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In addition to the ESIs identified that
2021-05-19

In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1
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br O GlcNAc transferase OGT belongs
2021-05-19

O-GlcNAc transferase OGT belongs to the metal-independent GT-B superfamily of glycosyltransferases, which has been well-reviewed previously [14,15]. OGT is an essential gene encoded on the X-chromosome, and it has two main regions: a long N-terminal tetratricopeptide repeat (TPR) region and a C-t
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In our opinion the precise function of
2021-05-19

In our opinion, the precise function of AE of S. mansoni (Sm32) remains unclear, and accurate knowledge of the three dimensional structure of this enzyme would be valuable for a better understanding the molecular basis of many of its properties, including its role in the host-parasite interaction, a
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How does an increase in E affinity for the
2021-05-19

How does an increase in E2 affinity for the RING domain favor higher activity and polyubiquitination by the E2? Binding of the RING domain to the E2 positions the donor Ub in the E2~Ub conjugate in a closed complex [16], [17], [18] that increases the reactivity of the thioester [60]. A higher affini
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While SCF E ligase activity was reconstituted with recombina
2021-05-19

While SCF E3 ligase activity was reconstituted with recombinant proteins two decades ago, the ability to probe APC/C was limited until recently because of its behemoth size. Human APC/C is a 1.2-MDa assembly comprised of 19 core subunits (one each of nine different APC subunits, and two each of five
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We found that the postnatal absence of norepinephrine
2021-05-19

We found that the postnatal absence of norepinephrine yields differing effects depending on noradrenergic receptor type and WM-8014 australia region. The density of α1-AR, indicated by [3H]prazosin binding was similar between Dbh+/− and Dbh−/− mice except for a significant increase in hippocampus i
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Although high concentrations of SCR G and SCR R
2021-05-18

Although high concentrations of SCR7-G and SCR7-R inhibited LigIV as reported [11], the SCR7 derivatives were more effective inhibitors of LigIIIα and, in particular, LigI. Although it is possible that differences in the DNA substrate underlie this discrepancy, it appears more likely that this refle
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At the cellular level TGF
2021-05-18

At the cellular level, TGF-β1 has been involved in the formation of invadosomes (Mandal et al., 2008, Varon et al., 2006). Invadosomes are actin-based structures involved in matrix degradation and cell invasion through metalloproteinases (MMP) activity (Linder et al., 2011). Invadosomes, constitutiv
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br Contributors br Acknowledgements br Introduction
2021-05-18

Contributors Acknowledgements Introduction Pemphigus disorders are characterized by autoantibodies binding to desmosomes between epidermal cells, resulting in the loss of cell to cell adhesion and blister formation. In pemphigus foliaceus, autoantibodies predominantly bind to desmoglein 1,
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Phylogenetic analysis indicates that in poikilothermic
2021-05-18

Phylogenetic analysis indicates that in poikilothermic vertebrates CXCR3a and CXCR3b have evolved independently from a common gene possibly after the 2nd round whole genome duplication but before the split of bony fish and tetrapods (Fig. 1 and Supplementary file 3). Owing to the extra round of whol
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MTT results show that both pancreatic cell lines
2021-05-18

MTT results show that, both pancreatic cell lines were quite sensitive to camptothecin (CPT), a well known topoisomerase I poison. Interestingly, CPT does not show any selectivity over cancer cell lines probably due to the duplication times for cancerous (MIA PaCa-2) and immortalized healthy (HPDEC)
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Stress is usually comprehended as
2021-05-18

Stress is usually comprehended as an event affecting mainly the HPA axis and initiating the alarm reaction represented by activation of the adrenal medulla. This means that the levels of related hormones and neurotransmitters are significantly elevated during and after the stress. CRF, following its
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Recently we have observed that pharmacological PPAR and
2021-05-18

Recently, we have observed that pharmacological PPARα and PPARβ/δ activation regulates the expression of genes involved in FA metabolism such as FAT/CD36, CPT1, LCAD and MCAD in Sertoli cells. We have also observed that PPARβ/δ activation can simultaneously regulate the expression of the above-menti
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Cot MAP K is the sole MAP K
2021-05-18

Cot (MAP3K8) is the sole MAP3K that activates the MEK1/2-Erk1/2 following the activation of the TLR/IL-1 receptor superfamily as well as some receptors of the TNF receptor family [8], [9], [10] and mediates the production of chemokines and cytokines in different cell systems [reviewed in [11]]. Thus
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To develop antagonists selective for the mouse EP
2021-05-18

To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic Moxidectin sale () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable alde
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