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Compounds were tested for GPR activity in a functional assay
2021-10-28

Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO FAK Inhibitor 14 transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure act
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During the course of our optimization of
2021-10-28

During the course of our optimization of the diarylsulfonamide chemotype as FFA4 agonists, we identified xanthene as a potent and selective antagonist of FFA4 (). Xanthene was able to block the agonist induced intracellular Ca response elicited by both linoleic 543 synthesis and compound in comp
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br Author contributions statement P N Y designed
2021-10-28

Author contributions statement P.N.Y. designed the study, analyzed the data and prepared the draft of the manuscript. C.S performed the experiments, analyzed the data and generated Fig. 1, Fig. 2, Fig. 3, Fig. 4, Fig. 5, Fig. 6, Fig. 7, Fig. 8. A.K. and S.D. made Supplementary Figs. S1 and S2. D.
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With the aim to identify potential novel targets in CVD
2021-10-28

With the aim to identify potential novel targets in CVD, we applied proteome analyses on vascular tissue of these frequently used mouse models of atherosclerotic disease in the presence and/or absence of diabetes. Potential targets for intervention identified with this approach were validated in hum
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Over recent decades there were three breakthroughs
2021-10-27

Over recent decades, there were three breakthroughs of high intensity heavy-ion acceleration [6]. The first is the invention of radio frequency quadrupole (RFQ) type accelerator, which could accelerate more than dozens of milli-ampere ion beams and is a good solution to space-charge-effect of heavy-
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br Discussion Naloxone and CTAP were
2021-10-27

Discussion Naloxone and CTAP were able to alter the febrile response induced by gp120. This effect was particularly evident during the initial hours following gp120 administration (90–210min). We also investigated the potential role of the delta-2 opioid receptor in gp120-induced fever. The delta
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During the structural transition the FD
2021-10-27

During the structural transition, the FD, the PHD and the TrD retain their tertiary structure. Nevertheless, they undergo large rearrangements in their relative orientation due to secondary changes in hinge segments (R1 to R5) which refold during the low-pH induced conformational change. Particularl
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br Materials and methods br Results br Discussion br Acknowl
2021-10-27

Materials and methods Results Discussion Acknowledgments Introduction As we move into an aging society, there has been a growing interest in neurological disorders [1]. Neurodegenerative diseases such as Parkinson’s disease (PD) and Alzheimer’s disease (AD) cause cognitive malfunction
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Studies have shown that coexpression of the
2021-10-27

Studies have shown that coexpression of the HAC1 gene in P. pastoris improved the Gambogic Acid receptor level of foreign proteins [24,25]. By coexpression with PDI and Ero1, the expression level of the coexpressed strains was increased by 60% [26]. In our study, the α-galactosidase gene was coexpr
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The overall very satisfactory potency profile of compounds a
2021-10-27

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 rxr receptor core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly
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CC is a widespread disorder affecting up
2021-10-27

CC is a widespread disorder affecting up to 20% of people worldwide, which also deteriorates the quality of life of patients and causes a substantial economic burden to society. There are 3 categories of CC: normal-transit constipation, slow-transit constipation and defecatory or rectal evacuation d
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Methods br Results br Discussion
2021-10-27

Methods Results Discussion SV exocytosis from excitatory boutons is more sensitive to inhibition by isoflurane than exocytosis from inhibitory boutons,4, 31 but the mechanism(s) of this synaptic selectivity is unknown. Although P/Q-type VGCCs contributed quantitatively more to SV exocytosis t
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(+)-Aphidicolin br Results br Discussion Impaired BBB functi
2021-10-27

Results Discussion Impaired BBB functions evoke vasogenic edema, which elevates intracranial pressure and leads to a life-threatening condition (Sperk, 1994, Unterberg et al., 2004, Simard et al., 2007). In addition, vasogenic edema formation results in the worsen consequence contributing to p
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BMP signals play pivotal roles in
2021-10-27

BMP signals play pivotal roles in the various processes of chondrogenesis [12], [13]. At early stages of chondrogenesis, BMP signaling regulates the differentiation of mesenchymal Disuflo Cy3 azide into chondrocytes via the induction of Sox9[29]. The loss of Noggin, a BMP antagonist, results in the
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The presence of the H receptor in humans was confirmed
2021-10-27

The presence of the H3 receptor in humans was confirmed approximately 25 years ago, and the receptor was successfully cloned in 1999 (Thurmond, 2010). The H3 receptor is unique, as it controls feedback of histamine release, particularly in the central nervous system, where it modulates neurotransmit
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