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Interestingly from our consensus SBVC protocol only few comp
2019-12-04
Interestingly, from our consensus SBVC protocol only few compounds (less than 150) have been scored with a full ‘ consensus’. That means that these compounds appear in the top 5% of the database when ranked by every scoring function independently. After visual inspection, we have realized that two a
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We have previously shown that
2019-12-04
We have previously shown that sustained 8-pCPT treatment favored Ca2+-dependent arrhythmogenic activity in rat ventricular cardiomyocytes [8]. Fig. 2 shows line-scan Ca2+ images of myocyte incubated without (Fig. 2A left) and with 8-pCPT (Fig. 2A right) subjected to a train of electrical stimulation
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Dyphylline Our study shows that deletion of Dpf in mouse ESC
2019-12-03
Our study shows that Dyphylline of Dpf2 in mouse ESCs decreased their self-renewal ability and dramatically impaired their differentiation into mesoderm and endoderm while promoting neural ectoderm differentiation. The differentiation defect to meso-endoderm could be rescued by restoring Tbx3 level
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We recently employed a functional drug screening approach
2019-12-03
We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito
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parp inhibitors At one time the biological
2019-12-03
At one time, the biological effects of cAMP were thought to be mediated exclusively by Protein Kinase A (PKA). Consistent with this, PKA inhibitors have been shown to reverse the effects of cAMP-elevating agents on VSMC proliferation [5]. However, we recently reported that cAMP-mediated inhibition o
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The growth inhibitory effect of PGE has been linked to
2019-12-03
The growth inhibitory effect of PGE2 has been linked to the ability of Gs coupled PGE2 receptors EP2 and EP4 to mediate elevation of cAMP [22], [23]. Evidence suggests that this mechanism may not be the key cause of growth inhibition [24]. In various cell types, EP4 receptor has been shown to utiliz
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Based on the SUMO SIM interaction involved in
2019-12-03
Based on the SUMO–SIM interaction involved in SUMOD positioning, a SUMO2ΔSBD (SIM-binding domain; Q30A, F31A, I33A) mutant can be investigated that disrupts this important binding interface (Eisenhardt et al., 2015; Meulmeester, Kunze, Hsiao, Urlaub, & Melchior, 2008). In Fig. 4A, multiturnover assa
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br Material and methods br Results and discussion br
2019-12-03
Material and methods Results and discussion Conclusions Acknowledgements S. De thanks DST, New Delhi for generous grant of the SERC Fast Track Scheme No. SR/FT/CS-057/2008. R. Kundu thanks the University of Kalyani for financial assistance. We are grateful to Prof. K. Bhattacharyya of IA
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Several research groups have disclosed potent and selective
2019-12-03
Several research groups have disclosed potent and selective DGAT-1 inhibitors from several chemically-distinct series. Pre-clinical studies with these compounds have confirmed that small molecule DGAT-1 inhibitors can elicit metabolic outcomes comparable to those observed in DGAT-1−/− mice.19, 20, 2
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FH1 br Conclusions This study showed that
2019-12-03
Conclusions This study showed that in EOC cells, tyrosine kinase receptor DDR1 was expressed mainly in EOC FH1 with an Epithelial phenotype. The repressed expression of DDR1 in EOC cells with Mesenchymal phenotype could be due to the higher CpG methylation levels observed at the promoter of this
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br Materials and methods br Results and discussion br
2019-12-03
Materials and methods Results and discussion Conclusions Clitocypin is another member of the mycocypin family of cysteine protease inhibitors that is unique to Dapivirine shown to exhibit strong insecticidal activity against Colorado potato beetle larvae. This effect is concentration depen
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Recently we have demonstrated that the
2019-12-03
Recently we have demonstrated that the synthesis of cysteinyl-LTs from LTA4 by human umbilical vein endothelial cells (HUVECs) is directly associated with the activation of the CysLT2 receptor (CysLT2R) in a typical autocrine fashion, and that solely the CysLT2R is responsible for the increase in in
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The excitatory amino acid L glutamate or
2019-12-03
The excitatory amino R547 L-glutamate or glutamate mediates most of the excitatory neurotransmission within the mammalian central nervous system (CNS) and has been implicated in numerous peripheral nervous system (PNS) pathways. The excitatory amino acids, including glutamate, are of great physiolog
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br Pre clinical combination studies using
2019-12-03
Pre-clinical combination studies using CSF-1/CSF-1R inhibitors In preclinical models, the CSF-1R pathway can be blocked by using either small molecule kinase inhibitors (GW2580 [30], PLX3397 [31], Ki20227 [32], BLZ945 [33] and CYC11645 [34]), antibody-mediated inhibition of CSF-1 using 5A1 [35] o
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In this context we initiated a program to develop
2019-12-02
In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in apexbio chemicals replication: the host (human) dihydrofolate reductase (DHFR) [21]. We recently identified this enzyme as the molecular target of 1-aryl-4,6-diamino-1,2-dihydrotriazines,
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