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Our previous studies found that some steroid
2024-09-06
Our previous studies found that some steroid mimetic structures such as stilbene, biphenyl, naphthalene and benzothiophene rings were suitable for lipophilic moieties of 17,20-lyase inhibitors, and several inhibitors obtained using a steroid A, C-ring mimetic approach have already been published. Du
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Thirty six of the analogs synthesized showed
2024-09-06
Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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Apelin APJ triggers a variety
2024-09-05
Apelin/APJ triggers a variety of cellular signaling pathways (Fig. 1). Recent studies from our laboratory showed that apelin-13 induces vascular smooth muscle cell (VSMC) proliferation by the upregulation of Cyclin D1 expression, which is involved in an ERK-dependent activation of Jagged-1/Notch3 si
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Negative regulation of AR expression
2024-09-05
Negative regulation of AR expression by NFκB was also correlated with the ‘age-dependent desensitisation’ of androgen action in the rat liver (Supakar et al., 1995). In this case the binding site was mapped upstream of the gene to sequences −555 to −565 bp, that binds heterodimers of p65 and p50, as
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br MHCI peptide editing N terminal
2024-09-05
MHCI peptide editing, N-terminal extensions and the peptide loading complex Conventionally, peptide-MHCI binding is thought to require both amino- and carboxyl-termini for stable interaction (Madden, 1995; Bouvier and Wiley, 1994). Peptides with longer than optimal length (10–13 residues) have be
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A disfun o cognitiva p s operat
2024-09-05
A disfunção cognitiva pós‐operatória é uma síndrome perioperatória bem reconhecida, consequência da anestesia e cirurgia cuja causa exata permanece por esclarecer. De que forma AS1404 disfunção cognitiva pós‐operatória e a doença de Alzheimer podem estar ligadas permanece uma questão em estudo. A bi
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A key building block in MT SGL is the computation
2024-09-05
A key building block in MT-SGL is the computation of the proximal operator in (12) when is the multi-task sparse group lasso regularizer given byFor MT-SGL, the iterates x ≡ Θ are matrices, and the proximal operator is computed at z ≡ Z = Θ + α(Θ − Θ). For the loss function L(·) corresponding to Ga
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br Functions essentially consisting in transport of
2024-09-05
Functions essentially consisting in transport of substrates across plasma membranes Direct activation of neurotransmitter transporters elicits responses in neurons As previously mentioned (Section 2.1), nerve terminals handling classical transmitters possess transporters able to (re)capture se
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br Conflicts of interest br
2024-09-04
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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Introduction Hepatocellular carcinoma HCC is one of
2024-09-04
Introduction Hepatocellular carcinoma (HCC) is one of the most difficult cancers to treat, and it threatens human health severely [1]. Although various interventions, including surgical operation, radiofrequency ablation, and chemotherapy, have been endorsed, the prognosis of HCC patients remains p
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Varlitinib receptor In the current investigation we studied
2024-09-04
In the current investigation, we studied the effect of propofol on prostate cancer cells. Propofol is one of the most commonly used drugs in the critical care setting and for the induction of general anesthesia and moderate and deep sedation intraoperatively. Recent studies indicated that propofol e
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In conclusion phenolic hydroxyl was
2024-09-03
In conclusion, phenolic hydroxyl was introduced not only to C3 side chain but also to C6 or C7 position of the quinoxalinone core, resulting in a new group of ARIs candidates exhibiting antioxidant activity. Biological activity tests suggested that compounds were not only sufficient to inhibit ALR2
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An important and well documented pathway
2024-09-03
An important and well-documented pathway involved in cellular growth and proliferation is the mTOR-mediated synthesis of proteins and lipids [7,13,14]. Although found to be tissue specific or context specific regulation, it has always been observed that either one or both the mTOR complexes regulate
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br Conclusions br Acknowledgments The authors are thankful t
2024-09-03
Conclusions Acknowledgments The authors are thankful to Hugo Santos, Olga Martinez and Ricardo Lacerda for the technical assistance provided in the maintenance of the aquaria. This work was supported by national funds, through FCT and co-funded by the European Regional Development Fund (ERDF)
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Implicit in this concept is
2024-09-03
Implicit in this concept is the idea that the β-adrenoceptors in the detrusor would be activated by adrenergic nerves of the sympathetic system: sympathetic activity promoting relaxation and enhancing bladder capacity. However, it has been demonstrated that there is only a sparse adrenergic innervat
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