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Several main strategies for targeting E s described
2019-08-21
Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f
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Against this backdrop we set out
2019-08-21
Against this backdrop, we set out to identify synthetic and endogenous ligands that bind directly to and regulate the activity of Nurr1. Owing to the pivotal role Nurr1 plays in producing and processing dopamine, and the need for neurons to tightly regulate dopamine levels, we postulated that the re
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Resistance to SP is linked to
2019-08-21
Resistance to SP is linked to point mutations that accumulate at several sites in the dihydrofolate reductase (dhfr) and dihydropteroate synthase (dhps) donepezil hydrochloride in of P. falciparum (Roper et al., 2003). These mutations have been identified in codons 16, 51, 59, 108, and 164 in the d
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Introduction Collagen deposition is a common feature found
2019-08-20
Introduction Collagen deposition is a common feature found in cancerous tissues and fibrotic organs/lesions. It is now well accepted that collagen deposition is not just a consequence of disease, but that it can also trigger a vicious cycle. Both chemical and physical signals elicited from collagen
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The nucleus accumbens is a critical
2019-08-20
The nucleus accumbens is a critical locus for ER/mGluR signaling in the context of addiction ER/mGluR signaling is regulated by caveolin proteins and palmitoylation Because of the vast implications of ER/mGluR association, it is important to understand what regulates their interaction. Such regu
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Further proof is required as to whether ER membrane receptor
2019-08-20
Further proof is required as to whether ER membrane receptors play a role in the maintenance of bone mass. It is also possible that other non-genomic pathways may be involved. Nevertheless, whatever the precise mechanism of action of estrogens may be, the imbalance between bone formation and resorpt
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The prospects of the use of this
2019-08-20
The prospects of the use of this novel approach for the selective local thermo-activation of enzymes include biomedical and biotechnological applications. As NPs could be engineered to gain access to Amphotericin B calculator through the endosomal compartment [47] or through non-endocytotic pathway
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In general we observed that the enolase gene with highest
2019-08-20
In general, we observed that the enolase gene with highest mRNA levels was TVAG_043500, under all three iron concentration conditions. mRNA levels for this gene are very similar in normal and iron rich cultures (73.9 and 78.1 fold change, respectively), and higher in iron depleted cultures (118.3 fo
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During the past few years several studies have addressed
2019-08-20
During the past few years, several studies have addressed macrophage phenotype in experimental models, such as angiotensin II-induced AAA. A first study investigated macrophage phenotype using flow cytometry to identify M1 and M2 macrophages and qPCR analysis for expression of NOS2 and Ym1/2. The au
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Three kinase inhibitors dasatinib type I imatinib type
2019-08-20
Three kinase inhibitors dasatinib (type I), imatinib (type II) and nilotinib (type II), identified initially as inhibitors of tyrosine kinase BCR-ABL, were found to target DDRs in a chemical proteomic profiling study (Bantscheff et al., 2007, Hantschel et al., 2008). These tyrosine kinase inhibitors
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Some natural products such as curcumin resveratrol and sulfo
2019-08-20
Some natural products, such as curcumin, resveratrol, and sulforaphane, are known to activate Nrf2 in both in vivo and in vitro experimental models where Nrf2-mediated gene Calmidazolium chloride in plays a crucial protective role [8]. Under basal conditions, Nrf2 binds to Kelch-like ECH-associated
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To assess whether the described cooperation between
2019-08-20
To assess whether the described cooperation between the EGFR and FGFR receptors was relevant at the clinical level, we determined the effect on progression-free survival of FGFR1 expression in patients with adenocarcinoma who were receiving erlotinib or gefitinib. As we had observed EGFR-FGFR1 coope
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The modification of proteins with the small amino acid
2019-08-20
The modification of proteins with the small 76-amino CD 3254 manufacturer protein ubiquitin (Ub) plays a central role in many key cellular processes. Ubiquitylation of a target protein requires the concerted action of a cascade of three enzymes (Figure 1). The ubiquitin-activating enzyme (E1) cataly
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br Acknowledgement br Introduction Human dihydroorotate
2019-08-20
Acknowledgement Introduction Human dihydroorotate dehydrogenase (hDHODH), a flavin-dependent mitochondrial enzyme involved in de novo xpo 1 biosynthesis, is a validated therapeutic target for the treatment of autoimmune diseases such as rheumatoid arthritis and cancer [1], [2], [3]. Leflunomi
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While the mechanism of DHODH inhibition induced
2019-08-20
While the mechanism of DHODH inhibition-induced differentiation is not fully understood, this phenomenon may be caused by pyrimidine depletion. Pyrazofurin, an inhibitor of OMP decarboxylase, was able to induce differentiation and suggests pyrimidine depletion as a potential mechanism (Sykes et al.,
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