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Cordycepin Across the scaffold the platform anchors the N te
2019-09-27
Across the scaffold, the platform anchors the N terminus of the elongated cullin structure of APC2 [21]. This connects to the flexible cullin–RING catalytic core consisting of the C-terminal region of APC2 and the associated APC11 11, 12, 21. The flexibility and positions of the catalytic core are c
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Since the interaction between the E
2019-09-27
Since the interaction between the E2 and E3 is weak and transient, it has been difficult to identify novel interactions between specific E2/E3 complexes [59], [64]. Here we used a modified bait consisting of the Mulan RING domain fused to one of the four E2s isolated in our screen and expressed in y
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br Competing interests br Acknowledgements br
2019-09-27
Competing interests Acknowledgements Introduction Diacylglycerol kinase (DGK) phosphorylates diacylglycerol (DG) in biomembranes to produce phosphatidic JNJ-26481585 (PA) [1], [2], [3], [4], [5], [6]. To date, ten mammalian DGK isozymes (α, β, γ, δ, ε, ζ, η, θ, ι and κ) have been identifie
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As for antiviral activity eight out of synthesized
2019-09-27
As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).
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br Conclusion New series of
2019-09-27
Conclusion New series of thiazolo[4,5-d]pyridazine and imidazo[2′,1′:2,3]thiazolo[4,5-d]pyridazine were designed and synthesized using thiazole as scaffold based on its previously observed activity as DHFR inhibitor. Compounds 13 and 43 (Fig. 9) proved to be the most active DHFR inhibitors with I
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Cysteine protease activities have been suggested
2019-09-27
Cysteine protease activities have been suggested to be important for Giardia’s pathogenesis [[11], [12], [13],16,18,19,21,28,29,35]. Recently several giardial CPs were shown to be released during host cell interactions [9,10]. The three major released CPs have recently been shown to be involved in t
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LY 294002 pathway Here we describe a novel series of arylazo
2019-09-27
Here, we describe a novel series of arylazoderivatives developed from CAN508, one of the first known selective CDK9 inhibitors. We focused on modification of both ends of parental molecule, CAN508, in order to improve cytotoxicity and CDK activity. We therefore analyzed how changes in molecules will
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As the principal receptors for regulating the inflammatory p
2019-09-27
As the principal receptors for regulating the inflammatory process in mammals, CXCR1 and CXCR2 have an important role in regulating the trafficking of phagocytes such as neutrophils, monocytes and macrophages (Viola and Luster, 2008). The evidence gathered to date from fish studies are in agreement
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The identification of a functional leucine rich NES
2019-09-27
The identification of a functional leucine-rich NES mediating 8E7 nuclear export led us to analyze the interaction between 8E7 and CRM1 nuclear export receptor. HeLa cell lysates containing EGFP-8E7, EGFP–8cE7, EGFP-16E7–NES (as a positive control), or EGFP (as a negative control) were incubated wit
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Our comparison of all ER iso
2019-09-27
Our comparison of all ERα (iso)forms with ERβ immunostaining suggests that overall ERβ expression is lower than that of ERα isoforms. This contrasts the so far reported data for ERs in the lung, but is not a paradox; in pathology routine, ER positivity is defined stricto senso by nuclear WT ERs. As
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br Materials and methods br Results
2019-09-27
Materials and methods Results and discussion Conclusions The current research work deals with preparation of CES from RHA and comparative study of Ni (II) ion adsorption on CES and RHA. It was observed that carbon embedded silica shows more porous structure and more surface area as compared
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Although there was little to no
2019-09-26
Although there was little to no expression change observed by TELI of the recA and ruvA genes upon CAA exposure, other specific repair pathways were induced by both CAA and SO and include the SOS-inducible gene sulA, the DNA repair gene ykfG, the mismatch repair gene mutS, the recombination and repa
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The compounds were ranked based on the
2019-09-26
The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR a
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Functional studies suggested the presence of a cysLT recepto
2019-09-26
Functional studies suggested the presence of a cysLT1 receptor. We observed an LTD4-induced cytosolic calcium response, albeit one that was very weak by most standards. The magnitude of the average response was partially explained by the low percentage of gap 27 showing a very transient response. B
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In sum although it is reasonable to assume that
2019-09-26
In sum, although it is reasonable to assume that the activities of an enzyme on alternative (metabolically available) substrates may often depend on neutral drift, the point is difficult to prove because various types of selective pressures can be at play, and these will be different in different or
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