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The kinase activity of DNA PKcs is essential
2020-02-11
The kinase activity of DNA-PKcs is essential for NHEJ, but the exact role of the enzymatic activity of DNA-PKcs plays in NHEJ is not fully understood [57]. In vitro, DNA-PKcs can phosphorylate each of the canonical NHEJ factors including Ku70/80 [58], [59], XRCC4 [60], [61], nop receptor IV [62], a
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High throughput screening HTS of
2020-02-11
High throughput screening (HTS) of the AstraZeneca nos inhibitor collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) and w
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The focus of this review is on the diacylglycerol
2020-02-11
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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Several reports by us and others
2020-02-11
Several reports by us and others have highlighted that dimerization or oligomerization of DDR1 ECD and DDR2 ECD enhances their binding to triple-helical collagen.18, 19, 22, 28, 29, 30, 31 The ECD of DDRs consists of a discoidin domain and a stalk region. It has been reported that independent Silden
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Fatty acid oxidation plays a crucial role in maintaining
2020-02-11
Fatty HOAt β-oxidation plays a crucial role in maintaining body energy homoeostasis mainly during catabolic states. It mainly occurs in mitochondria and involves a cyclical series of reactions that result in the shortening of fatty acids. Fatty acids comprise an efficient source of energy that resu
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BLU9931 The performance of the qCPA approaches is similar
2020-02-11
The performance of the qCPA approaches is similar with regards to the derivative properties of CO2 and for mixtures of CO2+self-associating compounds. For CO2+n-alkanes the four-parameter versions of qCPA both perform somewhat better than the three-parameter version. Nevertheless this modest improve
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This structure guided the variation of the
2020-02-11
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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Targeting the MAPK pathway has attracted significant interes
2020-02-11
Targeting the MAPK pathway has attracted significant interest in cancer therapy. Efforts directly targeting RAS protein are believed to be very challenging in spite of the promise shown by a few RAS inhibitors in the early development stage. Clinical benefits achieved by BRAF and MEK inhibitors have
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ER stress was monitored by both an increase of
2020-02-11
ER stress was monitored by both an increase of the ER chaperone (GRP78, GRP94) and the activation of the ER resident caspase-12. ER stress response (also known as the unfolded protein response) is a defense mechanism against various cellular stresses which causes accumulation of unfolded proteins in
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Pharmacogenomics is the study of the
2020-02-10
Pharmacogenomics is the study of the role of the prostaglandin receptors in drug response. It was reported that the effectiveness of atorvastatin was affected by genetic factors.26, 27 In previous studies, there are many genetic polymorphisms related to the efficacy of atorvastatin. Cerda et al rep
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For in vitro expression analysis of
2020-02-10
For in vitro expression analysis of CXCL8 and CXCRs by stimulated leucocytes, peripheral blood leucocytes (PBLs) were isolated using Percoll density gradient centrifugation as described earlier . Cell suspensions were adjusted to 5×10/ml. Four milliliters of tissue culture medium were plated per wel
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br Introduction br Literature review and hypothesis
2020-02-10
Introduction Literature review and Busulfan development CPA exam performance-related research has been of interest to academics for the past few decades. These studies have ranged from investigating the impact of the 150-hour requirement on pass rates (Allen & Woodland, 2006) to examining whe
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br Introduction To detect exposure to and
2020-02-10
Introduction To detect exposure to and effects of neuroactive pesticides in aquatic organisms, one widely used biomarker is cholinesterase (ChE) activity, which, among other possible functions, catalyzes the hydrolysis of the neurotransmitter 5-Formyl-UTP synthesis (ACh) in the cholinergic synap
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SB 225002 Carbamate and OP insecticides are
2020-02-10
Carbamate and OP insecticides are still among the most widely used pesticides in the world [151]. In 2012, the OP insecticides chlorpyrifos and acephate were ranked 14th and 22nd overall in estimated amounts of agricultural pesticides used in the US. The carbamate insecticide carbaryl and the OP ins
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As plants can only take up P in an
2020-02-10
As plants can only take up P in an inorganic orthophosphate form, it was expected that the proportion of orthophosphate P in the OA would be a good indication of the availability of the P in the OA. While the P speciation of the COMP sample could not be determined by deconvolution due to the broadne
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