• We have previously reported the characterization

  2020-10-16

  

  We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot

• br Allosteric inhibitors In general candidate drugs that

  2020-10-16

  

  Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d

• In most cases the ligand affinity between subtypes is

  2020-10-16

  

  In most cases, the ligand affinity between subtypes is similar, but their tissue distribution is different. In the case of the estrogen receptors (ER), two subtypes (ERα and ERβ) exist (Kuiper et al., 1996) and ERβ has several isoforms, designated ERβ1–5 (Moore et al., 1998) or ERβcx (Ogawa et al.,

• br STAR Methods br Acknowledgments We thank members

  2020-10-16

  

  STAR★Methods Acknowledgments We thank members of R.L. lab and F. Schweisguth for critical reading of the manuscript. We are also grateful to F. Janody, M. Miura, C. Bökel, H.D. Ryoo, G. Jiménez, the Bloomington Drosophila Stock Center, the Drosophila Genetic Resource Center, the Vienna Drosoph

• ACET The work described by Dong Groves and co

  2020-10-16

  

  The work described by Dong, Groves, and co-workers (11) tested the hypothesis that neural stem cell development is sensitive to the clustering and mechanical state of the EphB4:ephrin-B2 receptor-ligand complex. They show that the quality of ephrin-B2-ligand signaling depends on its biophysical stat

• br Physiological roles for EPAC isoforms

  2020-10-16

  

  Physiological roles for EPAC isoforms: vascular function The effects of cAMP on limiting vascular endothelial cell (VEC) inflammation and vascular smooth muscle cell (VSMC) proliferation have been well documented 36, 37, 38. However, recent work has demonstrated that several key effects of cAMP i

• Prostanoids typically act in an autocrine

  2020-10-16

  

  Prostanoids typically act in an autocrine and paracrine fashion by binding to specific receptors in target Swainsonine and there is evidence that both PGE2 and prostacyclin may be required for the optimal activation of angiogenesis (Hata and Breyer, 2004). PGE2 and prostacyclin bind to their specif

• Docking experiments showed that Me MeGlcA Xyl

  2020-10-16

  

  Docking experiments showed that Me-MeGlcA3Xyl4 and MeGlc3Xyl4 were bound to EcXyn30A and the R293A variant in the same way as MeGlcA3Xyl4, having MeGlcA or its modified forms accommodated in the -2b subsite. All ligands were coordinated by the same 5z mg and no new interactions were observed. The on

• First of all it should

  2020-10-16

  

  First of all, it should be emphasized that, although cPLA2α manifests a marked selectivity for phospholipids that contain AA at the sn-2 position, this does not mean in any way that, in cells, the enzyme cannot hydrolyze other fatty acyl residues to a significant extent even if this occurs at a lowe

• Importantly we observed significantly the

  2020-10-16

  

  Importantly, we observed significantly the reduced myocardial infarct size, the improved left ventricular function and the inhibited fibrosis after I/R with oral GA-BH4 supplementation before ischemia (Fig. 1, Fig. 2, Fig. 3). Usually, there is a view that the antioxidation induced by reducing agen

• Our results showed that in elastase induced

  2020-10-16

  

  Our results showed that in elastase-induced AAA, TGF-β neutralization finely tunes macrophage phenotype. Note that several studies have already addressed the role of M1 markers, such as IL-6 and IL-1β, or M2 markers, including IL-10 and TGF-β.4, 9, 10, 11 The expression and the role of ARG1 in AAA h

• Cytidine 5-triphosphate Previously we showed that MS a combi

  2020-10-16

  

  Previously, we showed that MS-10, a combined extract of Cirsium japonicum var. Maackii (Maxim.) Matsum. (Korean milk thistle) and Thymus vulgaris L., increases the efficiency of estrogen in the estrogen-deficient state by activating the estrogen receptor (ER). MS-10 increased bone mineral density (B

• br EBV Infection Epstein Barr virus EBV human

  2020-10-16

  

  EBV Infection Epstein–Barr virus (EBV, human herpesvirus 4) was discovered 50 years ago, when Epstein, Achong, and Barr used electron microscopy to identify viral particles in Burkitt\'s lymphoma cells. It belongs to the lymphocryptovirus (LCV) genus of the gammaherpesvirus subfamily (Fig. 1A). T

• Here we discuss implications of several

  2020-10-16

  

  Here, we discuss implications of several major families of RING-type E3 ubiquitin ligases (MDM, Cullin, GRAIL, TRAF, TRIM) as targets in inflammation and immunity, and provide insights into potential small molecule interventions to mediate the cellular responses (summarized in Table 1). We briefly c

• The present study is a genetic association study

  2020-10-15

  

  The present study is a genetic association study using the classic candidate gene approach. This method has been repeatedly criticized in the past to produce highly unreliably findings (e.g. Flint & Munafò, 2013). The alternative would be the conduction of a Cilomilast wide association study (GWAS)

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