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While published data around the functional significance
2022-07-15

While published data around the functional significance of GPR84 are quite sparse, details of signaling pathways initiated by the receptor are even more limited, including in recombinant systems. In recombinant cells, GPR84 activation reportedly leads to Gi pathway activation, resulting in pertussis
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Finally LC ESI MS MS was applied to explore
2022-07-15

Finally, LC-ESI-MS/MS was applied to explore the effects of increased fT4 levels 4 and 8 weeks after induced thyrotoxicosis and have revealed an upregulation of proteins involved in blood coagulation, thus providing a clear association [126]. Conclusions Introduction Diabetes mellitus (DM) ha
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Clotrimazole br Methods br Results br Discussion Our
2022-07-15

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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br GPR is a class A GPCR expressed
2022-07-15

GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine Compstatin which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated β-cell
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br TGR agonists current developments and future landscape Th
2022-07-15

TGR5 agonists: current developments and future landscape The amphipathic nature of bile acids is crucial in aiding the digestion and bromophenol blue of vitamins and fats. With the emerging roles of bile acids in the regulation of energy and glucose homeostasis through TGR5, the pharmaceutical i
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2-MeOE2 Elevated methylglyoxal levels also contribute to car
2022-07-15

Elevated methylglyoxal levels also contribute to carbonyl stress, cytotoxicity, DNA damage, apoptosis and cell death. These mechanisms may be important for normal aging of the nervous system as well as for the development of neurodegenerative diseases such as Alzheimer's and Parkinson's disease wher
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br Ca influx through glutamate receptors
2022-07-14

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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Introduction Glucocorticoids are released in
2022-07-14

Introduction Glucocorticoids are released in response to stress and play an important role in inflammation, cellular growth, development, body fluid homeostasis, carbohydrate, lipid, and protein metabolism. However, circulating glucocorticoid excess has been associated with a classical phenotype of
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br Materials and methods br Conflicts of interest Some
2022-07-14

Materials and methods Conflicts of interest Some of the peptidomimetic compounds in this work are the subject of the patent application “Peptidomimetics for Imaging the Ghrelin Receptor”, WO/2016/191865 A1, December 8th, 2016. Acknowledgements Special thanks go to Rebecca McGirr (Lawson He
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tetraethylammonium The overall very satisfactory potency pro
2022-07-14

The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic tetraethylammonium core in order to improve affinity to FFA1. The agonist activity in this series appears to be particu
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94 8 However the clinical development of was terminated in d
2022-07-14

However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this rece
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Introduction High mobility group box HMGB is a nuclear prote
2022-07-14

Introduction High mobility group box 1 (HMGB1) is a nuclear protein that plays a fundamental role in the regulation of DNA-associated events such as DNA repair, transcription, and replication. HMGB1 can be translocated to the cytosol, plasma membrane, and extracellular space in response to various
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Collectively these observations demonstrate that FAAH is fun
2022-07-14

Collectively, these observations demonstrate that FAAH is functionally positioned to modulate the actions of AEA and other NAEs on BLA neurons and anxiety processes mediated by this region. By extension, manipulations that lead to alterations in FAAH activity, such as stress or administration of com
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It is well known that TLR induced
2022-07-14

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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Our understanding of the genetic basis of myeloid
2022-07-14

Our understanding of the genetic basis of myeloid malignancies has been profoundly improved in recent years. Studies have revealed new recurrent somatic mutations in myeloid malignancies, including myeloproliferative neoplasms (MPNs), myelodysplastic syndrome (MDS) and acute myeloid leukaemia (AML).
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