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During the course of our research on mGlu PAMs the
2021-04-30
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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Wu et al explored the anti inflammatory mechanisms by
2021-04-30
Wu et al. explored the anti-inflammatory mechanisms by which osthole 35 acted on HepG2 cells cultured in a differentiated medium from cultured 3T3-L1 preadipocyte cells. HepG2 cells, a human liver cell line, were treated with various concentrations of osthole 35 in differentiated media from cultured
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br Collagens as new drivers of zebrafish
2021-04-29
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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Studies of nuclear transplantation of diploid
2021-04-29
Studies of nuclear transplantation of diploid imprint-free PGCs have shown that the reconstituted oocytes developed to day 9.5 of gestation, with severely retarded embryos and abnormal placentae (Kato et al., 1999). We also reported that MII oocyte injection of imprint-free phESCs without imprinted
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The transcription factor CREB has been extensively studied
2021-04-29
The transcription factor CREB has been extensively studied for its role in hippocampus-dependent learning and memory (West et al., 2002, Lonze and Ginty, 2002). Previous research has demonstrated that the phosphorylation of CREB at Ser133, performed by the ERK1/2 signaling pathway, initiates a casca
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Elastase belongs to chymotrypsin family of proteases and
2021-04-29
Elastase belongs to chymotrypsin family of proteases and it is responsible for the breakdown of elastin and other proteins, such as collagen and fibronectin, which are fundamental for the ECM elastic properties (Imokawa and Ishida, 2015). Misregulations of this enzyme are involved in skin ageing pro
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In our study the TIP P model
2021-04-29
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 parameterized with optimize
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As an endogenous negative modulator CRBN
2021-04-29
As an endogenous negative modulator, CRBN inhibits AMPK’s activation (phosphorylation of Thr172) by directly binding to the α-subunit of AMPK, disrupting γ-subunit recruitment to the AMPK complex (Lee et al., 2011, Lee et al., 2013). In our study, we did not focus on AMPK activation, since only a si
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Protein deubiquitination is becoming increasingly
2021-04-29
Protein deubiquitination is becoming increasingly instrumental in understanding the complexities of the Ub system. Adding to this complexity is the discovery of bacterial effectors with DUB activity that have structurally adapted themselves to interfere with the eukaryotic Ub system (Pruneda et al.,
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Because macrophages clear the injured tissue of dead
2021-04-29
Because macrophages clear the injured tissue of dead heat shock protein inhibitors and matrix debris, macrophage infiltration is essential for normal tissue repair. In cardiac remodeling by MI, however, macrophages infiltrate excessively into not only the infarct area and marginal area of MI. Infilt
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br DAG kinase activity is confined to specific cell compartm
2021-04-29
DAG kinase activity is confined to specific cell compartments A number of reports demonstrating agonist-dependent translocation of DGKs to distinct membrane compartments suggest that DGK activity is restricted to localized DAG pools generated after activation of receptors. Perhaps the best eviden
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We also discovered important clues to domain binding
2021-04-29
We also discovered important clues to domain Apramycin Sulfate of DGKs and how to exploit these regions for development of DGKα-selective inhibitors. The identification of a probe-modified site at the C1 domain provided the first evidence of a ligand binding site remote from the ATP binding region
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br Acknowledgements br Introduction Lung cancer treatment st
2021-04-29
Acknowledgements Introduction Lung cancer treatment strategies, especially molecular targeted therapy, have progressed rapidly. However, most established treatments are for adenocarcinoma of the lung, not for squamous cell carcinoma (SQCC). SQCC constitutes approximately 30% of lung cancers, w
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br Conclusion br Funding source br Ethical approval br
2021-04-29
Conclusion Funding source Ethical approval Conflict of interest statement Introduction Traditionally, schizophrenia (SZ) was thought to be associated with neuronal dysfunction; however, the current hypothesis that myelin and, specifically, oligodendrocytes are also involved in the dev
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The levels of circulating pro inflammatory cytokines are mar
2021-04-29
The levels of circulating pro-inflammatory cytokines are markedly elevated in ESRD, and have been speculated to play an important role as causative factors in a number of uremic complications [37]. The impairment of phagocyte functions and deregulated cytokine productions are highly prevalent in CRF
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