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Epinastine HCl receptor Goel et al reported study of diaceto
2021-01-30

Goel et al. reported study of 7,8-diacetoxy-4-methylcoumarin (DAMC) 63 and its thiocoumarin derivative 7,8-diacetoxy-4-methylthiocoumarin (DAMTC) for their effect on human non-small cell lung cancer A549 cells. The study suggested that the 7,8-diacetoxy-4-methylcoumarin (DAMC) 63 downregulates Bcl-x
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Many studies have shown that
2021-01-30

Many studies have shown that curcumin delays the progression of atherosclerosis in different atherosclerotic animal models [18], [19], [20], [37] and the risk of atherosclerosis in human studies [15], [38], [39]. Curcumin also has many properties that contribute to combat atherosclerosis, such as an
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MNs can be obtained from iPSCs using signaling
2021-01-30

MNs can be obtained from iPSCs, using signaling molecules such as retinoic Deferoxamine mesylate (RA) and Sonic hedgehog (Shh) (Table S1).4, 5, 12, 23, 24, 25, 26, 27, 28, 29 These methods rely on developmental principles and require changing the combinations of signaling molecules at multiple step
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In SLO permeabilized human sperm the AR
2021-01-30

In SLO-permeabilized human sperm, the AR elicited by calcium, persistently active Arf6 [41] and Rab3A, 8-pCPT-2′-O-Me-cAMP [8], diacylglycerol and a non-hydrolyzable analog [35], is sensitive to the PLC blocker U73122. Furthermore, 8-pCPT-2′-O-Me-cAMP elicits a calcium signal in non-permeabilized sp
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Our results demonstrated that ET a Wnt ligand stimulated
2021-01-30

Our results demonstrated that ET-1, a Wnt ligand, stimulated the Wnt/β-catenin signaling pathway. First, ET-1/ETRA binds to Frizzled family cell-surface receptors, resulting in the activation of Dvl1, a Dishevelled (DSH) family protein. Next, activated DSH inhibits the Axin, GSK-3β, and APC protein
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br Introduction Our understanding of how ligands interact wi
2021-01-30

Introduction Our understanding of how ligands interact with G protein coupled receptors is evolving, particularly the recognition that some have the ability to preferentially activate a subset of intracellular signalling cascades – so called pathway biased ligands [1]. Additionally, it is now acc
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Carmustine br Materials and methods br Results br Discussion
2021-01-30

Materials and methods Results Discussion In this study, we employed a liquid chromatography mass spectrometry (LC–MS)-based metabolomic approach to profile GEF metabolism and bioactivation in human and mouse liver microsomes. Metabolomic approaches rendered us readily screen out the GEF-rel
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Several functions of FAT have been suggested It has
2021-01-30

Several functions of FAT10 have been suggested. It has been shown that FAT10 binds noncovalently to the mitotic spindle checkpoint protein MAD2 and that this binding might cause chromosome instability in the cancer Protease Inhibitor Library overexpressing FAT10 (Liu et al., 1999, Ren et al., 2006)
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PDK1 inhibitor br Materials and methods br Results The i v a
2021-01-29

Materials and methods Results The i.v. administration of urocortin 2 reduced the mean arterial blood pressure in a dose-dependent manner (Fig. 1). The ED50 for the urocortin 2 cumulative dose–response effect on mean arterial blood pressure was 0.014±0.004 mg kg−1. Urocortin 2 administration ha
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R547 MdHCLB channels expressed in Xenopus
2021-01-29

MdHCLB channels expressed in Xenopus oocytes produced currents in response to HA and GABA (Fig. 1, Fig. 3). This is in agreement with the findings with Drosophila HCLB channels (Gisselmann et al., 2004). In the HA concentration-response curves, the effects of GABA were additive to those of HA only i
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Primary renal PNET was first reported by Seemayer et al
2021-01-29

Primary renal PNET was first reported by Seemayer et al in 1975. The possible etiology of rPNET is based on the theory of neural cell intussusception in the kidney during development that initiates the tumorigenesis. rPNET most commonly affects young adults, with a mean age of 30.4 years and male p
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Our previous work has demonstrated that two glutamate residu
2021-01-29

Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi
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To study the effect of DDR inhibition by imatinib nilotinib
2021-01-29

To study the effect of DDR inhibition by imatinib, nilotinib and dasatinib in a cellular environment we generated DDR1 and DDR2 expressing HEK293 cell lines by stable transfection. Of the five DDR1 splice variants we focused on the 1b variant whose over-expression has been associated with pulmonary
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Historically covalent drugs have had great success e g
2021-01-29

Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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br Chain specific ubiquitin probes The conventional
2021-01-29

Chain specific ubiquitin probes The conventional way of assessing linkage specificity is by measuring turnover rates of different diubiquitin molecules as substrates. Although this method has been applied successfully in several studies [7••, 8] it is limited to isolated DUBs, whereas linkage spe
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