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AdipoRon is an orally active synthetic small molecule that a
2024-09-06
AdipoRon is an orally active, synthetic small molecule that activates adiponectin receptor (AdipoR). It mimics the antidiabetic effects of adiponectin, exhibiting its effect through the activation of AMPK and PPARα pathways via AdipoR1 and AdipoR2, respectively (Fig. 2) [62]. AdipoR activation has r
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The theoretical calculations of ADME parameters molecular
2024-09-06
The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) c
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br Materials and methods br Results Bilateral microinjection
2024-09-06
Materials and methods Results Bilateral microinjections (n = 6) of 10 mM ACh (300–500 pmol) and 5 mM physostigmine (150–250 pmol) at the two selected caudal NTS sites caused within 1 min significant increases in respiratory frequency (from 54.5 ± 1.7 to 70.9 ± 4.1 breaths/min; +30.8 ± 7.0%; P
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The hippocampus is the primary brain structure involved in
2024-09-06
The hippocampus is the primary brain structure involved in learning and memory. The role of hippocampal synaptic plasticity in neurological processes in cognition and depression has been extensively demonstrated. Synaptophysin is a critical substance in synaptogenesis, which is necessary for learnin
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br Acknowledgments This work was
2024-09-06
Acknowledgments This work was supported by a grant of the Romanian National Authority for Scientific Research, CNCS – UEFISCDI, project no. PN-II-ID-PCE-2011-3-0571, awarded to F.A.M. D.V.N. was co-financed from the European Social Fund through Sectorial Operational Program Human Resources Develo
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It has been known that
2024-09-06
It has been known that 5-LOX is the rate-limiting enzyme for the products of LTs, and LTs actively participate in the activation of neutrophils [10]. In our study, we determined whether 5-LOX was upregulated in pancreatic tissues during ANP. Moreover, we investigated whether the inhibition of expres
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The benzimidazole group seems to be a key feature for
2024-09-06
The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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br Phosphorylation of P c Initial studies In addition to
2024-09-06
Phosphorylation of P450c17 – Initial studies In addition to the molar ratio of POR to P450c17 and the allosteric action of cytochrome b5, a third factor that governs 17,20 lyase activity is the serine/threonine (Ser/Thr) phosphorylation of P450c17 itself. In a search for post-translational factor
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To identify the kinase s mediating H S
2024-09-06
To identify the kinase(s) mediating H3.3S31 phosphorylation, we devised a 96-well-plate-compatible immunostaining assay, with Nilvadipine specific for H3.3S31ph, and utilized it to screen both a Qiagen siRNA library covering 720 human kinases and a kinase inhibitor library (Selleck) containing 194
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br Conflict of interest statement br Funding
2024-09-05
Conflict of interest statement Funding Acknowledgments We thank the team at Medical and Collider-Accelerator Departments at BNL and for their support at NSRL. We thank Dr. Janice Pluth and Professor Peter O’Neill for useful discussions related to our work. Introduction The DNA damage re
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Another contributor for the G M arrest in A
2024-09-05
Another contributor for the G2/M arrest in A549 and H1299 cells might be p21WAF1/CIP1 which was up-regulated upon ovatodiolide treatment. p21WAF1/CIP1 is a common CDKs inhibitor which blocks Cinchonidine G2/M phase progression in various types of cancer cells (Kim et al., 2015, Liberio et al., 2015
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tpca Although several different membrane estrogen receptors
2024-09-05
Although several different membrane estrogen receptors have been reported (Qiu et al., 2008; Revankar et al., 2005), a large percentage of membrane-initiated steroid hormone signaling appears to be performed by a subpopulation of the same receptors that act in the nucleus. Specifically, estrogen rec
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Fourth non canonical sites may be
2024-09-05
Fourth, non-canonical sites may be targeted. Classical benzodiazepines require the presence of a γ subunit for high-affinity binding, which limits their activity to a specific large pool of receptor isoforms, leaving other isoforms unaffected. In particular, δ subunit-containing receptors, as well a
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br Conflicts of interest br
2024-09-05
Conflicts of interest Financial support This work was supported by grants from the Fondazione Cariplo [Grant number 2011-0463] (Carini); and by Funds for Original Research of the Università del Piemonte Orientale (2016, Project: Carini-Boldorini). The sponsors had no involvement in study desig
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br Materials and methods br
2024-09-05
Materials and methods Results and discussion During recent years, recombinant ASK1 has been obtained by expensive baculovirus-insect cell Heparin sodium systems [20], [27]. In the present study, we constructed recombinant ASK1 and expressed in active form at high level in E. coli. Human ASK1
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