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Molecular docking study of compound was performed using the
2020-04-09
Molecular docking study of allopurinol zyloprim receptor 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 Arg
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br Materials and methods br Results br
2020-04-09
Materials and methods Results Discussion Plant U-box E3 Ub ligases regulate diverse plant-specific cellular processes [1], [2], [3], [4]. However, structural and functional relationships between U-box E3s and their E2 partners are largely unknown in higher plants [24], [25]. In this study,
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br Conclusions There is significant interest in understandin
2020-04-09
Conclusions There is significant interest in understanding the contribution of biological mechanisms to the non-linear/bilinear dose–response curves for DNA-reactive agents. Model monofunctional alkylating agents have datasets amenable to PoD determination for genotoxic effects in both in vitro a
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Introduction PGE is a major mediator present at
2020-04-08
Introduction PGE2 is a major mediator present at sites of inflammation [1]. It is well established that PGE2 contributes to the localized and systemic symptoms of inflammation. A key study by Portanova et al. [2] demonstrated that anti-PGE2 SAR-302503 australia were able to reverse the swelling and
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Intriguingly one E residue may
2020-04-08
Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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These studies established IAP proteins as dimeric RING E
2020-04-08
These studies established IAP proteins as dimeric RING E3 ligases, but did not account for the essential role of dimerization. In IAPs and related E3s, such as RNF4 and MDM2, dimerization not only depends on contacts from the core RING domain but also residues N- and C-terminal to the RING domain (B
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nebivolol hcl The instructive precedent for galectin
2020-04-07
The instructive precedent for galectin phosphorylation is human galectin-3 (hGal-3). Its serine modification by protein kinase CK1 in the N-terminal tail is relevant for nuclear export during the course of apoptosis regulation and contact formation with the neural cell adhesion molecule L1 , , , . T
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It is now known that
2020-04-07
It is now known that cholinergic signaling plays a vital role in controlling many peripheral functions including skeletal and smooth muscle contraction, autonomic postganglionic neuron activation, parasympathetic end-organ activation (e.g., salivary, lacrimal and bronchial glands), regulation of car
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Although the presence of calcium in RHA P active site
2020-04-07
Although the presence of calcium in RHA-P active site is confirmed by the homology modeling, some additional observations can be made following the metal depletion and reconstitution experiments performed on RHA-Phis. EDTA-treated RHA-Phis recovers its activity in the presence of divalent cations su
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br Material and methods br Results and discussion br
2020-04-07
Material and methods Results and discussion Conclusions Prostanoid-E receptor selective antagonists that inhibit EP2 or EP4 receptor activities may be used as a pharmacological strategy to limit cyst formation and ADPKD progression. Our study follows on from our previous observations of the
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The discoidin domain receptors DDR and DDR are receptor
2020-04-07
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases that are activated by different types of collagen (Shrivastava et al., 1997, Vogel et al., 1997). Both receptors interact with a number of fibrillar collagens, and DDR1, but not DDR2, is also activated by the network-formin
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A previous study suggested that DARs and octopamine tyramine
2020-04-07
A previous study suggested that DARs and octopamine/tyramine receptors (OARs/TARs) have close pharmacological properties (Beggs et al., 2011). Their relationships were also supported by phylogenetic analyses (Balfanz et al., 2005, Hauser et al., 2008, Wu et al., 2014), indicating that some of DAR an
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In addition to glutamatergic inputs the
2020-04-07
In addition to glutamatergic inputs, the RTn integrates cholinergic, serotonergic and noradrenergic synapses of fibers coming from nuclei located in the brainstem (Asanuma, 1992, Morrison and Foote, 1986, Pare et al., 1988) involved in the alternating firing mode and in the frequency changes of reti
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Electron transport via DHODH activity
2020-04-07
Electron transport via DHODH activity will allow the generation of mitochondrial ROS without the consumption of α-ketoglutarate or NADH. Glutamine-dependent flux through the TCA cycle and oxidative phosphorylation can also enable generation of mitochondrial ROS (Weinberg et al., 2010). The latter pr
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The second DDR binding partner identified
2020-04-07
The second DDR1-binding partner identified here, Shp-2, which was not found in the two-hybrid screen but using a bioinformatics approach, is also a mediator of cell migration. Since Shp-2 has two SH2 domains, as well as phosphotyrosine phosphatase enzymatic activity and two C-terminal tyrosines targ
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