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D appears to be important
2022-09-15
D83 appears to be important for receptor function as a mutation to an alanine produced a non-functional channel. Interestingly, maintaining the charge as in D83E produced only a small reduction in GABA sensitivity. Other mutations at this position which included residues capable of hydrogen bonding
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br FXR expression in normal
2022-09-15
FXR Anhydrotetracycline hydrochloride in normal intestine and cancer Of note, there are several question marks about FXR post-translational modifications (such as acetylation or SUMOylation) and their involvement in the pathogenesis of metabolic and inflammatory disease (Balasubramaniyan et al.,
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Studies of human and mouse GPR as ascertained by mRNA
2022-09-15
Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infla
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Active compounds and were further tested and EC and pEC
2022-09-15
Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of
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To meet the requirement of ferroptosis
2022-09-15
To meet the requirement of ferroptosis-based therapy, a couple of small molecule drugs and nanomaterials were introduced to the design of ferroptosis inducers, separately. As we know, iron is a key regulator of ferroptosis. When small molecule drugs are employed to induce ferroptosis, the endogenous
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We also evaluated the effect of varying ionic str http
2022-09-15
We also evaluated the effect of varying ionic strength. These experiments included previously characterized H3 (residues 1–21) and SNAIL (residues 1–9) peptides [8], [34] to allow a comparative analysis with different ligands (Fig. 1A). As shown in Fig. 2 and listed in Table 2, it is evident that a
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One important aspect about GSK inhibitors is their effect on
2022-09-09
One important aspect about GSK-3 inhibitors is their effect on pluripotency of Cyclopiazonic acid receptor [4]. Many GSK-3 inhibitors are ATP-competitive and suppress both GSK-3alpha and GSK-3beta [476]. BIO was shown to suppress GSK-3 activity and promote Wnt/beta-catenin signaling. This combinati
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GPR is present primarily in the
2022-09-09
GPR119 is present primarily in the pancreas and the intestine. Activation of GPR119 increases insulin, GLP-1, GIP and PYY secretion. GPR119 agonists stimulate insulin release in a glucose-dependent manner. The glucose dependent insulin secretion (GIDS) mechanism makes GPR119 an attractive target for
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To further explain the energy differences between Group A an
2022-09-09
. To further explain the energy differences between Group-A and Group-B, the average distances between ligands and the zinc cation were obtained from the last 1ns trajectory. It turns out that the members of group A were within the coordination distance of the zinc ion, whereas those of group B stay
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In Locusta migratoria a worldwide agricultural pest
2022-09-09
In Locusta migratoria, a worldwide agricultural pest, we previously identified 51 CPRs containing eight endocuticle structural glycoproteins, which are homologs of SgAbd-1, SgAbd-2, SgAbd-3, SgAbd-4, SgAbd-5, SgAbd-6, SgAbd-8, and SgAbd-9 in the adult desert locust, Schistocerca gregaria [17,26]. Al
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To further investigate the molecular mechanisms that underli
2022-09-09
To further investigate the molecular mechanisms that underlie glycine's β-cell protective effects through its antioxidative activity in diabetes, we used a H2O2/high glucose-induced apoptosis cell model. Similar effects on ROS generation of high glucose and H2O2 support the in vivo results, suggesti
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Bergmann glia cells BGCs are the most abundant glia
2022-09-09
Bergmann glia EIPA (BGCs) are the most abundant glia cells in the cerebellum, comprising more than 90% of the cerebellar glia. These cells span the entire cerebellar molecular layer and encapsulate neuronal somata, dendrites and axons. BGC are involved in neurotransmitter uptake, K+ homeostasis and
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The association between mental disorders and smoking was fir
2022-09-09
The association between mental disorders and smoking was firmly established, and their inter-relationship was due to the reciprocal causal effects (Tjora et al., 2014). Previous research found that negative affect and the urge to smoke as well as the urge to smoke and nicotine dependence had signifi
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pHi regulation in astrocytes has
2022-09-09
pHi regulation in astrocytes has been examined primarily in cell culture rather than in situ. Two HCO3−-dependent transporters, NBC and Na+-driven Cl-HCO3 exchange (NDCBE), have been described [10,16], in addition to Cl-HCO3 anion exchange (AE) [96]. Culture studies indicate that NHE is the principa
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This work was supported by the
2022-09-09
This work was supported by the National Natural Science Foundation of China (Grants 81471101 and 81870852), the Natural Science Foundation of Jiangsu Province (Grant BK20181146), the Natural Science Foundation of the Jiangsu Higher Education Institutions of China (Grants 18KJA320007 and 17KJB320018)
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