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Previous synthetic lethal screening efforts Cox et al
2020-05-14
Previous synthetic lethal screening efforts (Cox et al., 2014) have mainly used RNAi as a means of identifying potential targets (Barbie et al., 2009, Kim et al., 2016, Luo et al., 2009, Scholl et al., 2009), although a few screens (Shaw et al., 2011, Steckel et al., 2012) have been performed with s
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Recent pharmaceutical research in the field of
2020-05-13
Recent pharmaceutical research in the field of respiratory diseases has sought to make available new agents that specifically and selectively antagonize the actions of cysteinyl–leukotrienes. Such an effort has resulted in the development of two classes of drugs, effective in counteracting Cys-LTs p
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5-ht1a During the course of our research on mGlu
2020-05-13
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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CXCR is not only critical
2020-05-13
CXCR5 is not only critical in the B cell lineage in FL. A high proportion of CXCR5-expressing follicular helper T cells (TFH) were observed in FL but not in closely related DLBCL [141] and further investigation revealed that FL regulatory T cells (Tregs) used a CXCL13-CXCR5 autocrine loop for positi
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br Inhibiting APC C during
2020-05-13
Inhibiting APC/C during Interphase and prior to Anaphase Because ubiquitylation by APC/C triggers cell division, it is essential that APC/C is restrained until cells are prepared for its substrates to be degraded. In addition to regulation by phosphorylation, an additional layer of control comes
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A putative SHBG receptor SHBG R has
2020-05-13
A putative SHBG a83 synthesis (SHBG-R) has been postulated for about thirty years [66], [69], [70]. The characterization of this receptor has been researched by several groups. There are different ideas on how this receptor works. On the one hand Fortunati et al. provide evidence that SHBG is alread
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Several DA receptors heteromers with a therapeutic potential
2020-05-13
Several DA receptors heteromers with a therapeutic potential have been described, including D1R/D3R (Fiorentini et al., 2010), but their roles remain to be established. Moreover, most studies on receptor heteromers in addiction focused on the striatum because of its key role in the pathology and its
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Our results indicate a deregulation of DNA methylation machi
2020-05-13
Our results indicate a deregulation of DNA methylation machinery during seed development in apomixis. Since DRM2 is targeted loci through an RNA-directed DNA methylation (RdDM) pathway involving 24-nt siRNAs (Stroud et al., 2014, Law and Jacobsen, 2010) and differentially expressed between apomict a
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Mutation in BRCT II domain W
2020-05-13
Mutation in BRCT-II domain (W893R) either in the full-length context or the C-terminal context greatly reduced the expression of LIG4 (Fig. 2B, Fig. 3B), suggesting the importance of BRCT-II domain in the maintenance of LIG4. In this regard, it might be noted that LIG4 protein was undetectable in Li
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Expression of MGMT in human cells can be
2020-05-13
Expression of MGMT in human Manumycin A can be switched off by enzymatic methylation of a cytosine residue in the MGMT promoter sequence. In this regard, both MGMT and the mismatch repair function MLH1 belong to a subset of DNA repair genes that are subjected to epigenetic control. In consequence,
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One possible explanation for differences in the
2020-05-13
One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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br Cholesterol handling in the
2020-05-13
Cholesterol handling in the arterial wall cells Foam cell formation in the arterial intima is a major hallmark of early-stage atherosclerotic lesions, which is attributed to uncontrolled uptake of modified lipoproteins, excess cholesterol esterification and impaired cholesterol release [44]. As a
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br Introduction Melatonin mainly originates from the pineal
2020-05-13
Introduction Melatonin mainly originates from the pineal gland (Reiter, 1991) and is well known for its physiological functions in the regulation of circadian rhythms (Cajochen et al., 2003) and as a potent free radical scavenger and broad-spectrum antioxidant in mammals (Paradies et al., 2010, T
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Dioscin Twin studies have shown that P has moderate
2020-05-13
Twin studies have shown that P has moderate heritability. Zuckerman (1989) reviewed the earlier studies of P or related traits and found a median heritability of 0.51. However, twin studies using an Eysenckian P scale have tended to estimate somewhat lower heritabilities than this, in the range 0.36
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The discoidin domain receptors DDR and DDR
2020-05-13
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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