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The nuclear receptor NR superfamily of ligand regulated tran
2021-01-05
The nuclear receptor (NR) superfamily of ligand regulated transcription factors has proven to be a rich source of targets for the development of therapeutics for a wide range of human diseases. The NR3B subfamily known as the estrogen-related receptor (ERRα[NR3B1], ERRβ[NR3B2] and ERRγ[NR3B3]) regul
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EPAC induces SOCS gene expression in VECs
2021-01-05
EPAC1 induces SOCS3 gene expression in VECs, resulting in suppression of the JAK–STAT activation initiated by the sIL-6Rα/IL-6 trans-signalling complex [67]. EPAC1 regulates SOCS3 gene induction through the activation of C/EBP and c-Jun transcription factors, which interact directly with the SOCS3
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Metal ions are known not to be necessary
2021-01-04
Metal ions are known not to be necessary for catalytic activity of serine proteinases. Nevertheless, Co2+ and Ca2+ ions were found to stabilize glutamyl endopeptidase molecule [1], [7], [19]. In our previous study, we have described significant stimulating effect of Ca2+, Mg2+, and Co2+ on biosynthe
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br Conclusion Conventional surgical excision of
2021-01-04
Conclusion Conventional surgical excision of the tumoral lesions is the primer therapy for the BCC. Recurrence rates are significantly higher for surgical margin positive lesions that also creates challenges for the surgeons on obtaining best cosmetic and oncologic results. In our study, EGFR KPT
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The aniline R group was extensively
2021-01-04
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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In vitro work by us and others
2021-01-04
In vitro work by us and others revealed that high affinity interaction with collagen requires dimerization and/or pre-oligomerization of DDR1 (Agarwal et al., 2007, Abdulhussein et al., 2008, Leitinger, 2003). It has also been reported that a significant percentage of the DDR1 population forms ligan
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br Acknowledgements This work was supported by the National
2021-01-04
Acknowledgements This work was supported by the National Institute of Neurologic Disorders and Stroke (U54 HD061222, 1K23 NS107646-01, and 1K12NS089417-01), Rocky Mountain Rett Association, International Foundation for CDKL5 Research, the Ponzio Family Chair in Neurology Research, and NHMRC Senio
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Behaviors were compared between saline and
2021-01-04
Behaviors were compared between saline and amphetamine pre-treatment groups at 24h and 2 weeks following the last treatment, or between pre-treatment groups that received vehicle or ASV-30 infusions, using separate two-way ANOVAs. Significant effects were analyzed further using Student–Newman–Keuls
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Prostaglandins PGs are lipid mediators that
2021-01-04
Prostaglandins (PGs) are lipid mediators that exhibit a variety of physiological properties by interacting specific G protein-coupled receptors (GPCRs) [10]. PGD2 is synthesized from PGH2 through two distinct PGD synthases; lipocalin-type PGD synthase (L-PGDS) and hematopoietic PGD synthase (H-PGDS)
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No effect on the A production
2021-01-04
No effect on the Aβ production by γ-secretase was observed at 50μM, the highest effective concentration used in cultured elastase inhibitor by the study of Flajolet et al. IC261 did also not exert a modulatory effect on the production of Aβ, Aβ and Aβ species in the cell-free assay at this concentr
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During the past decade it became increasingly clear that
2021-01-04
During the past decade, it became increasingly clear that the affinity and efficacy of small agonists acting on the orthosteric binding site of a GPCR can be modulated by ligands that bind to a topographically distinct (allosteric) binding site on the same GPCR molecule 33, 39, 40, 41, 42. This allo
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In silico modelling studies might
2021-01-04
In silico modelling studies might aid our understanding of the functionality and potential biological activity of food and, in the long-term they might underpin the development of personalised diets to reduce health risks and help us to better understand pharmaceutical/food interactions. Acknowle
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To elucidate whether the impact of hypoxia
2021-01-04
To elucidate whether the impact of hypoxia on EGFR expression is cell context specific or culturing density dependent, we chose the following cancer Ozagrel driven by EGFR and evaluated the EGFR expression after hypoxia treatment at different culturing density: a highly aggressive and poorly differe
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br Results br Discussion br Conclusions The present study de
2020-12-31
Results Discussion Conclusions The present study demonstrates that CRF1 receptor-deficiency prolongs whereas CRF2 receptor-deficiency shortens the duration of recognition memory deficits induced by morphine discontinuation, unraveling opposite roles for the two known CRF receptor subtypes i
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Future analysis could consider using
2020-12-31
Future analysis could consider using fixed effects also with the level set field, , in order to investigate which covariates explain the classification, a feature of the proposed model that we have not yet investigated. Further, multi-type point patterns may also be analyzed with the proposed model
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