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After establishing improved GSNOR potency some of the
2022-04-16
After establishing improved GSNOR potency, some of the potent inhibitors were further evaluated for microsomal stability and CYP inhibition studies (). Majority of the tested analogs revealed high metabolic stability in human and rat liver microsomes, and moderate to low stability in mouse liver mic
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The observed glucose intolerance and elevated fasting blood
2022-04-16
The observed glucose intolerance and elevated fasting blood glucose in this study is in consonance with earlier study (Ferris and Kahn, 2012). These have been the common features of GC exposure and are not unexpected. Previous researches that reported IR during GC exposure have shown controversy con
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In conclusion this is the first description
2022-04-16
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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Canagliflozin br Materials and methods br Results br Discuss
2022-04-16
Materials and methods Results Discussion GPR35 expression has been identified within discrete regions of the nervous system, including the spinal cord [[43], [44], [45], [46], [47], [48]]. Importantly, GPR35 is expressed not only in neurons but also in spinal glial cells [43]. Unfortunately
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DOI hydrochloride GPR levels were not changed by any treatme
2022-04-16
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 fatt
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It appears that not all GPR agonists require a
2022-04-16
It appears that not all GPR119 agonists require a high dose to elicit acceptable 279 3 control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved by 30mg/kg sitaglipt
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LPC OMe LPC LPC and OMe LPC were
2022-04-16
LPC 14:0, 2-OMe-LPC 14:0, LPC 16:0 and 2-OMe-LPC 16:0 were shown to be most potent stimulators of intracellular calcium flux in the β cell model, which is one of key processes leading to insulin exocytosis. Yet, species with myristoyl residue initiate calcium influx through voltage-gated L002 where
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Dendritic damage and loss of synaptic connections correlate
2022-04-16
Dendritic damage and loss of synaptic connections correlate with cognitive decline in HAND patients. Synapse loss induced by HIV proteins occurs early and via a different signaling pathway from that leading to neuronal death (Kim et al., 2008), suggesting that synapse loss might be a mechanism to re
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br Acknowledgments br Introduction Oocyte donation has
2022-04-16
Acknowledgments Introduction Oocyte donation has increasingly been used as an option for infertile women with preserved ovarian function but expected poor outcomes, e.g. low responders to standard ovarian stimulation and women who have experienced repeated implantation failure. Transfer of emb
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Interestingly mGlu and mGlu receptors differ notably by
2022-04-15
Interestingly, mGlu2 and mGlu3 receptors differ notably by their cellular distribution. Whereas mGlu2 receptors are mostly neuronal, mGlu3 receptors are expressed both in glia and in neurons. In neurons, mGlu3 receptors are present at the post-synapse and in presynaptic elements (Tamaru et al., 2001
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Epinephrine responses to hypoglycemia are probably
2022-04-15
Epinephrine responses to hypoglycemia are probably triggered centrally, perhaps with input from peripheral hypoglycemia sensing [3], [4]. We observed increased epinephrine responses in GCK-MODY and I366F diabetic mice. Consistent with a role for except GCK in detecting a low blood glucose, we also s
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LbGlcK and the HsHxKIV d glucose
2022-04-15
LbGlcK and the HsHxKIV-d-glucose complex (PDB entry 3IDH) [17] were superimposed from individual subunits. The active site regions revealed the key toll like receptor binding residues to be present for LbGlcK; also, the superposition showed that HsHxKIV had residues that were absent in LbGlcK, such
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Phylogenetic trees of receptors for peptides similar to gluc
2022-04-15
Phylogenetic trees of receptors for peptides similar to glucagon from diverse vertebrate species typically are similar to the tree presented in Fig. 3 (Sivarajah et al., 2001, Chow et al., 2004, Irwin and Wong, 2005, Cardoso et al., 2005, Cardoso et al., 2006, Ng et al., 2010, Park et al., 2013, Hwa
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It is notable that pharmacological or genetic inhibition of
2022-04-15
It is notable that pharmacological or genetic inhibition of GCGR signaling results in the engagement of a number of compensatory mechanisms that potentially impact glucose control. These include alpha-cell hyperplasia [2], [11], [12], [13] and increased beta-cell proliferation under low insulin cond
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br Acknowledgments The authors gratefully acknowledge the
2022-04-15
Acknowledgments The authors gratefully acknowledge the support provide by National Natural Science Foundation of China (Number 31301415). Introduction β-Galactosidases (EC 3.2.1.23), frequently known as lactases, are widely used in lactose hydrolysis. This disaccharide is present in mammalian
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