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Since the initial identification of DNA ligase inhibitors by
2019-08-09
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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The aim of this study was to evaluate
2019-08-09
The aim of this study was to evaluate the role of aberrant methylation of promoter regions of tumor suppressor genes in the clonal evolution from MGUS to MM. Thus, we analyzed in MGUS, SMM, and symptomatic MM patients, the methylation status of 4 genes—p15, p16, p53, and DAPK—whose promoter hypermet
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Interaction between neutrophils and ECs represents the
2019-08-09
Interaction between neutrophils and ECs represents the first step of the cellular phase of the inflammatory response, and provide the best condition for the transfer of the PMNL-derived LTA4 to the ECs, leading to the transcellular formation of cysteinyl-LTs. It is intriguing therefore to think that
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For LAU extracted ion chromatograms of the blank
2019-08-09
For LAU 399, extracted rac1 inhibitor chromatograms of the blank, t0, and t120 samples for the diagnostic product ion m/z 163.0216 are provided in Fig. S11, and extracted ion chromatograms of the t120 sample for m/z 163.0216 (diagnostic product ion), and m/z 308.1677 and 306.1522 (metabolites) are s
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Naringenin is the one of the
2019-08-09
Naringenin is the one of the many components in grapefruit juice. It was assumed that administration of 20mL grapefruit juice per kilogram of body weight is completely glucuronidated in the hepatic or gut wall for first pass metabolism [38]. It has been detected that one liter of grapefruit juice co
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br Materials and methods br
2019-08-09
Materials and methods Results and discussion In the present work, we have applied two methodologies, CoMFA and CoMSIA to build 3D-QSAR models. There is no crystal structure available; therefore, an indirect method i.e., a ligand-based approach is the method of choice. The highly active molecul
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Previous studies from our laboratory in CD mice using
2019-08-09
Previous studies from our laboratory in CD1 mice using the incisional postoperative pain model have shown that the incision induces significant mechanical postoperative hyperalgesia lasting between 7 and 10days, with peak effect between 4h-2days (Cabañero et al., 2009a, Cabañero et al., 2009b, Campi
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histamine receptor antagonist In mammals ribonucleotide redu
2019-08-09
In mammals, ribonucleotide reductase (RNR) is a unique enzyme that catalyzes the rate-limiting step of de novo synthesis of deoxyribonucleoside triphosphates (dNTPs).7, 8 Mammalian RNR consists of two homodimer subunits: the large catalytic dimer RRM1 and the small regulatory dimer RRM2 or RRM2B. An
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br Conclusion br Acknowledgment The authors
2019-08-09
Conclusion Acknowledgment The authors would like to thank “Science and Engineering Research Board (SERB) of Department of Science and Technology (DST) Govt. of India” (Grant No.YSS/2015/002017) for funding the project. Introduction Mutations occurring within EGFR exons 18 to 21 are present
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br Material and methods br Results
2019-08-08
Material and methods Results Discussion The present study shows that peripheral administration of the nonpeptidic corticotropin-releasing factor CRF1 receptor antagonist CP-154,526 before a social defeat inhibits the development of CPP induced with a subthreshold dose of cocaine and reverse
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Common enzyme quantitative methods include enzyme
2019-08-08
Common enzyme quantitative methods include enzyme-linked immunosorbent assay [,] (ELISA), chemiluminescence (CLIA) [, , ] and immunochromatography []. The advantages of ELISA are cost reduction and automation, but non-specific reaction caused by HOOK effect, false positive caused by cross-contaminat
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DHODH activity has been traditionally measured with
2019-08-08
DHODH activity has been traditionally measured with the standard colorimetric assay that monitors 2,6-dichloroindophenol (DCIP) reduction as absorbance decrease at 600 nm . This assay has permitted the identification of several families of DHODH inhibitors in a successful high-throughput screening (
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Beside the previously reported Topo I inhibition time
2019-08-08
Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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Several highly selective COX inhibitors coxibs
2019-08-08
Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d
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br Disclosure and conflicts of interest br Acknowledgements
2019-08-08
Disclosure and conflicts of interest Acknowledgements This research was supported by grant (BT/PR/11293/BRB/10/849/2008) from Department of Biotechnology (DBT), Government of India and a DST YOS Chair Professorship to PB. The mass spectrometry facility is supported by an institutional program
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