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In a series of experiments
2022-08-18

In a series of experiments, the clotrimazole concentration was varied and the NSVDC channel conductances were calculated from Eq. (1) to obtain the dose-response relation (Fig. 3). The data were fitted to the Michaelis–Menten-type activation curve (Eq. (3)) and gave an EC50 value of 14 μM and a dose
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br Author contributions br Transparency
2022-08-18

Author contributions Transparency document Acknowledgments The financial contributions of the Marie-Curie Action: BIOCONTROL, contract number MCRTN – 33439, the Agence Nationale de la Recherche (projects membraneDNP 12-BSV5-0012, MemPepSyn 14-CE34-0001-01, InMembrane 15-CE11-0017-01 and the
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Based on the previous report that
2022-08-18

Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regulat
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The fibroblast growth factor receptor FGFRs including
2022-08-18

The fibroblast growth factor receptor (FGFRs), including four highly conserved proteins (FGFR1-4), are important membrane sensors for extracellular signals [4]. By binding to their ligands, FGFRs are activated and can trigger various downstream intracellular signaling cascades, which is required for
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The typical pharmacophore for GPR
2022-08-18

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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Having shown that some of
2022-08-18

Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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AZD-9291 mesylate mg In the present study we investigated th
2022-08-17

In the present study, we investigated the mechanisms underlying the ability of 5-FU to modify histone acetylation. Our results suggested that 5-FU induces global histone de-acetylation in CRC by promoting the degradation of p300 and CBP, two important homologous HATs catalyzing acetylation at multip
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br Conclusions and future perspectives br
2022-08-17

Conclusions and future perspectives Declarations of interest Acknowledgements The authors thank Mrs. Kamala Pandey for the help in the preparation of this manuscript. This work was supported by NIH grants R01HL057531 and R01HL062147. Introduction Separation of short exons by long non-co
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hGPR was mapped to human chromosome q and in
2022-08-17

hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen, and striatum (Sawzdargo et al., 1999). In rats, in situ hybridization indicated expression in hippocampus, thalamus and regions of the midbrain (Sawzdargo et al., 1999). Ryberg et
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Given that inactivation of GLO by BAB is an
2022-08-17

Given that inactivation of GLO1 by 4BAB is an active site directed mechanism, as the transition state analogue CHG protects GLO1 against inactivation by 4BAB (Figs. 2D and S6b), we next set out to determine the amino omacetaxine that is covalently modified by 4BAB. From the X-ray crystallographic st
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Mast cells isolated from mice and rats are able to
2022-08-17

Mast MPI-0479605 isolated from mice and rats are able to take up histamine from the microenvironment (Day and Green, 1962, Cabut and Haegermark, 1966). It has been considered that the uptake of extracellular histamine into bone marrow-derived mast cell granules is mediated by two membrane transport
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In contrast to short term effects
2022-08-17

In contrast to short-term effects, long-term exposure of beta cells to FFAs impairs insulin secretion and triggers apoptosis [13]. The deleterious effects of FFAs have been linked to altered glucose/fatty Sulfasalazine oxidation cycle [13], decreased NADPH content [14], endoplasmic reticulum (ER) s
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br Mechanisms of gap junction internalization disaggregation
2022-08-16

Mechanisms of gap junction internalization: disaggregation, endocytosis and annular gap junctions It has been clearly shown that gap junction internalization can occur by a distinctive mechanism where one cell internalizes an entire gap junction via formation of double membrane structure termed a
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TXNIP interacts with various proteins including NLRP Yoshiha
2022-08-16

TXNIP interacts with various proteins, including NLRP3 (Yoshihara et al., 2014, Zhou et al., 2010). Emerging evidence suggests that TXNIP plays a role in ER stress-mediated cell death and in the NLRP3 inflammasome activation step (Abderrazak et al., 2015, Lerner et al., 2012, Oslowski et al., 2012,
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Recent evidence indicates that prolonged vasoconstriction of
2022-08-16

Recent evidence indicates that prolonged vasoconstriction of conductance and resistance arteries involves VSMCs Chk1 and MK2 Inhibitors set sale polymerization, through activation of small GTPases [4] and a subsequently transition to a more solid rheology [5]. Actin polymerization occurs in two ste
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