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EC barrier dysfunction triggered by inflammatory mediators i
2020-06-23
EC barrier dysfunction triggered by inflammatory mediators involves more than one mechanism, explaining the partial attenuation of EC barrier compromise obtained with PKA and Epac activators. PKA-dependent phosphorylation of vasodilator-stimulated phosphoprotein (VASP) has been shown to make a posit
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Imatinib STI is a first
2020-06-23
Imatinib (STI-571) is a first-line tyrosine kinase inhibitor (TKI) targeted at breakpoint cluster region-Abelson kinase (ABL) for the treatment of chronic myeloid leukemia (CML) [26]. As a type II inhibitor, imatinib achieves significant selectivity by binding to an inactive DFG-out conformation (D
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One possible explanation for differences in the binding abil
2020-06-23
One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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The importance of G S phase progression to the formation
2020-06-23
The importance of G1–S phase progression to the formation of malignant tumors has been highlighted by the high incidence of aberrations in the genes involved in this progression in a wide variety of tumors. p27Kip1 is a member of the Cip/Kip family of cyclin-dependent kinase inhibitors (CKI). Its ro
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In the context of E ligase drug discovery it
2020-06-22
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 Phe
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Just as Dorin et al and Nguyen et
2020-06-22
Just as Dorin et al. [2] and Nguyen et al. [3] write in regard to their models, our static model can be used to estimate the affinities of risperdone to albumin and CBG. Dorin et al. [2] estimates the K, but not K, since they find that their model is not particular sensitive towards changes in K. O
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Furthermore software engineering practices are important for
2020-06-22
Furthermore, software engineering practices are important for addressing productivity problems in scientific software. Even though the speed of the hardware is rapidly increasing, the additional complexity makes it more difficult for scientists to be productive developers. According to Faulk et al.,
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Previous studies showed that many
2020-06-22
Previous studies showed that many steroidogenic enzymes act when the enzyme binds to the cofactor first [30]. In the present study, we showed that HPTE inhibited both AKR1C14 and RDH2 in a mixed mode when cofactor was used. This indicates that HPTE interferes with cofactor-binding residues although
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Several extragenic cot ts suppressors have been identified
2020-06-22
Several extragenic cot-1 (ts) suppressors have been identified. Among them, cytoplasmic dynein, dynactin, and nuclear distribution mutants of N. crassa, as well as an additional gene gul-1 (NCU01197), have been shown to have genetic interactions with cot-1 (Bruno et al., 1996, Seiler et al., 2006, T
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It is noteworthy that epidemiological studies
2020-06-22
It is noteworthy that epidemiological studies have demonstrated that some GAD patients have experienced anxiety symptoms in childhood and young adulthood, whereas others have developed their disorder at a later age (especially persons ≥ 50 years of age) (Hoehn-Saric et al., 1993; Le Roux et al., 200
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The instructive precedent for galectin phosphorylation is hu
2020-06-22
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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br Acetylcholinesterase and cholinergic signaling The
2020-06-22
Acetylcholinesterase and cholinergic signaling The concept of a synapse between a neuron and an innervated cell, and the receptors that mediated their interaction, was developed by Bernard, Ehrlich, Sherrington, Langley and others (see [7], [8], [9]. It was long debated whether transmission of ne
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Neurons in the striatum unlike those in the cerebral
2020-06-22
Neurons in the striatum, unlike those in the Topotecan HCl and cerebellum, do not form a layered or columnar structure. Although they appear to be randomly distributed, they are actually scattered in two embryologically different compartments called striosomes (often referred to as “patches” in rode
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A second advance came with the discovery that conformational
2020-06-22
A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop
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Gefitinib hydrochloride Gene amplification PCR amplification
2020-06-22
Gene amplification. PCR amplifications were performed using genomic DNA from the different organisms studied as template and two degenerate oligonucleotides (PP1 and PP2) as primersPP1 corresponded to the sense codons of the amino Gefitinib hydrochloride motif AGGI(A/S)EM, and PP2 to the antisense
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