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KPT-9274 synthesis br Materials and methods br Results br Di
2021-09-17
Materials and methods Results Discussion In this study, we demonstrated that zaprinast (a cGMP-PDE inhibitor) induced the intracellular calcium mobilization in the KPT-9274 synthesis coexpressing GPR35 and Gqi5, Gqo5, or Gα16. Induction of intracellular calcium mobilization by zaprinast in
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Compounds and were tested for
2021-09-17
Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion at bo
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In the present study we aimed to investigate
2021-09-17
In the present study, we aimed to investigate the effect of a common dairy and beef genetic background on the mRNA kainic acid of the AdipoQ system and GPR109A in different adipose depots and liver. Materials and Methods Results Comparing fat masses between families (fat-type vs. lean-type c
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Additionally OsGly I overexpressing transgenic rice plants h
2021-09-17
Additionally, OsGly I-overexpressing transgenic rice plants had higher grain yields than WT (Table 2). Although there were no significant differences in the number of effective panicles per plant, panicle length, grain numbers per panicle, or 1000-grain weight between WT and transgenic plants, the s
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Overall ABC transporters are hypothesised to prevent the
2021-09-17
Overall, ABC transporters are hypothesised to prevent the penetration of AEDs and other pharmacological compounds into the brain, being a hurdle for therapeutic delivery in neurological diseases. DRE is thought to be in part related to an increased expression of efflux transporters in the BBB, altho
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Fatty acids have been repeatedly shown to
2021-09-17
Fatty acids have been repeatedly shown to increase the responsiveness of pancreatic islets to glucose both in vitro and in vivo[6]. The recent identification of GPR40 as a receptor for free fatty acids that is localized to the pancreatic islet cells has therefore stimulated interest in obtaining sma
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Congenital Gcgr mice exhibit increased hepatic
2021-09-17
Congenital Gcgr mice exhibit increased hepatic Fgf21 expression and circulating FGF21 levels. Previous studies by other investigators demonstrated that neutralization of circulating FGF21 with specific BS-181 impairs glucose control in these mice [6]. In addition, the FGF21 analog LY2405319 lowers
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Moreover we examined inhibition of GLI
2021-09-17
Moreover, we examined inhibition of GLI-mediated mRNA expression by 1. Colubrinic SP2509 (1) inhibited the mRNA production of PTCH in PANC1 cells in the dose-dependent manner. This result clearly shows 1 inhibits GLI-mediated transcription (Fig. 6). Discussion In this study, we identified three
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The ghrelin receptor is expressed in
2021-09-17
The ghrelin receptor is expressed in a number of human malignancies including prostatic carcinoma cell lines [18,19] and tissues [20], breast carcinoma tumours and cell lines [21], testicular tumours [22], and malignant ovarian cysts and tumours [23]. In addition, it has an elevated level of express
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br Materials and methods br Results
2021-09-17
Materials and methods Results and discussion Conclusion Altogether, our data provide an unexpected insight into Cx26 trafficking pathway and gap junction assembly in the cochlea. Since many of the disease-causing mutations in GJB2 impair the trafficking and delivery of Cx26 to the cell surf
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To improve the preferential GalR binding
2021-09-17
To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollenb
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Most of the above mechanisms are implicated
2021-09-17
Most of the above mechanisms are implicated in attenuation of myocardial I/R injury. However, the role of GalR2 receptor activation in cardioprotection remains unclear because of the lack of receptor subtype selectivity of peptides G2 and G3. It has been shown that Ala5-galanin (2–11) (G4) has a hig
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br Acknowledgements This work was supported
2021-09-17
Acknowledgements This work was supported under the National Natural Science Foundation of China (Grant numbers 31200576, 21472197, 21675162), Beijing Natural Science Foundation (Grant No. 7182189), and Project supported by the Joint Funds of the National Natural Science Foundation of China (Grant
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Inflammasomes are multimeric protein complexes involved in t
2021-09-17
Inflammasomes are multimeric protein complexes involved in the host defense protecting activity against invading pathogens and in physiological aberrations such as cancer and auto-inflammatory, metabolic, and neurodegenerative diseases. Inflammasomes induce the inflammatory process by triggering the
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Hydantoin in region F bridging the
2021-09-17
Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR,
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