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Targeting the MAPK pathway has attracted significant interes
2020-03-12

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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ISX 9 OHC is a potent regulator of LXR
2020-03-12

25-OHC is a potent regulator of LXR-mediated pathways, that impact on ISX 9 lipid homeostasis [8]. This oxysterol affects expression of the cholesterol efflux pumps ATP-binding cassette transporter (ABC)A1 [9] and ABCG1, and expression of apolipoprotein E [10], [11], [12]. 25-OHC is able to stimulat
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Structure similarity searches were conducted using the stand
2020-03-12

Structure similarity searches were conducted using the standalone version of the DALI program with the query structures scanned against a local current version of the PDB that has all chains as separate entries (Holm and Sander, 1995). The structural hits for each query were collected, even if the D
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In the livers mefenamic acid ibuprofen and meloxicam signifi
2020-03-11

In the livers, mefenamic acid, ibuprofen, and meloxicam significantly reduced expression of both 20-HETE and EETs synthesizing cyp450 genes (ANOVA, p value 0.05, Fig. 6). Control group: The lobular architecture and zonal accentuation in the liver of the control group were well preserved and kept
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Although the phase I clinical trial of LMB
2020-03-11

Although the phase I clinical trial of LMB was unsuccessful, the detailed review of this trial only mentions some malaise and anorexia as side effects, which are common for most effective chemotherapeutic drugs. These side effects may diminish if lower doses are administered. In view of the novel CR
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Unexpectedly CRF receptor agonist and antagonist evoked
2020-03-11

Unexpectedly, CRF2 receptor agonist and antagonist evoked similar effects in the fall in tail skin temperature caused by restraint. However, Ucn3 reduced basal values of tail skin temperature, thus indicating that some degree of basal vasoconstriction caused by BNST treatment with Ucn3 may have cont
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Our results for imidacloprid were unexpected
2020-03-11

Our results for imidacloprid were unexpected: considering that imidacloprid (Im) is a neonicotinoid insecticide with a different mode of action (agonist of the nicotinic btk inhibitor receptor) than OPs, we expected Es-ChE and T-ChE activity to be largely insensitive to changes in Im concentrations.
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In studies directed toward the development of sequence speci
2020-03-11

In studies directed toward the development of sequence-specific major-groove binding small TKI-258 sale [11], we desired a non-intercalating molecular scaffold that could direct attached moieties into the major groove. As an initial step toward this goal, we wished to study the DNA binding mode and
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Herein in continuation of our interest in designing new
2020-03-11

Herein, in continuation of our interest in designing new DNA photocleavage agents [18], we report the synthesis, characterization and DNA binding and cleaving properties of a novel compound: trans-N,N-dimethyl-10,11-di(pyridin-4-ium)-10,11-dihydro-9,12-dioxobenzo[e]phenanthrene tetrafluoroborate (1)
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Many studies have found that
2020-03-11

Many studies have found that there is an aberrant DNA methylation in the imprinting control region of development-related genes in the spermatozoa of oligozoospermic men (Kobayashi et al, 2007, Marques et al, 2004, Marques et al, 2008), which most likely results from expressional changes in the DNMT
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In general the DNMT encompass three
2020-03-11

In general, the DNMT encompass three different structural regions: N-terminal regulatory domain, C-terminal catalytic domain and a central linker region (). The N-terminal regulatory domain is particularly implicated in determining subcellular localization of the DNMT and in allocating unmethylated
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br Acknowledgments Studies in the Tomkinson
2020-03-11

Acknowledgments Studies in the Tomkinson laboratory on DNA ligase III are supported by research grants from the National Institutes of Health (P01 CA92584 and ES12512 to AET), a grant from the V Foundation and the University of New Mexico Cancer Center. Introduction Ionizing radiation (IR) as
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LY 2157299 Given the excellent in vitro pharmacology profile
2020-03-11

Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic LY 2157299 functionality of 1. Acetonitrile 49 was found to have a good balance of DGAT-1 inh
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br Introduction Biocatalysis can be
2020-03-11

Introduction Biocatalysis can be used to synthesize chiral building blocks, such as monomers for polymer materials, and precursors for pharmaceuticals [[1], [2], [3], [4]]. Enzymes are very suitable for catalyzing reactions with high enantioselectivity to obtain chiral products. For instance, alc
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While showing that deletion of EP maintains
2020-03-11

While showing that deletion of EP1 maintains femur bone volume fraction and trabecular bone parameters during aging, perhaps more importantly we have also demonstrated that increased initial BV/TV in EP1 is protective against OVX-induced bone loss. That is, while mice lose an approximately equal pe
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