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The development of novel approaches to study GPCR mediated
2020-12-09

The development of novel approaches to study GPCR-mediated transactivation in live ha peptide is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitment of Gr
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The mesolimbic dopamine system is
2020-12-08

The mesolimbic dopamine system is believed to be highly important for evaluating environmental stimuli in order to generate an adaptive behavioral response. Thus, not surprisingly these functions appear to have been highly conserved across the vertebrate subphylum. Even though teleost fish lack midb
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The in vivo IC M in the
2020-12-08

The in vivo IC (0.0003μM) in the adipose tissue assay is in very good agreement with the in vitro IC (0.0005μM), and it is larger than the one measured in the OLTT assay (0.00005μM) for this compound. These differences in in vivo IC between OLTT and TAG synthesis are expected as we used free Clodron
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br Authors contributions br Acknowledgements br Introduction
2020-12-08

Authors’ contributions Acknowledgements Introduction Retinoic igf 1 inhibitor is a key signalling molecule in healthy development and in differentiation of stem cells, albeit uncontrolled levels of retinoic acid can lead to mutagenesis [1]. In eukaryotes retinoic acid is made by oxidation
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hsp70 inhibitor Introduction Formate dehydrogenase enzymes F
2020-12-08

Introduction Formate dehydrogenase enzymes (FDHs) are a group of heterogeneous proteins that catalyse the reversible formate () oxidation to carbon dioxide () (Eq. (1)). These enzymes are classified in two families, one gathering the enzymes that hold no redox-active centres and another that includ
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L-161,982 A small subset of compounds
2020-12-08

A small subset of compounds composed the 5-[1,2,4]triazino[5,6-]indole cluster (). This series of compounds was characterised by a central heterocyclic core with an R1 alkyl amine chain, required for potency (. , , and ), with preference for morpholine over piperidine (. ). The scaffold can be subst
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Studies of LRRK tagged with green fluorescent
2020-12-08

Studies of LRRK2 tagged with green fluorescent protein revealed the presence of monomeric LRRK2 in the CD 1530 synthesis of living cells, while LRRK2 oligomers were found in the proximity of the plasma membrane, suggesting that both oligomerization status and compartmentalization of LRRK2 defines i
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BCECF-AM In contrast to chordates authentic chemokine and re
2020-12-08

In contrast to chordates, authentic chemokine and receptor orthologues can be found in the agnathan fishes (Bajoghli, 2013, Kuroda et al., 2003, Nomiyama et al., 2011, Nomiyama et al., 2013); sea lamprey has at least five chemokine receptor genes, one CXCR4 (Ensembl Acc. No.: ENSPMAP00000007678) (Ku
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Nucleophosmin NPM which also plays a role on the
2020-12-08

Nucleophosmin (NPM1), which also plays a role on the nuclear export of ribosomal proteins and subunits (Maggi et al., 2008), is also a relevant MYC target, presumably through an interaction with CRM1. Conversely, it has been recently reported that specific SINE compounds reduce the levels of MYC in
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br Materials and methods br Results br Discussion In
2020-12-08

Materials and methods Results Discussion In this study, we investigated two novel candidate therapeutics, the related CRM1-inhibiting SINEs KPT-185 and KPT-276, in treatment of NHL. The results showed that KPT-185 induced growth inhibition, cell-cycle arrest, and apoptosis in tumor 103 9 mg
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Unlike the CRF receptor the CRF a
2020-12-08

Unlike the CRF1 receptor, the CRF2(a) receptor binds and is activated by agonists with a broad range of potencies. Therefore, we assessed the ability of strong and weak ligands to desensitize retinoblastoma CRF2(a) receptors. Although stresscopin's N-terminus is two Sapitinib longer than the N-termi
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br Acknowledgements We thank Jeus Perez Clausell
2020-12-08

Acknowledgements We thank Jeus Perez-Clausell from the Department of Cell Biology, School of Biology, University of Barcelona, Felipe Casanueva's group from the Department of Molecular Endocrinology and Carlos Diéguez's group from the Department of Physiology, School of Medicine, University of Sa
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Anidulafungin We did not find any significant
2020-12-08

We did not find any significant associations between APOE genotype and BDI-II, BAI, or PAI clinical scale scores. Our results indicate that APOE is not likely to play a major role in psychiatric comorbidities in epilepsy. This is in line with studies in the general population, which have not found a
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Since protein kinase CK has over known substrates
2020-12-08

Since protein kinase CK2 has over 300 known substrates we examined if the inhibitory effects described above could also be detected using another substrate. Therefore, we employed the synthetic peptide RRRADDSDDDDD which is often used in CK2 inhibitory studies. Quite contrary to the phosphorylation
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br Discussion The membrane PVase activity components were
2020-12-08

Discussion The membrane PVase activity components were discriminated in this work by pre-incubating with PMSF, mipafox, paraoxon or PMSF + mipafox to irreversibly inhibitPVase activity to discriminate the enzymatic components, (EPα, EPβ, EPγ and EPδ). The concentrations employed to discriminate t
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