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GPR which is also known
2022-01-10
GPR40, which is also known as FFA receptor 1 (FFAR1 or FFA1), was identified as an orphan receptor in the search for novel human galanin receptor (GALR) subtypes in 1997. Using reverse pharmacology approaches measuring calcium transients, GPR40 were deorphanized and characterized as being activated
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Dual H H receptor antagonists developed by GlaxoSmithKline
2022-01-10
Dual H1/H3 receptor antagonists developed by GlaxoSmithKline have also reached clinical trials at various stages. These candidates are useful for alleviating the symptoms associated with allergic rhinitis(Daley-Yates et al., 2012). GSK-1004723, 4-[(4-chlorophenyl)methyl]-2-( (2R)-1-[4-(4- [3-(hexahy
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One of the key epithelium derived factors required
2022-01-10
One of the key epithelium-derived factors required to maintain immune tolerance in the intestine is Indian Hedgehog (Ihh). Ihh is secreted exclusively by intestinal epithelial cells, and signals in a paracrine manner to the inhibitory receptor Patched1 (Ptch1) on mitotic inhibitors in the mesenchy
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In addition for the function
2022-01-10
In addition, for the function of GSNOR in brain, since GSNOR is the sole alcohol dehydrogenase isozyme in brain, the failure to detect ethanol dehydrogenase activity poses a problem if it is assumed that this enzyme has evolved and developed as a protective mechanism for ethanol detoxification in th
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br Conclusions br Competing interests br Introduction Ethano
2022-01-10
Conclusions Competing interests Introduction Ethanol exposure has been linked to changes in the pattern of histone acetylation and deacetylation through histone acetyltransferases (HATs) and histone deacetylases (HDACs) in the Riluzole mg and in peripheral tissues, leading to ethanol depend
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Post translational ubiquitination has been shown to regulate
2022-01-07
Post-translational ubiquitination has been shown to regulate a wide range of cellular responses, such as the synaptic trafficking and turnover of neurotransmitter receptors (Rape, 2018). Ubiquitination is also engaged in the modification of protein-protein interaction and intracellular signaling tra
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The glucokinase protein sequence is most closely
2022-01-07
The glucokinase protein sequence is most closely related to the C-terminal domain of 100kD hexokinases, thus for glucokinase to evolve from a larger hexokinase ancestor it must have lost its N-terminal kinase domain. The genetic mechanism by which this occurred is currently unknown. Here we propose
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The in vivo biological activity of the four novel analogues
2022-01-07
The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent
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In the absence of HH ligand HH
2022-01-07
In the absence of HH ligand, HH signaling is actively maintained in a repressed state by the activity of the HH receptor Patched (PTCH). PTCH is a 12-transmembrane domain protein whose intracellular localization is concentrated at the racecadotril of the primary cilium, a single antenna-like structu
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Galanin a amino acid peptide was first isolated in
2022-01-07
Galanin, a 29/30-amino-acid peptide, was first isolated in 1983 from porcine intestine by Tatemoto and collaborators [70]. It is widely distributed throughout the central and peripheral nervous systems as well as other tissues. It is involved in a wide range of physiological functions, such as modul
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Consistent with our result Camacho
2022-01-07
Consistent with our result, Camacho-Barquero and coworkers showed that curcumin reduced phospho-P38 MAPK. P-38 MAPK is a key effector of several downstream factors that eventually modulate the homing of monocytic cells during the onset of intestine inflammation (Camacho-Barquero et al., 2007). Along
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Although it is well documented that FAAH substrates can
2022-01-07
Although it is well documented that FAAH substrates can elicit analgesic effects [for review see [47,48] and that systemic poly I:C administration induces mechanical allodynia in rats [14], to our knowledge this is the first study to demonstrate that enhancing FAAH substrate levels can modulate TLR3
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ricolinostat br Introduction The period around birth is a
2022-01-07
Introduction The period around birth is a risky time for stroke in infants. Ischemic stroke has been diagnosed in about 1/4000 full-term infants (Nelson and Lynch, 2004) and perinatal stroke represents the second most frequent cause of acute seizures in this age group (Levy et al., 1985). Further
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The H autoreceptors distributed mainly in the CNS act as
2022-01-07
The H3 autoreceptors distributed mainly in the CNS act as a negative feedback on histamine synthesis and release from histaminergic neurons. Histamine is involved in many physiological functions such as sleep-wake regulation, circadian and feeding rhythm, thermal regulation, locomotion, learning, co
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br Mechanism of HH pathway
2022-01-07
Mechanism of HH pathway activation in NSCLC Despite the role of the HH pathway in basal cell carcinoma and medulloblastoma, it has been postulated that epithelial tumors do not demonstrate cell autonomous HH ligand activity. The main evidence comes from the study by Yauch et al showing no correla
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