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In the present study we showed that reduced neuron formation
2022-03-15

In the present study, we showed that reduced neuron formation in vitro induced by IL-1β was ameliorated by activation of GPR55 in both human and mouse cultures of NSCs. Pre-treatment with GPR55 agonists also blocked upregulation of inflammatory cytokine receptor mRNA (IL-1R1, IL-6st) while increasi
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Strengths The primary feature of GPR agonists resides
2022-03-15

Strengths The primary feature of GPR119 agonists resides in their dual mechanism of action in regulating blood glucose 1, 2, 3, 15. GPR119 agonists stimulate GLP-1 release from intestinal L Busulfan as well as glucose-dependent insulin secretion and insulin promoter activity enhancement in pancreat
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Acknowledgments We would like to thank Dr Greg Morriello
2022-03-15

Acknowledgments We would like to thank Dr. Greg Morriello, Mr. Lehua Chang, Mr. Chris Moyes and Mr. Nam Fung Kar for intermediate 3 syntheses. Cheng Zhu would like to thank Dr. Milana Maletic, Mr. Kake Zhao and Mrs. Wanying Sun for helpful discussions. Introduction Glucagon-like peptide-1 (GLP-
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KPT-9274 mg Active compounds and were further tested and EC
2022-03-14

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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br GluR A knockout mice
2022-03-14

GluR-A knockout mice Genetically modified, adult mice lacking the GluR-A AMPA receptor subunit exhibit fast synaptic transmission in the hippocampus, mediated by the receptors formed from the remaining AMPA receptor subunits GluR-B and GluR-C (Sommer et al., 1991), but are deficient in a rapidly
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Although encoded by a single gene GR displays considerable h
2022-03-14

Although encoded by a single gene, GR displays considerable heterogeneity through the combined effects of alternative mRNA splicing, alternative translation initiation, and complex post-translational modification. Differential expression of the various GR isoforms may contribute to tissue-specific f
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Here we used chemogenetic modulation of MBH GHSR
2022-03-14

Here, we used chemogenetic modulation of MBH GHSR neurons to address the role of the endogenous ghrelin system in the normal, hyperphagic response to a short-term fast. Studies demonstrating the requirement of an intact ghrelin-GHSR system for the rebound food intake following fasting have been inco
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br Conclusion In summary a series of novel GPR
2022-03-14

Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic Cyprodime hydrochloride motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist poss
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br PEPCK This enzyme decarboxylates
2022-03-14

PEPCK This enzyme decarboxylates and then phosphorylates oxaloacetate to form phosphoenolpyruvate (PEP) in the second step of gluconeogenesis after the carboxylation of pyruvate catalyzed by PC. PEPCK1 (PEPCK-C, encoded by the PCK1 gene) and PEPCK2 (PEPCK-M, encoded by the PCK2 gene) are two isof
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br Materials and methods Patients charts were
2022-03-14

Materials and methods Patients’ charts were reviewed retrospectively, and 165 consecutive patients (82 with cancer and 83 without cancer) who either started edoxaban (Lixiana®, Daiichi-Sankyo, Tokyo, Japan) therapy for the treatment of VTE or were switched from other oral anticoagulants to edoxab
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EMD638683 receptor Another important question for future
2022-03-14

Another important question for future studies will be whether FAAH inhibitors work to normalize impairments in fear extinction that are known to be produced by environmental insults such as exposure to abused drugs and stress 97, 103. Indeed, several authors have posited utility of FAAH inhibitors f
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In spite of decades of research the mechanisms
2022-03-14

In spite of decades of research the mechanisms of SV endocytosis and recycling remain controversial. Accumulating evidence suggests that SV endocytosis occurs by more than one mechanism (e.g. clathrin-independent endocytosis, clathrin-mediated endocytosis, bulk endocytosis; reviewed in (Dittman and
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The root of Danshen has been
2022-03-14

The root of (Danshen) has been widely used as traditional Chinese medicine for many years and shown to exhibit significant pharmacological activities for a variety of human diseases including cancers. Tanshinones, the major active components, belong to a group of an abietane-type diterpenes contain
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individuals with variants in the codon region
2022-03-14

13 individuals with variants in the codon 1031–1159 region had global developmental delay and apparent ID, ranging from speech delay and learning difficulties to markedly impaired basic life functions (Table 2 and Table S3). The last available occipitofrontal-circumference measurements revealed micr
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In NAFLD models the first hit is
2022-03-14

In NAFLD models, the “first hit” is liver fat accumulation, which causes insulin resistance, whereas the interplay of inflammatory cytokines, which causes inflammation, acts as the representative “second hit” [9]. However, recently, the “multiple hit” hypothesis has taken into consideration that mul
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