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E ubiquitin ligases are key players in the ubiquitin proteas
2020-04-18
E3 ubiquitin ligases are key players in the ubiquitin-proteasome pathway because they catalyse ubiquitination of substrate proteins.39, 40, 41 As important regulators of cellular ubiquitination, E3 ligases are emerging as attractive drug targets, particularly in cancer.42, 43, 44 However, E3 ligases
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The expression of EBI has been found
2020-04-17
The expression of EBI2 has been found to be dysregulated in several types of B cell malignancies and is thus reduced in e.g. diffuse large B-cell lymphomas [12] and chronic lymphocytic leukemia [13] and increased in post-transplantation lymphoproliferative disorders (PTLDs) [14]. EBI2 is also highly
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GLP signaling mediates important renal functions as
2020-04-17
GLP-1 signaling mediates important renal functions [101], as suggested by the expression of both DPP-4 and GLP-1R in the kidney of several species, including humans [102]. However, controversial data exists on the specific expression pattern of these proteins, based on the specificity and sensitivit
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The in vivo IC M in the adipose tissue
2020-04-17
The in vivo IC (0.0003μM) in the adipose tissue assay is in very good agreement with the in vitro IC (0.0005μM), and it is larger than the one measured in the OLTT assay (0.00005μM) for this compound. These differences in in vivo IC between OLTT and TAG synthesis are expected as we used free VX-950
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BIIB021 Interestingly genome wide association studies have l
2020-04-17
Interestingly, genome-wide association studies have linked the chromosomal region harboring RDHE2 (SDR16C5) and seven other genes to stature and growth in cattle, humans, and pigs [30], [31], [32], [33], [34], [35], [36], [37], and beak deformity in chickens [38]. The most recent study specifically
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Another question concerns the mechanism
2020-04-17
Another question concerns the mechanism of PC reduction during the phosphate starvation response. There are at least three main mechanisms of PC depletion: suppression of PC synthesis due to substrate exhaustion, downregulation of PC synthase expression by suppression of gene transcription or intens
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Tigecycline receptor Organ fibrosis is thought to
2020-04-17
Organ fibrosis is thought to be initiated by repeated or chronic epithelial injury. The current belief is that damaged epithelial Tigecycline receptor induce an aberrant and unresolved wound repair process by activating fibroblasts via various profibrotic cues. Upon injury, epithelial cells activat
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Activating GSK signaling to inhibit PK signaling during isch
2020-04-17
Activating GSK3β signaling to inhibit PK signaling during ischemia/reperfusion (I/R) is protective of WM ischemic injury. Glycogen synthase kinase (GSK3), which was the first substrate identified for AKT [44], is inhibited by AKT phosphorylation at positions S9 and S21 [45]. When GSK3β is active, it
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Propranolol initially discovered in is first and most widely
2020-04-17
Propranolol, initially discovered in 1964, is first and most widely studied as a non-selective beta-blocker. Propranolol through β-adrenergic receptor blockade has reduced heart rate and blood pressure and have anti-arrhythmogenic and anti-ischemic effects, and been proposed as an effective strategy
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Organometallic compounds exhibited remarkable potential for
2020-04-16
Organometallic compounds exhibited remarkable potential for the development of new cancer drugs not only due to the direct cytotoxicity but also to the drug targeting and active anticancer immune response ability [4]. Among the organometallic compounds, ferrocene is one of the most well-known compou
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A An optimized BEI SEIscore based
2020-04-16
(A) An “optimized BEI-SEIscore” based on the trends, emerged from the statistical analysis of several optimization studies in pharmaceutical industry (Abad-Zapatero, 2007, Abad-Zapatero and Blasi, 2011). This type of optimized scores has been used in many previous studies. Ki=1nM at 300° K, compare
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Flexible alignment of isopropylphenylaminobenzimidazole with
2020-04-16
Flexible alignment of 7-isopropylphenylaminobenzimidazole 16 with the lead Tirapazamine 1 was performed using MOE. It was found that the aryl group of compound 16, exemplified as a yellow circle in Figure 2, overlapped well with the corresponding alkyl chain of compound 1 as well as the other key f
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The importance of mitochondria as site
2020-04-16
The importance of mitochondria as site of aerobic oxidation of metabolic fuels, such as FA, has been recognized for a long time. It has been observed that the number of mitochondria may vary in response to cellular metabolic requirements and hormonal environment (Gao et al., 2014). In order to susta
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On top of the hardware ASTS employs
2020-04-16
On top of the hardware, ASTS employs Linux SUSE with High-Availability (HA) Extension: a COTS OS provided with two clustering software (Pacemaker Cluster Resource Manager (CRM) and Corosync) responsible for resources orchestration, failure diagnosis, nodes coordination, and fail-over management. The
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br Transparency document br Results and
2020-04-16
Transparency document Results and Discussion Experimental Procedures Acknowledgments The casein kinase 1 (CK1) family consists of at least seven different gene products, often referred to as isoforms (α, β, γ1, γ2, γ3, δ, ε, with splice forms described for CK1α, γ, and ε (reviewed in )
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