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br Conflict of interests br
2021-10-15
Conflict of interests Acknowledgements This work was supported by the National Institutes of Health grants HD058577 and ES01678 to Kirill Kiselyov. We thank Sreeram Ravi for technical support. We also thank Mike Myers at the University of Pittsburgh Cancer Institute Flow Cytometry Facility.
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Sometime ago we have described diamino
2021-10-15
Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by JNJ 5207852 dihydrochloride and zymosan. In this work we
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Apoptosis is one of critical toxic mechanisms of
2021-10-15
Apoptosis is one of critical toxic mechanisms of benzene metabolites. In this work, overexpression of HIF-1a could significantly reduce the increase in cell apoptosis caused by 40 μM BQ. At the meanwhile, anti-apoptotic protein Bcl-2 level was significantly elevated in HIF-1a overexpression cells th
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It has been demonstrated that HO inhibits
2021-10-15
It has been demonstrated that HO-1 inhibits the production of proinflammatory mediators including TNF-α and IL-6 in response to sepsis [35], and the expression of iNOS and COX-2 [36,37]. An inverse association between HO-1 and iNOS has previously been described: the NO levels decline with increases
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It is difficult however to assure that observed alterations
2021-10-15
It is difficult, however, to assure that observed alterations of pro-oxidant/antioxidant levels within the studied organisms are related directly to heavy metal pollution, rather than to other accompanying environmental stressors. Environmental factors like oxygen partial pressure, temperature, sali
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In conclusion this is the first description of a
2021-10-15
In conclusion, this is the first description of a GPR81 agonist with an ability to exert in vivo efficacy without causing flushing. These results demonstrate that GPR81 small-molecule agonists may be effective for treating dyslipidemia. In addition, targeting GPR81 could prevent the unwanted side ef
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The physiological and pharmacological roles of GPR remain la
2021-10-15
The physiological and pharmacological roles of GPR81 remain largely unclear because of several reasons. The low potency of lactate agonizing GPR81 in the millimolar range, together with its fast metabolic turnover, renders as a challenge in in vivo studies using lactate. Furthermore, there are no po
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To further implicate the role of EAAT in
2021-10-15
To further implicate the role of EAAT3 in morphine-induced place preference, the effects of morphine on EAAT3 dofetilide was determined. Interestingly, morphine increased EAAT3 protein expression in the plasma membrane of mPFC, nucleus accumbens and VTA but not in the hippocampus of wild-type mice
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Introduction Glucose dependent insulinotropic polypeptide GI
2021-10-15
Introduction Glucose-dependent insulinotropic polypeptide (GIP) is a hormone secreted postprandially from enteroendocrine K cells in response to ingestion of either fat [1], protein [2], or carbohydrates [3]. GIP is primarily known for its glucose-dependent insulinotropic actions mediated via the G
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This study compared PMS ascorbate and
2021-10-15
This study compared PMS+ascorbate and t-BHP in terms of their effects on the volume-dependent parameters of normal human RBCs. Incubation with both oxidative systems resulted in the RBC density and osmotic resistance distribution shifts. Clotrimazole or Са2+ added into the medium, as well as high ex
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We are aware that the
2021-10-15
We are aware that the classical biochemical view is centered on the local concentrations of specific ion and molecules rather than on cell electric potentials. However, important downstream processes can be influenced by acting locally on these potentials because they regulate the conductance of the
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Two excellent GSMs with clear pharmacological
2021-10-14
Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas
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GLP is released in response
2021-10-14
GLP-1 is released in response to ingestion of nutrients including carbohydrates, protein, and fat. Recent studies aimed at identifying the receptors involved in nutrient stimulated GLP-1 secretion have identified free fatty Endoxifen synthesis receptor 4 (FFA4/GPR120) as a potential 7TM receptor in
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The Ala to Leu substitution would
2021-10-14
The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several
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At the molecular level AZ scaffold
2021-10-14
At the molecular level AZ scaffold proteins including piccolo and bassoon have been shown to directly or indirectly associate with endocytic and actin-binding proteins such as ABP1 (Fenster et al., 2003), profilin, and GIT (Podufall et al., 2014) (Fig. 2B). ABP1 and profilin, via regulating F-actin,
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