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We elucidated that the ten
2021-01-07
We elucidated that the ten DGK isozymes have different relative 1-MGK and 2-MGK activities vs DGK activity under the same conditions. However, because the octylglucoside-mixed micellar assay was developed for DGK, it is not known whether the DGKs exhibit maximum 1-MGK and 2-MGK activities in this as
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br Experimental section br Author contributions br
2021-01-07
Experimental section Author contributions Acknowledgements Introduction Many CHIR-124 in cells are sequential enzymatic reactions where the product of one enzyme serves as the substrate of a second enzyme (1, 2). Experimental evidence suggests that some of these consecutive enzyme-cataly
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Herein we explored by docking
2021-01-07
Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the
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Besides by substrate and product KSTDs may also be
2021-01-07
Besides by substrate and product, Δ1-KSTDs may also be inhibited by other steroids. N. simplex ATCC 6946 Δ1-KSTD was strongly inhibited non-competitively by dicortinone (60), a steroidal dimer, and by bis-1-dehydrodicortinone, with values of 0.7 and 0.75 μM, respectively. This enzyme was also inhib
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DDR plays a crucial role in regulating a wide variety
2021-01-07
DDR2 plays a crucial role in regulating a wide variety of fundamental cellular processes, including cell proliferation, differentiation, and adhesion [17], [28], [29], [30]. The authors revealed compromised cell migration in DDR2-silenced fibroblasts exposed to Ang II, most likely due to the loss of
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While these previous correlative studies
2021-01-07
While these previous correlative studies have measured tDDR1 protein by IHC, these studies have not considered that pDDR1 could also be an important marker of cancer prognosis. A phosphoproteomic survey of lung cancer tissues did identify pDDR1 as one of the most commonly phosphorylated receptor kin
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Given the importance of cysteine cathepsin inhibitors as put
2021-01-07
Given the importance of cysteine cathepsin inhibitors as putative therapeutic molecules and microbial virulence factors, we chose to investigate whether Yersinia enterocolitica may be a potent producer of such inhibitors. Y. enterocolitica is the most heterogeneous species within the genus Yersinia.
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Introduction Since the recognition of AIDS in more than
2021-01-07
Introduction Since the recognition of AIDS in 1981 more than thirty-five years ago, nearly 70 million individuals have been infected with human immunodeficiency virus type 1 (HIV) and roughly half have died (http://www.unaids.org/en/resources/documents/2016/AIDS-by-the-numbers). Although the introd
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Oleamide mg FGF ERK signaling has been
2021-01-06
FGF/ERK signaling has been implicated in epithelial-mesenchymal interactions in a wide range of tissues (Huh et al., 2015, Klein et al., 2006, Rice et al., 2004, Zhang et al., 2006, El Ramy et al., 2005, Volckaert and Langhe, 2015). During embryonic organogenesis and in adult organs, we often observ
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Nevertheless because of the preclinical work and the
2021-01-06
Nevertheless, because of the preclinical work and the interference with EWS–FLI1 transcriptional activity, we believe that there may be a role for ET-743 in Ewing sarcoma. An analysis of the pharmacokinetic data published in the phase II clinical trial shows that at most the drug spent 5 to 6days ou
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Recently roflumilast has been approved as
2021-01-06
Recently, roflumilast has been approved as the first selective PDE4 inhibitor for the treatment of chronic obstructive pulmonary disease (COPD) [2]. Roflumilast has been suggested to target several different pathogenetic mechanisms, including inflammation, fibrotic, emphysematous and vascular remode
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Cyclosporine NEORAL Oral Solution Novartis is
2021-01-06
Cyclosporine (NEORAL® Oral Solution, Novartis) is an immunosuppressant widely used in organ transplantation and many other clinical conditions [12]. It undergoes extensive hepatic and intestinal biotransformation mainly via the metabolizing enzyme, CYP3A4 [[12], [13], [14], [15]]. Considering the na
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Altogether these data suggested that GlmU might be
2021-01-06
Altogether these data suggested that GlmU might be involved in the M. smegmatis biofilm mediated defence mechanisms. GlmU belongs to a metabolic pathway leading to UDP-GlcNAc from fructose-1-phosphate involved in the biosynthesis of peptidoglycan and lipopolysaccharide (Fig. 8). Recently, we demonst
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The focus of this review is on the diacylglycerol
2021-01-06
The focus of this review is on the diacylglycerol acyltransferase (DGAT, EC 2.3.1.20) enzymes, DGAT1 and DGAT2, that catalyze the esterification of a fatty acyl moiety to a DAG molecule to produce TAG. These enzymes commit DAG to being stored as TAG rather than being diverted for the synthesis of ph
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Our observation that FAK is downregulated in
2021-01-06
Our observation that FAK is downregulated in vascular smooth muscle Tirofiban hydrochloride monohydrate on fibrillar collagen confirms observations reported for other cell types [14]. However, unlike the results reported previously [14], our work suggests that matrix rigidity per se does not determi
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