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In the previous study we demonstrated the importance of
2023-12-29

In the previous study, we demonstrated the importance of the mPFC postsynaptic 5-HT1A receptor in the sustained antidepressant effects, because a sustained antidepressant effect was obtained with intra-mPFC injection, but not systemic injection of 8-OH-DPAT, a 5-HT1A receptor agonist (Fukumoto et al
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Extracellular ATP and downstream purinergic signaling have a
2023-12-29

Extracellular ATP and downstream purinergic signaling have also been proposed to contribute to dental pulp tissue healing and dentin regeneration. Mechanical and thermal stimulation of external dentin can induce ATP release in dental pulp through pannexins [13]. Cold stimulation was also reported to
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We further analyzed selected hit compounds for their ability
2023-12-29

We further analyzed selected hit compounds for their ability to inhibit human AdK in intact cells. Human 1321N1 astrocytoma ethionamide were utilized which were found to express AdK. The whole cell assay was performed using a 96-well format. The standard AdK inhibitor 5-iodotubercidin was employed
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br Introduction ACK or Activated Cdc
2023-12-29

Introduction ACK1, or Activated Cdc42-Associated Kinase, located on chromosome 3q, is a ubiquitously expressed non-receptor tyrosine kinase cloned from a human lomitapide cDNA library (Manser et al., 1993). It was first identified to bind to activated Cdc42, a small Ras GTPase via its CRIB domain
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During myeloid cell maturation expression
2023-12-29

During myeloid cell maturation, expression of 5-LO mRNA and protein is strongly induced (60–130-fold) by calcitriol (1,25(OH)2D3) and transforming growth factor-β (TGFβ) [6,7]. The upregulation of 5-LO mRNA transcription is mainly due to transcript elongation and mRNA maturation [8,9]. Interestingly
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Compounds are representatives of an
2023-12-29

Compounds – are representatives of an array of MBG targets (, ) related to imidazole standard that were synthesized and initially tested in a rat CYP17 lyase screening assay (). The inhibitors were synthesized as racemates by coupling of 6,7-dimethoxy-naphthalene-2-isopropyl ketone with the requisit
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Here we show that the co activation of RTKs and
2023-12-29

Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC Ozagrel and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhibitor TPX-0005 (Z
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br Expression of autotaxin in
2023-12-29

Expression of autotaxin in cancer Autotaxin (ATX) is a member of the family of NPPs (Nucleotides pyrophosphatases phosphodiesterases (NPP) family with a unique lysophospholipase D (lysoPLD) activity, allowing the synthesis of LPA from lysophospholipid precursors such as the lysophosphatidylcholin
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Oseltamivir phosphate Chronic inflammation is associated wit
2023-12-29

Chronic inflammation is associated with both initiation and progression of many neoplastic conditions [149], and ATX may be a player in the process. ATX/LPA signaling is positively correlated with the invasive and metastatic potential of several cancers including melanoma, breast cancer, ovarian can
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Ryoichi et al modified potent clinical candidate VX with
2023-12-28

Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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Although the exact mechanisms are not fully
2023-12-28

Although the exact mechanisms are not fully understood, IGF-1 is tightly linked with ER and estrogen actions and a crosstalk occurs between these two systems in breast cancer. To illustrate this close relationship, studies have identified a synergy between IGF-1 and estrogen in GDC-0834 expressing
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The subnuclear localizations of redox
2023-12-28

The subnuclear localizations of redox regulators is also largely unknown. The potential role of thiol reductases as transcription regulators or DNA repair molecules may suggest an association to DNA. In this way, the presence of a zinc finger domain potentially involved in protein/DNA interactions o
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Introduction AMP activated protein kinase AMPK is mainly kno
2023-12-28

Introduction AMP-activated protein kinase (AMPK) is mainly known as a highly conserved and ubiquitously expressed energy sensor that is highly sensitive to changes in cellular energy levels (by sensing increases in AMP:ATP and ADP:ATP ratios) and makes appropriate adjustment to balance the consumpt
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Following activation of mGluRs GRIP stabilized
2023-12-28

Following activation of mGluRs, GRIP-stabilized AMPARs appear to be the primary target for endocytosis. Consistent with this model, we find that using siRNA to reduce GRIP1/2 expression blocks the AMPAR internalization and the synaptic depression mediated by mGluRs. Reductions in GRIP1/2 expression,
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br Conclusion These studies broadly demonstrate that dopamin
2023-12-28

Conclusion These studies broadly demonstrate that dopamine and endocannabinoid signaling in the NAc can have diverse effects on AMPAR-mediated synaptic function depending on previous psychostimulant experience. Here, we examined mechanisms underlying the depotentiation of AMPAR-mediated synaptic
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