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Simulation methods In our study
2019-12-16

Simulation methods In our study, the TIP3P model is applied for water, AMBER99sb force field [24] is used to describe three types of EGFR, including the wild type (PDB: 2ITY) [25], its mutant G719S (PDB: 2ITO) [25] and mutant T790M (PDB: 3IKA) [26]. The force field of Tubemoside molecule is paramet
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As mentioned above EBI and its ligand show some similarities
2019-12-16

As mentioned above, EBI2 and its ligand show some similarities to the sphingosine 1-phosphate (S1P)/S1P-receptor system, which mediates T cell egress from lymph nodes. Blockade of this system yielded in the first oral drug for MS patients named fingolimod. Therefore, the hope that EBI2 deficiency wo
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br Collagens as new drivers of zebrafish tissue
2019-12-14

Collagens as new drivers of zebrafish tissue regeneration Contrary to mammals, zebrafish possess very high regeneration capacities and thereby represent a versatile model to study tissue and organ regeneration. Adult fish can fully reconstruct their brain, spinal cord, retina, kidney, liver, panc
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One possible pitfall of using EPAC activators in
2019-12-14

One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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br Epac in cardiovascular pathophysiology Epac orchestrates
2019-12-14

Epac in cardiovascular pathophysiology Epac orchestrates signaling actors that regulate fundamental cellular functions and general biological effects. However, some important gaps still remain in the knowledge of the physiopathological role of Epac in the heart. So far, Epac has been implicated i
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The attachment of ubiquitin to RTKs such as EGFR
2019-12-14

The attachment of ubiquitin to RTKs, such as EGFR, mediates efficient delivery through the endosome-lysosome system for proteolysis. In this way, RTK degradation enables cessation of signal transduction. A recent siRNA screen identified a number of USPs that can significantly modulate EGFR levels an
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Contrary to the downregulation of
2019-12-14

Contrary to the downregulation of S1PR family GPCRs, CLL cells have increased mRNA expression of the lysophosphatidic leucine enkephalin (LPA) family receptors LPAR1, LPAR3 and LPAR4 compared to normal B cells [47]. Increased LPAR1 mRNA has been shown to be associated with more aggressive disease [4
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Carbazole could be recrystallised from ethyl acetate to prov
2019-12-14

Carbazole could be recrystallised from ethyl acetate to provide bright red crystals suitable for single crystal X-ray diffraction (see ). The first crop showed had crystallised preferentially as the ()-isomer (A). Examining the single crystal X-ray data of it was interesting to find that the N2C1
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Several reports by us and others have highlighted that
2019-12-14

Several reports by us and others have highlighted that dimerization or oligomerization of DDR1 ECD and DDR2 ECD enhances their binding to triple-helical collagen.18, 19, 22, 28, 29, 30, 31 The ECD of DDRs consists of a discoidin domain and a stalk region. It has been reported that independent ana ca
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In this review we first introduce the in vivo metabolism
2019-12-13

In this review, we first introduce the in vivo metabolism profile of VD3, and the mediation of Cyp3a gene transcription by PXR and CAR in humans, mice and rats. We then focus on the species-specific VDR-dependent regulation of human (CYP3A4, CYP3A5 and CYP3A7), mouse (mainly CYP3A11 and CYP3A13), an
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Previous studies found that depression
2019-12-13

Previous studies found that depression primarily results from impaired monoaminergic neurotransmission systems [1], [2]. The glutamatergic and GABAergic systems as well as several neuropeptide systems have also been the focus of pathophysiological studies on depression [1], [2]. Inflammatory cytokin
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The kinase activity of DNA
2019-12-13

The kinase activity of DNA-PKcs is essential for NHEJ, but the exact role of the enzymatic activity of DNA-PKcs plays in NHEJ is not fully understood [57]. In vitro, DNA-PKcs can phosphorylate each of the canonical NHEJ factors including Ku70/80 [58], [59], XRCC4 [60], [61], gsk3b inhibitor IV [62]
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The identification of a gatekeeper mutation also suggests
2019-12-13

The identification of a gatekeeper glucocorticoid receptor antagonist also suggests that alternative DDR2 inhibitors may be required to overcome acquired resistance. Additional DDR2 inhibitors that have been isolated include the recently identified alkaloid natural products discoipyrroles A-D and t
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Our observation that FAK is downregulated in vascular smooth
2019-12-13

Our observation that FAK is downregulated in vascular smooth muscle topotecan on fibrillar collagen confirms observations reported for other cell types [14]. However, unlike the results reported previously [14], our work suggests that matrix rigidity per se does not determine FAK downregulation. Thi
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br Introduction Localized degenerative and progressive enlar
2019-12-13

Introduction Localized, degenerative and progressive enlargement of the aortic diameter involves all layers of the vessel wall may ultimately rupture creating a catastrophic cardiovascular event [1,2]. An aneurysm may be located in the thoracic or abdominal aortic wall with different clinical app
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