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Hepatocyte proliferation is accompanied by
2019-12-18
Hepatocyte proliferation is accompanied by changing gene expression [1,2]. as two of the three estrogen receptors are transcription factors: Estrogen Receptor alpha (ERα) and ERβ [[3], [4], [5]]. The most potent ligand estradiol, binds to ERα/ERβ and exerts changing cognate gene transcription [5]. O
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ucf101 receptor The aim of the following work was to untap
2019-12-18
The aim of the following work was to untap the potential of DIS as a low-cost substrate for fungal production of lignocellulolytic enzymes via SSF. Fungal strains with the ability to transform the unpretreated DIS to a mixture of industrially relevant lignocellulases were identified. Furthermore, th
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High throughput screening HTS of the AstraZeneca compound co
2019-12-18
High throughput screening (HTS) of the AstraZeneca Etoposide collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) and was s
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In recent years there has been a dramatic increase
2019-12-18
In recent years there has been a dramatic increase in identification and optimization of potent CRTh2 antagonists which may not only inhibit the recruitment and activation of Th2 cells but also accelerate apoptosis and clearance of these cells from inflamed tissue, thereby promoting the resolution o
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Currently approved anti obesity drugs for
2019-12-18
Currently approved anti-obesity drugs for long term use such as orlistat, lorcaserin and liraglutide are efficient in reduction of weight gain but are limited in usage due to their adverse effect profile and higher cost (Krentz et al., 2016; Mopuri and Islam, 2017). In ticarcillin synthesis to this
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Introduction Primitive neuroectodermal tumors PNETs are mali
2019-12-18
Introduction Primitive neuroectodermal tumors (PNETs) are malignant, small round cell tumors of neural crest origin which typically arises from bone or soft tissue in the trunk/axial skeleton/paraspinal regions in adolescents and young adults and comprises of 50% cases with local recurrence and met
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Considering these reports and with
2019-12-18
Considering these reports, and with the aim of further investigating the mechanism by which the cAMP-Epac/PKA pathway activates eNOS, we have performed imaging experiments evaluating the effect of drugs that increase cAMP or modify its signalling pathways (PKA or Epac activators and inhibitors) on b
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Introduction Obesity constitutes a global healthcare problem
2019-12-18
Introduction Obesity constitutes a global healthcare problem and has many adverse effects on the cardiovascular function [1,2]. Recently, the perivascular adipose tissue (PVAT) has emerged as a relevant fat depot for cardiovascular risk and as a potential trigger in vascular dysfunction. Indeed, PV
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In vitro studies in NSCLC cell lines expressing EGFR
2019-12-18
In vitro studies in NSCLC cell lines expressing EGFR mutants (T790M mutation, exon 19 deletion E746-A750, L858R/T790M double mutation), demonstrated that Rociletinib potently inhibits proliferation in the mutant EGFR NSCLC Piperine with Growth inhibition (GI50) values ranging from 7 to 32 nmol/L. I
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br Ubiquitin ligases Ubiquitin ligases are
2019-12-18
Ubiquitin ligases Ubiquitin ligases are categorized into different AP-III-a4 based on their specific structural configuration and the composition of subunits—HECT (homologous to E6-AP1 (E6-associated protein 1) carboxy-terminus)-type, RING (really interesting new gene)-finger-type, U-box-type, o
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In contrast to SQLE HMGCR could be efficiently
2019-12-18
In contrast to SQLE, HMGCR could be efficiently degraded in BX795 synthesis lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent with our re
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Crystallographic and NMR based analyses have
2019-12-18
Crystallographic and NMR-based analyses have revealed that RINGs and U-boxes have a common mode of interaction with E2s (Fig. 2A). The key structural elements are two loop-like regions, which, in the case of RINGs, coordinate Zn. The loops surround a shallow groove formed by the central α-helix. Tog
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In order to validate the ATP competitive mode of
2019-12-17
In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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Thienoguanosine Two additional hydrogen bonds are formed
2019-12-17
Two additional hydrogen-bonds are formed by the -substituted methoxy-group with Ser and Asp. Ser exerts the role of a gate keeper in CK1: Entry of the ATP in the binding-site causes a conformational change into the closed form by Ser, which locks the binding-site and prevents ATP-diffusion out of th
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The reduction of the calcium response
2019-12-17
The reduction of the calcium response to AVP could be also due to a PKA-mediated effect of desensitization of IP3R, as described in rat megakaryocytes [41]. Furthermore, PKA activation inhibits intracellular Ca release in mouse pancreatic acinar cells [42] or in rat cerebellum [43]. The phosphorylat
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