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Thus this work aims to evaluate
2022-02-03

Thus, this work aims to evaluate the effect of tannic ac 723 on β-galactosidase activity, by observing the variations in the molecular interaction kinetic parameters ( and ). Besides, these data were correlated with the modifications that the tannin caused to the enzyme’s secondary structure (CD),
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br Acknowledgements We apologize to our distinguished collea
2022-02-03

Acknowledgements We apologize to our distinguished colleagues whose work has not been cited owing to space limitations. This work was funded by the Italian Association for Cancer Research (AIRC, Milan, Italy, IG 14732 to A.M.); Italian Ministry of University and Education (Finanziamenti per la Ri
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Regulation of FGF signalling is critical
2022-02-03

Regulation of FGF signalling is critical to ensure a balanced response to receptor stimulation. This occurs largely through negative feedback mechanisms, including receptor internalisation via ubiquitination (Wang et al., 2002) and induction of negative regulators, for example SPRY, SPRED 1 and 2 an
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With the nitrogen containing heterocycle components
2022-02-03

With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic (-)-Bicuculline methiodide (, and ), followed by deprotection by TFA, smoo
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There has been conflicting evidence
2022-02-03

There has been conflicting evidence on the possible receptor mechanisms that mediate the neuro-immuno-modulatory effects of FAAH substrates. Evidence from in vitro studies indicates that AEA-mediated modulation of TLR4-induced neuroinflammation may be mediated by CB1/CB2 receptor dependent (Correa e
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br Acknowledgments The work in the Vancurova
2022-02-01

Acknowledgments The work in the Vancurova lab is supported by St John’s University, and by NIHCA202775 grant. HDACs are Epigenetic Achilles’ Heels in Tumors with ICLs On the one hand, proficient and accurate DNA repair mechanisms ensure the genomic integrity of cells. On the other hand, the D
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There are important questions that remain to be answered
2022-02-01

There are important questions that remain to be answered. How does Rap2a protein affect NF-κB activation? Why do Rap2a silencing and overexpression results to the identical hampered NF-κB activation phenotype? Overexpression experiments have demonstrated that atypical κB-Ras GTPases could inhibit NF
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br Introduction High dose niacin
2022-02-01

Introduction High dose niacin, or nicotinic acid, has been used as an athero-protective drug for more than 50 years (Carlson, 2005, Offermanns, 2006). When taken in pharmacological doses (>1g/day), the nicotinic Sal 003 form of niacin modulates plasma lipid profiles including decreasing circulat
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In conclusion we demonstrated that
2022-02-01

In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 ProteOrange results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 receptor. This network acts as “Cl−
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Tight junctions regulate the transfer of ions
2022-02-01

Tight junctions regulate the transfer of ions as well as small molecules across endothelial barriers (Li et al., 2015). We also investigated whether resistin affects tight junctions, which play an important role in the conformation of polarized endothelial barriers (Matsuzaki et al., 2010). A previo
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br Role of ghrelin in reward and addiction
2022-01-31

Role of ghrelin in reward and addiction In addition to its well-known effects on kinase inhibitor homeostasis regulation at the hypothalamic level [reviews in (Al Massadi et al., 2017, Muller et al., 2015)], ghrelin also has the ability to increase food motivation acting on hypothalamic and extr
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The suboptimal trypsin selectivity profile of DPC
2022-01-31

The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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Together the epigenetic interplay revealed in this study ena
2022-01-31

Together, the epigenetic interplay revealed in this study enabled us to expand the therapeutic potential of EZH2is from hematological malignances to solid tumors. In solid tumors, EZH2i-driven transcriptional changes are shown to be dispensable of H3K27me-regulated transcriptional network. Instead,
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Camptothecin is a type of topo I inhibitor and
2022-01-30

Camptothecin is a type of topo I inhibitor, and its prodrugs irinotecan and topotecan have been approved by the FDA for clinical cancer treatment. It has been reported that SAHA can enhance the cytotoxicity of camptothecin derivatives in several cancer cell lines20., 21., 22., 23., 24.. Taking the s
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In addition during the preparation
2022-01-30

In addition, during the preparation of this manuscript, Oka et al. [7] demonstrated that LPA acts as receptor ligand for GPR35 and that LPA is more potent than KYNA in eliciting a calcium mobilization (EC50: 30nM vs. 39μM for LPA and KYNA, respectively). Other endogenous GPR35 ligands, therefore, mi
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