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Notably we observed that GPR
2021-12-01
Notably, we observed that GPR35 activation induced by PA, an in vivo GPR35 agonist [6], significantly decreased DAI, colon weight, and histological score, while increasing colon length in mice with DSS-induced colitis. Furthermore, fibronectin and integrin α5 were co-localized with GPR35 on the colo
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br Experimental br Acknowledgments The
2021-12-01
Experimental Acknowledgments The authors are grateful to Fundamental Scientific Research Fund of Chinese Academy of Medical Sciences (No. 2016ZX350030) for financial support. Introduction 2-Lysophosphatidylcholines (1-acyl-glycero-3-phosphocholines, 2-LPC) are blood derived factors involve
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Previous studies have demonstrated that cannabinoid potentia
2021-11-30
Previous studies have demonstrated that cannabinoid potentiation of GlyR α3 subunits contributes to cannabinoid-induced analgesia. For instance, Dehydroxylcannabidiol (DH-CBD), a chemically modified cannabinoid, can alleviate acute pain and chronic inflammatory pain by targeting spinal α3 GlyRs (Xio
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Entry into CNS is tightly regulated by highly dynamic barrie
2021-11-30
Entry into CNS is tightly regulated by highly dynamic barriers, namely, the BBB, the blood-CSF barrier, and the arachnoid epithelium (Abbott et al., 2010; Yasuda et al., 2013). Similar barriers also exist within the CNS including the ependymal barrier as well as the cellular membrane barriers of the
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br Ca influx through glutamate receptors is thought to
2021-11-30
Ca2+ influx through glutamate receptors is thought to play a critical role in synaptogenesis and in the formation of neuronal circuitry during early development[45]. Because AMPA receptors might contribute to these processes, particularly at times and in cells in which NMDA receptor expression is
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So in this study our results firstly demonstrated that i
2021-11-30
So in this CRT0044876 study, our results firstly demonstrated that i.c.v. injection of ghrelin(1–7)-NH2 played a significant role in the modulation of the acute heat pain at the supraspinal level in mice. Our results showed that i.c.v. injection of ghrelin(1–7)-NH2 produced dose- and time- dependent
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Recently they reported an enyne chemotype agonist Fig with
2021-11-30
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral Dehydrocostus Lactone (tmax=15min) and a decent pharmacokinetic
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Hardy et al had demonstrated
2021-11-30
Hardy et al. had demonstrated the role of GPR40 in mediating the proliferative effect of the FFA oleate's in breast cancer cells, and found that such effect can be reversed by silencing of GPR40 [14]. Similarly we have observed that inhibition of GPR40 function by its antagonist GW1100 inhibited cel
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br Acknowledgments This research was supported by the Nation
2021-11-30
Acknowledgments This research was supported by the National Institutes of Health Grants GM58442 and GM084152, as well as the National Institutes of Health Predoctoral Training Grant 5T32GM008700-13. We thank Eric Oldfield (University of Illinois, Urbana-Champaign) for providing the FDPS inhibitor
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they have to say Several other assay parameters were also ex
2021-11-30
Several other assay parameters were also explored. First, the thermal dependence of the assay was investigated by measuring the specific activity at different temperatures (Fig. 7). That data show that enzymatic activity increases with increasing temperature. Interestingly, the observed rate increas
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Although epigenetic mechanisms are implicated in the
2021-11-30
Although epigenetic mechanisms are implicated in the pathogenesis of hematopoietic malignancies, little is known about the role of lysine-specific histone demethylases and whether manipulation of these enzymes can be translated into targeted therapies. KDM6A is the most frequently mutated histone de
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br Introduction Circulating tumor cells CTCs are
2021-11-30
Introduction Circulating tumor NFAT Inhibitor (CTCs) are cancer cells that have invaded blood vessels or lymphatics and are carried around the body by the blood. CTCs constitute potential seeds for metastasis because they can reach and implant into distant organs. The clinical importance of CTCs
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br Parkinson disease Idiopathic PD is a hypodopaminergic mov
2021-11-30
Parkinson disease Idiopathic PD is a hypodopaminergic movement disorder of uncertain etiology that affects 3% of persons over age 65 (Dexter and Jenner, 2013). Cardinal signs of this common neurodegenerative condition include bradykinesia, rigidity, rest tremor and postural instability. Autonomic
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HOs can be found in
2021-11-30
HOs can be found in both plants and animals and they are evolutionarily conserved proteins [8]. There are two HO isoenzymes: inducible heme oxygenase-1 (HO-1) and constitutive heme oxygenase-2 (HO-2) encoded by different genes [9,10]. Biosynthesis of a stress-inducible HO-1 can be triggered by a var
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br Conflict of interest statement br Introduction The Hedgeh
2021-11-30
Conflict of interest statement Introduction The Hedgehog (Hh) family of secreted protein signals patterns many tissues and structures during embryogenesis (Chiang et al., 1996, Dessaud et al., 2008, Ingham, 1993) and, post-embryonically, governs tissue homeostasis and regeneration by regulatin
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