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This structure guided the variation of the compounds aiming
2021-04-15
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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Although we observed increases in AR mediated cAMP productio
2021-04-15
Although we observed increases in α1-AR mediated cAMP production separately in the nucleus and cytoplasm, compartment specificity was observed for PKA activation. GPCRs and their effector proteins are commonly found in multiprotein signalosomes with A-kinase anchoring proteins (AKAPs) serving as sca
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In addition to the ESIs identified that target
2021-04-15
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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The current study demonstrates a link between heme metabolis
2021-04-15
The current study demonstrates a link between heme metabolism and mitochondrial Co-I, which deficits instigate abnormalities in the metabolism of heme and its downstream targets both in-vitro in patients and healthy subjects derived LCLs and in-vivo in brains of SZ-rat model. A further study of the
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br Acknowledgements The research leading to these
2021-04-15
Acknowledgements The research leading to these results has received funding from the European Union Seventh Framework Programme (FP7-PEOPLE-2013-COFUND) under grant agreement no 609020 − Scientia Fellows (JB) and the Research Council of Norway (NFR-grant 221444) (JB, JPM, OB). Introduction Hu
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A prominent example of such enzyme is the
2021-04-15
A prominent example of such enzyme is the proteasome, a highly promising target not only in cancer, but also in inflammatory and autoimmune diseases. Circulating proteasomes and respective anti-proteasome autoantibodies were detected in serum samples from patients with autoimmune diseases such as mu
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Db model cells showed various aberrant phenotypes that
2021-04-14
Db model cells showed various aberrant phenotypes that seemed to reflect the pathological abnormalities found under diabetic conditions. First, in Db model cells after insulin stimulation, we found the inhibition of the transcriptional repression of the gluconeogenic genes, PCK1 and G6PC, and aberra
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br Materials and methods br
2021-04-14
Materials and methods Results Discussion Tuberculosis is caused by the mycobacterium M. tuberculosis, a pathogen able to survive in the hostile conditions through sophisticated defence mechanisms. In an attempt to clarify some aspects of the M. tuberculosis defence mechanisms, we have inves
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E cadherin is an adhesive Ca dependent transmembrane protein
2021-04-14
E-cadherin is an adhesive Ca2+ dependent transmembrane protein mediating tight and strong cell-cell adhesion through homophilic interactions. There is strong evidence in favour of the major role of E-cadherin in melanocytes adhesion to keratinocytes in the engineering male (Tang et al., 1994). The
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HvPap a member of the cathepsin F
2021-04-14
HvPap-1, a member of the cathepsin F-like family, was identified in germinating barley seeds (Sreenivasulu et al., 2008). This enzyme participates in the mobilization of stored proteins (mainly hordeins) during the last phase of grain germination, and its activity is modulated by a propeptide or/and
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During host cell interactions G intestinalis trophozoites
2021-04-14
During host-cell interactions, G. intestinalis trophozoites up-regulate several cell-associated proteins, including high-cysteine membrane proteins (HCMPs) and variant surface proteins (VSPs) [8]. The parasite also releases around 200 proteins upon host-cell contact, including many proteases [9,10].
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Based on our studies presented above atipamezole can
2021-04-14
Based on our studies presented above, atipamezole can be used as a new in vitro and in vivo tool smoothened as a pan-CYP inhibitor for CYP mediated metabolism study. It carries many unique characteristics compared to ABT which is currently being widely used for this purpose. These new characteristi
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Recently it has been shown that among the ELR chemokines
2021-04-14
Recently, it has been shown that among the ELR (+) chemokines mentioned above, particularly IL-8 induces neutrophil migration via CXCR-1 chemokine receptor. For example, Godaly et al. [18] reported the potent role of CXCR-1 chemokine receptor in the process of neutrophil migration across epithelial
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Recent studies investigating the effects of mesenchymal stem
2021-04-14
Recent studies investigating the effects of mesenchymal stem cell (MSC) therapy in rodent models including chronic renal failure and glomerulonephritis have demonstrated that MSC therapy can result in beneficial effects [57], [58]. In cats, autologous intra-renal injections of either adipose tissue-
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Carnitine acetyltransferase CrAT transesterifies short
2021-04-14
Carnitine acetyltransferase (CrAT) transesterifies short-chain acyl-CoAs, and is located both in mitochondria and peroxisomes. In yeasts and mammals this protein is the product of a single gene [20,21] and the sorting to different organelles is evolutionary conserved, although the mechanism of diffe
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