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Molecular docking study of compound was performed using
2020-02-20

Molecular docking study of KN-92 phosphate 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 and the cyano
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br Chemistry The test compounds listed in Table Table Table
2020-02-20

Chemistry The test compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5, were synthesized as outlined in Scheme 1, Scheme 2, Scheme 3, Scheme 4, Scheme 5. Synthesis of 2–5 is described in Scheme 1. N-Sulfonylation of the aniline 26 with benzenesulfonyl chloride afforded the sulfonamide
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br Conflicts of interest br Financial support NZ
2020-02-20

Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818
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br Biological roles of DGK br Summary and future perspective
2020-02-20

Biological roles of DGKϵ Summary and future perspectives The most K-252c segment of DGKϵ, comprised of residues 20–42, appears to have no role in binding the lipid substrate DAG or in the acyl chain specificity of substrate phosphorylation. Nevertheless, the sequence in this segment of DGKϵ i
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The presence of external NAD P H dehydrogenases
2020-02-20

The presence of external NAD(P)H dehydrogenases (NDE) on the outer surface of the inner mitochondrial membrane enables the mitochondria to oxidize cytosolic NAD(P)H (Moller 2001). A porin (a voltage-dependent anion-selective channel, VDAC) that is abundant in the outer mitochondrial membrane permits
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Calcium dependence of CaM target interaction was analyzed
2020-02-20

Calcium dependence of CaM/target interaction was analyzed using a titration matrix in which both Ca2+ and CaM concentrations were changed. This gave us access to different parameters characterizing the interaction and namely to the number of bound Ca2+ required for the interaction to occur. Our app
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Caspi et al first identified that
2020-02-19

Caspi et al. (2005) first identified that the COMT polymorphism moderated the influence of adolescent cannabis use on developing adult psychosis (Caspi et al., 2005). In particular, compared to Met carriers, subjects with the Val/Val genotype were most likely to exhibit psychotic symptoms and to dev
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Cholesterol homeostasis is maintained through a tight regula
2020-02-19

Cholesterol homeostasis is maintained through a tight regulation between endogenous de novo synthesis, dietary absorption, utilization and excretion of bile salts. The Idarubicin HCl of cholesterol from the intestine constitutes the central part of cholesterol homeostasis in the body [41]. In partic
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We further verified the presence of CLIC CLIC
2020-02-19

We further verified the presence of CLIC1, CLIC4 and CLIC5 in purified mitochondria following protocols described earlier (Singh et al., 2012). As shown in Fig. 4, CLIC4 and CLIC5 were present in the ultra-pure mitochondrial fraction (M3). All the three fractions obtained from 30% (v/v) Percoll grad
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It is common for plants
2020-02-19

It is common for plants that are deficient in P to invest in their roots in order to maximise P uptake from the soil. Here, plants grown in soil amended with OA had a higher root biomass:shoot Aclacinomycin A ratio compared with plants in the INORG-P treatment. Additionally, greater allocation of C
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Research done thus far supports
2020-02-19

Research done thus far supports the hypothesis that MPA has detrimental effects on cognition, alone and in combination with estrogen; there are other FDA-approved progestogens that satisfy the uterus opposing effects that have not been cognitively profiled. An important goal to aid women\'s health i
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In conclusion our study has demonstrated that PGE
2020-02-19

In conclusion, our study has demonstrated that PGE2 stimulates expression of survivin in hepatocellular carcinoma cells. Although there are 4 subtypes of EP receptors, the EP1 receptor appears to be the predominant receptor that regulates PGE2-induced expression of survivin, mainly through trans-act
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br Halogenases Enzymatic C H activation leading
2020-02-19

Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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The indigenous populations living at high mountain
2020-02-19

The indigenous populations living at high mountain regions of the Himalayas represent successful human 745 to hypoxia. These populations have undergone selective positive natural selection over millennia across several genomic loci and exhibit unique respiratory, cardiopulmonary and haematological
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br Results br Discussion Taking advantage of
2020-02-19

Results Discussion Taking advantage of the highly specific protein–protein interactions among cognate pterostilbene receptor that mediate SUMO conjugation to substrates, we have developed a novel strategy for achieving inhibition of SUMO conjugation in vivo based on disruption of SUMO E1–E2 i
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