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Replacement of the saturated propoxy group in compound
2020-10-30

Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have
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br Ultrasonic pretreatment of substrates Substrate pretreatm
2020-10-30

Ultrasonic pretreatment of substrates Substrate pretreatment is widely used in the biofuel, textile and food industries since the substrates are always difficult to degrade. During some enzymatic hydrolysis reactions, the protective layer of the substrate impedes the reaction. Ultrasonic treatmen
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It has been reported that the ECD of DDRs require
2020-10-30

It has been reported that the ECD of DDRs require dimerization and/or oligomerization for binding to collagen.,, Here, we have established using SPR that antibody-mediated oligomerization of DDR2-Fc significantly enhances its binding to immobilized collagen type 1. Our results are consistent with ea
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EBI and its ligand s EBI
2020-10-30

EBI2 and its ligand(s) EBI2 was found in a screen of upregulated genes in human B cells upon infection with EBV [1]. EBI2 is a G-protein (Gαi type) coupled receptor [2] but as long as 18 years after its discovery the nature of its ligand remained undisclosed. With the help of transfected cell lines
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Herein the interactions of etamicastat nepicastat
2020-10-30

Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the bio bio exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP remains u
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One of the most frequent gene alterations
2020-10-30

One of the most frequent gene alterations in MM is methylation of the p15 and p16 genes in the 5′ upstream region. P15 and p16 proteins are Colistin Sulfate synthesis regulators involved in the inhibition of transition from G1 to S phase. Frequencies of p15 or p16 gene methylation up to 32% and 53
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br Stem cell based therapies In
2020-10-30

Stem cell–based therapies In the previous years, excessive efforts have been conducted to induce the least aggression and more efficient sources of human cardiomyocytes for different application, particularly for myocardial regeneration. The pluripotent stem cell seems to be an appropriate candid
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br Methods br Results br Discussion Here we
2020-10-30

Methods Results Discussion Here we have shown that two GPCR subtypes thought to trigger similar signalling events by coupling to Gαq in fact regulate different signalling networks via coupling to distinct G proteins. Thus global effects regulated by both receptors in events such as cardiac
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It is particularly notable that CYP
2020-10-29

It is particularly notable that CYP2D6 appears to be the most stable of the major CYP450 KNK437 in its expression over time in vitro and appears to be least affected by culture conditions and sample to sample variability (i.e., CYP2D6 expression is remarkably consistent over time and between indivi
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br Orthotopic liver transplantation OLT is the only curative
2020-10-29

Orthotopic liver transplantation (OLT) is the only curative therapy available for patients with end-stage liver disease. The surgical procedure of liver transplantation inherently involves cold ischemia during graft preservation , followed by reperfusion of the transplanted graft which results in
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br Conclusions br Declaration of interest br Acknowledgment
2020-10-29

Conclusions Declaration of interest Acknowledgment This work was supported by an AIRC (Associazione Italiana Ricerca Cancro-Milan) Grant KFR062-2 to A.G.L, by Ricerca Funds by Fondazione IRCCS Ca’ Granda Ospedale Maggiore Policlinico (Grant No. 180/01) and by the ERA-NET “ERare” (Grant GO
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Prostaglandin E receptor subtype EP is a transmembrane G
2020-10-29

Prostaglandin E receptor subtype 4 (EP4) is a transmembrane G-coupled protein receptor activated by prostaglandin E2 (PGE2). EP4 activation exerts anti-inflammatory effects in adipose tissue by dampening the levels of inflammatory chemokines [12]. In the mouse, EP4 deficiency aggravates fragmentatio
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Collectively our results indicate that
2020-10-29

Collectively, our results indicate that GSK682753A functions as a competitive antagonist and binds to the receptor in the same region as 7α,25-OHC. First, we observe linearity in the Schild plot analysis (Fig. 2B). Second, GSK682753A is highly dependent on F111 at position III:08/3.32 in TM-III (Fig
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br Materials and methods br Results br
2020-10-29

Materials and methods Results Discussion Plant U-box E3 Ub ligases regulate diverse plant-specific cellular processes [1], [2], [3], [4]. However, structural and functional relationships between U-box E3s and their E2 partners are largely unknown in higher plants [24], [25]. In this study,
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br In half a century after its first biochemical
2020-10-29

In 2015–2016, half a century after its first biochemical characterization as a template-independent polymerase, it was shown that TdT can, firstly, assemble a DNA synapsis by itself, optimally with one micro-homology base-pair between strands [] and secondly, perform a template-dependent nucleotid
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