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Molecular docking study of compound
2020-06-09
Molecular docking study of Dihydroartemisinin synthesis was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg448
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We have previously shown that sustained pCPT treatment favor
2020-06-09
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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Hymenialdisine the most potent inhibitor of parasite TgCK en
2020-06-08
Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this Flufenamic acid also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition of
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In terms of its protease activity MME has a
2020-06-08
In terms of its protease activity, MME has a broad range of substrates being able to target glucagon, bradykinin, GLP1, and several other Haloperidol synthesis of circulating small molecules [25]. MME has been shown to target free insulin B-chain [32], although whether MME could target and degrade
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Ozagrel HCl To further confirm the roles of the CYP enzymes
2020-06-08
To further confirm the roles of the CYP450 enzymes involved in the metabolism of Dip in rat liver microsomes, we utilized not only chemical inhibitors but also a correlation analysis and a panel of recombinant rat CYP450 enzymes to evaluate the contribution of CYP450 enzymes. The results of the corr
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br Authors contribution br Disclosure statement br Acknowled
2020-06-08
Authors contribution Disclosure statement Acknowledgements This study has received funding from the Italian Ministry of University and Research (PRIN 2015, grant number 2015373Z39_008) and from the Innovative Medicines Initiative 2 Joint Undertaking under grant agreement No 115797 (INNODIA)
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In light of the overall loss of
2020-06-08
In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The
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During these processes meiotic recombination plays
2020-06-08
During these processes, meiotic recombination plays a critical role by physically associating homologs and ensures accurate chromosome segregation. In addition, meiotic recombination redistributes genetic material between homologs, resulting in haplotype diversity among progeny, impacting ecological
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The data from drug screening in P berghei Fig
2020-06-08
The data from drug screening in P. berghei (Fig. 3D) provide proof of concept that chemogenomic profiling can be accomplished in P. berghei in the same manner as P. falciparum, in that significant increases in the EC50 ratio were found only for antifolate drugs in the parasite with attenuated TgDHFR
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Pharmacogenomics is the study of the
2020-06-08
Pharmacogenomics is the study of the role of the TL32711 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 reported that SCARB
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Ung et al examined a
2020-06-08
Ung et al. examined a variety of structural features based upon the location of the DFG-motif and the αC-helix to define the conformational space of the catalytic domain of protein kinases [75]. They reported that the DFG motif can move from its active DFG-Din location to the inactive DFG-Dout locat
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In solid tumors such as those in
2020-06-08
In solid tumors, such as those in breast and pancreatic cancer, infiltrating CD68+ or CD163+ tumor-associated macrophages (TAMs) correlate with poor outcome (DeNardo et al., 2011, Kurahara et al., 2011, Shabo et al., 2008). The tumor-promoting function of TAMs is based on their capacity to secrete p
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While several C terminal peptides have been reported to
2020-06-08
While several C-terminal peptides have been reported to have modest (astressin) or substantial (astressin2-B, antisauvagine-30) subtype selectivity for the CRF2 receptor (), [125I]YP20 is the first reported small analog of the C-terminus of CRF exhibiting subtype selectivity for the CRF1 receptor vs
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Gastrodin Completion of h of education was significant in vi
2020-06-08
Completion of 150 h of education was significant in virtually all prior studies of the 150-h requirement (Allen and Woodland, 2006, Boone et al., 2006 and others). While the 150-h requirement applies to licensure, students are often permitted (as in California) to sit for the CPA exam with fewer tot
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The action of pt PGE as an
2020-06-05
The action of 17-pt-PGE2 as an EP1 receptor agonist [34] was demonstrated in several experimental settings, including cancer, neurons, vascular system, kidney and was confirmed by application of EP1 receptor selective antagonists [35], [36], [37], [38], [39], [40], [41]. Receptor binding studies in
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