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Moreover we have demonstrated that
2022-06-23

Moreover, we have demonstrated that internalization and subcellular trafficking of NPRA, using IF staining (IFS) and co-IP of plasma membrane, endosomal, lysosomal, and recycling endosome markers to follow intracellular trafficking and signaling by confocal IF microscopy (CIF) and immunoblotting (IB
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Molecular modeling of the sGC H NOX domain has
2022-06-23

Molecular modeling of the sGC H-NOX domain has placed the β1-domain Cys, β1-C78 and β1-C122, close to the heme binding pocket; specifically, the β1-C78 is placed diametrically opposite to β1-H105, the residue responsible for coordinating the heme iron [42,43]. β1-C78 is enclosed in a highly Miconazo
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Interestingly systemic circulating levels of NOx were not
2022-06-23

Interestingly, systemic circulating levels of NOx were not dramatically increased by treatment with isosorbide mononitrate or sodium nitrite at a dose which exerted beneficial effects on the progression of PH. In line with our results, Mathew et al. [13] demonstrated that the long-acting NO donor mo
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We recently reported that the
2022-06-23

We recently reported that the human-derived PancCa cell line PANC-1 and the human-derived hepatocellular HepG2 cell line express GPR55 mRNA and protein [21]. In PANC-1 and HepG2 cells, knockdown of GPR55 with specific siRNAs abrogates cellular uptake of Tocrifluor 1117, a selective GPR55 ligand [21]
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br Methods br Results br Discussion Our results show that
2022-06-23

Methods Results Discussion Our results show that the DRG and the spinal cord express significant amount of GPR35, a previously orphan Gi protein coupled receptor whose stimulation with zaprinast or with KYNA may reduce inflammatory pain. The receptor is also expressed in primary cultures of
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The amino hydroxy methyl isoxazolepropionic acid AMPA recept
2022-06-23

The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic TAK-875 (AMPA) receptors are related ionotropic glutamate receptors (iGluRs) that mediate fast excitatory neurotransmission, and are also typically heteromeric ion channels, composed of GluA2 subunits in conjugation with GluA1, GluA3, or GluA4 sub
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The typical pharmacophore for GPR agonists contains four par
2022-06-23

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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Introduction l Glutamate is a
2022-06-23

Introduction l-Glutamate is a major excitatory neurotransmitter in the mammalian central nervous system (CNS) that contributes not only to fast synaptic neurotransmission, but also to complex physiological processes like memory, learning, plasticity, and neuronal cell death [30], [81]. Glutamate is
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br Conclusions Temporally controlled disruption of Gcgr
2022-06-23

Conclusions Temporally-controlled disruption of Gcgr reveals a lack meaningful contribution to the improvement of glycemic control in insulinopenic conditions attributable to the intrinsic loss of GCGR signaling. On the other hand, these data highlight the importance of compensatory systems, incl
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Although the ramifications of non additive SAR are context d
2022-06-22

Although the ramifications of non-additive SAR are context-dependent, the knowledge that perturbations in one region of a chemical series are not synergistic with perturbations in another region of the same chemical series is clearly pertinent to any medicinal chemistry effort. In our experience, no
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Among sensitizers tested in the previous study six
2022-06-22

Among 22 sensitizers tested in the previous study, six test chemicals were pre- or pro-haptens (Nepal et al., 2018a). Among 6 chemicals, hydroquinone and 2-aminophenol, strong sensitizers, were falsely classified as non-sensitizers due to the lack of metabolic activation (Nepal et al., 2018a). Liter
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In this work we constructed a versatile platform
2022-06-22

In this work, we constructed a versatile platform based on MoS2-loaded molecular beacon(MB) and HCR for miRNA detection with high sensitivity and low-background. In this method, the G-quadruplex/Thioflavin T (THT) as fluorescent signal output, which possesses a variety of advantages, such as label-f
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Cryptochlorogenic acid In summary the SAR of a
2022-06-22

In summary, the SAR of a series of phenylpropanoic acid-free fatty Cryptochlorogenic acid receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded r
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Current studies have identified five orphan G protein couple
2022-06-22

Current studies have identified five orphan G protein-coupled receptors (GPCRs) that can be activated by free fatty acids (FFAs), GPR40, GPR41, GPR43, GPR84, and GPR120. Short-chain fatty acids (FAs) are specific agonists of GPR41 and GPR43 [21] and middle-chain FAs agonize GPR84 [22]. Long-chain FAs
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It has been shown that mice
2022-06-22

It has been shown that mice lacking SMAD2 in T cells do not develop spontaneous lymphoproliferative autoimmunity (Malhotra et al., 2010). Further, FOXO1 is known to activate proinflammatory MCP-1 and IL-6 (Ito et al., 2009). To this end, we also validated the downstream target FOXO1 and SMAD2 after
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