evidence has been readily available and mounting, demonstrating that obesity increases incidences of chronic comorbidities, such as non-alcoholic fatty liver diseases, diabetes, cardi
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To date types of glucose transport protein have been discove
2022-01-31

To date, 14 types of glucose transport protein have been discovered, each having its own specific functions with different distributions [33]. Among these, GLUT4 is particularly important for maintaining glucose metabolism homeostasis and insulin sensitivity, since it is involved in glucose transpor
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