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The authentic PPase was purified from B subtilis as
2019-09-21
The authentic PPase was purified from B. subtilis as described previously [21], whereas the recombinant enzyme was purified to homogeneity from E. coli by a simplified procedure including only phenyl-Sepharose CL-4B column chromatography and DEAE-HPLC [21]. About 26 mg of pure enzyme was obtained fr
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We have previously disclosed the discovery of
2019-09-21
We have previously disclosed the discovery of a 7-azaindole-3-acetic 99026 kinase CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of that work
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Alvocidib flavopiridol is a piperidine chromenone
2019-09-20
Alvocidib (flavopiridol) is a piperidine-chromenone derivative (Fig. 6D) that is not FDA approved, but is in clinical trials for breast, endometrial, and several other cancers and hematological malignancies (Table 4) [[100], [101], [102], [103], [104]]. This drug targets CDK9 (IC50 = 3.2 nM) and CDK
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In summary these findings show that the knockdown of
2019-09-20
In summary, these findings show that the knockdown of tra2 in the Drosophila fat body results in an increased triglyceride phenotype, which could be explained in part by altered splicing of the gene coding for the lipid breakdown enzyme, CPT1. These findings are consistent with previous studies anal
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Phenylbenzofurans are a very important molecule skeleton
2019-09-20
Phenylbenzofurans are a very important molecule skeleton due to their synthetic versatility and their proved pharmacological properties [2]. They are synthetic compounds in which an additional phenyl ring is present in any position of the benzofuran nucleus. This could be easily obtained possible by
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In our former work our interest was in discovery
2019-09-20
In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b
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In many studies spatial and temporal expression and subcellu
2019-09-19
In many studies, spatial and temporal expression and subcellular localizations of the DNMTs are examined in greater detail. These studies are evaluated and discussed in the remaining part of the article. DNMT1 protein expression was characterized in the genital ridge of the primitive mouse gonad at
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Introduction BRs are well known class of steroid
2019-09-19
Introduction BRs are well known class of steroid phytohormones involved in the regulation of key processes of plant growth and development [1], [2], [3], [4], [5]. A lot of attention is driven to BRs in the last decade because of their undeniable functions in promoting Propidium iodide reactions
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In our current work we have undertaken liquid phase combinat
2019-09-19
In our current work, we have undertaken liquid phase combinatorial synthesis methods for the synthesis of 1,2,5-trisubstituted benzimidazole derivatives as hDHODH inhibitors. Synthesised TRAM 39 were also screened by molecular docking studies over the reported hDHODH structure. The synthesised mole
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Compound was advanced to a chronic
2019-09-19
Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, phenanthroline 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured da
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br Introduction Cerebral stroke causes an efflux of various
2019-09-19
Introduction Cerebral stroke causes an efflux of various groups of progenitor and stem cells from bone marrow to bloodstream and the levels of these cells correlate with neurological status of stroke patients (Gójska-Grymajło et al., 2012, 2018). It is thought that paracrine factors produced by t
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In this study we were
2019-09-19
In this study, we were able derive new insights into the biology of DDR2 including the demonstration that cellular tyrosine phosphorylated proteins co-localise with DDR2 and exogenously added collagen I (Fig. 1G). This finding suggests that similar to the focal adhesion complexes associated with int
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br Conclusions br ISG is an ubiquitin like protein that
2019-09-19
Conclusions ISG15 is an ubiquitin‐like protein that is induced by treating mammalian thrombin inhibitors with interferon‐α/β. UbE1L was identified as the E1‐activating enzyme for ISG15 in the course of experiments that demonstrated that the nonstructural or NS1 protein of influenza B virus inhi
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br Materials and methods br Results br Discussion The presen
2019-09-19
Materials and methods Results Discussion The present study shows that 1) overexpression of wild-type or mutant α-SYN interferes with forskolin-induced DBH up-regulation, 2) α-SYN enters into the nucleus and is able to bind to CRE region, compete for CREB, and attenuate CRE-mediated transcri
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The kinase activity of DNA
2019-09-19
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], Sodium Phenylbutyrate I
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