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The experiments indicate that a major component of the vasod
2022-04-14
The experiments indicate that a major component of the vasodilatation is due to antagonism of α 1-adrenoceptors. Evidence for α1-adrenoceptor antagonism is that vasodilatation was observed in WP1066 preconstricted with α1-adrenoceptor agonists, phenylephrine or methoxamine, but not in vessels precon
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Similarly spectrophotometric titrations were carried
2022-04-13
Similarly, spectrophotometric titrations were carried out under conditions identical to those used for the fluorescence titrations. exhibited a predominant Epinephrine HCl band at around 493 nm. The titrations with all G-quadruplex DNAs resulted in a hypochromic effect along with a bathochromic sh
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br Experimental br Results and discussions br Conclusion br
2022-04-13
Experimental Results and discussions Conclusion Notes Introduction The noncanonical DNA structures that is, i-motif [[1], [2], [3], [4], [5], [6], [7], [8], [9]] and G-quadruplex [[10], [11], [12], [13], [14]] have recently been carefully studied using either experimental or computati
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FXR agonists represent an attractive class of drugs
2022-04-13
FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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On the other hand histone deacetylase
2022-04-13
On the other hand, histone deacetylase inhibitors can accelerate inflammation resolution by promoting the externalization of AnxA1, a main ALX/FPR2 agonist, with concomitant inhibition of cytokine gene expression in mouse macrophages [30]. Thus, our present results provide an additional mechanism,
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It is well known that TLR induced
2022-04-13
It is well known that TLR4-induced inflammation is associated with behavioural alterations including fever, hypolocomotion, altered appetite, anxiety and anhedonia (Dantzer, 2006, Dantzer et al., 2008). The current data demonstrate that while PF3845 potently attenuates TLR4-induced cytokines in the
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A complimentary approach with Per Luc
2022-04-13
A complimentary approach with Per2:Luc Argatroban exposed to hypoxia as well as with mBmal1:Luc circadian reporter cells in which we overexpressed variants of HIF-1α and HIF-2α revealed that hypoxia and HIFs can not only shorten the period but also decrease the amplitude of the clock (Figures 2 and
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HOs can be found in both plants and animals and
2022-04-13
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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In our study SHH protein overexpression was significantly as
2022-04-13
In our study, SHH protein overexpression was significantly associated with lymph node metastasis which is in agreement with the study done by Marechal et al. wherein they have reported that SHH is a prognostic biomarker in PDAC and high levels correlate with lymph node metastasis (Maréchal et al., 2
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Compound containing dimethylglutarimide P cap P propyl
2022-04-13
Compound containing, dimethylglutarimide P-cap, P propyl group, α-methylbenzyl urea resulted in inhibitor with much improved binding (=0.064μM) and EC=0.3μM. This was an aza-peptide analog with an EC comparable to our first generation clinical candidate . Analog was evaluated for its selectivity
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NPxY was recognized as the first short signal sequence
2022-04-13
NPxY was recognized as the first short signal sequence motif in the cytoplasmic domain of membrane receptors and proteins with critical roles in internalization and trafficking of receptor molecules [130]. Including LDL receptor, beta-1 integrin, megalin, beta-amyloid precursor protein, EGF receptor
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GPR levels were not changed by any treatment
2022-04-12
GPR40 levels were not changed by any treatment. GPR40 has the same agonists as GPR120 but only a 10% homology [35] despite using the same intracellular signaling cascades [7]. Previous data on the ability of exercise to modulate G protein coupled receptors in general are scarce. The long-chain fatty
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br GPR is a class A
2022-04-12
GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine Missed Opportunities which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediat
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In order to elucidate the mechanisms behind
2022-04-12
In order to elucidate the mechanisms behind the observed changes in metabolic activity in the cardiomyoblasts we investigated changes in gene and protein expression subsequent to treatment with PSN632408 with or without concurrent exposure to palmitate. Activating GPR119 in basal and high palmitate
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While NR upregulation in the spinal cord is
2022-04-12
While NR1 upregulation in the spinal cord is known to contribute to pathological pain [7], [22] and furthermore, NR1 expression in the spinal cord has been shown to be reduced by continuous administration of the GlyT1-inhibitor ALX5407 [23], little is known about possible expressional changes of NR1
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