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Previously we reported the structure activity relationships
2020-08-06
Previously, we reported the structure–activity-relationships (SAR) of a series of pyrazinone-based CRF receptor antagonists, , , leading to highly potent and efficacious compounds such as , and ultimately to the discovery of (BMS-764459, ). Detailed SAR studies of the lower phenyl/pyridyl substituen
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In a small case series
2020-08-05
In a small case series of 4 EGFR exon 19 del/T790M NSCLCs patients with acquired resistance to Osimertinib enrolled into the AURA trial, re-biopsy after AR revealed the presence of different mechanisms of resistance: none of the 4 patients developed C797S mutation, but loss of EGFR T790M mutation wa
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Pirfenidone The experimentally determined molecular masses o
2020-08-05
— The experimentally determined molecular masses of Δ1-KSTDs are around 53-61 kDa [27,28,47,48,62,90,93,100,105,109]. The Δ1-KSTDs from R. rhodochrous IFO 3338 [27], N. simplex IFO 12069 [48], and R. erythropolis SQ1 isoenzyme 1 [30] are monomeric proteins, whereas the enzyme from S. denitrificans
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BMS-626529 australia The number substrate specificity and Ca
2020-08-05
The number, substrate specificity, and Ca2+ dependence of alternative NAD(P)H dehydrogenases vary significantly when different organisms are compared. For instance, Arabidopsis mitochondria may possess up to seven proteins, including three external dehydrogenases: two are NADH dehydrogenases, one of
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Some limitations to our study
2020-08-05
Some limitations to our study should be noted. First, the sample size of our study was limited. As DDR2 mutations are rare in lung SCC, it is possible that the power of our study was insufficient to detect potential associated factors. Second, a significant proportion of the 271 sequenced patients h
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br Movement disorders Hand stereotypies were reported
2020-08-05
Movement disorders Hand stereotypies were reported in 80% of individuals, and 59% of females and 12.5% of males achieve functional hand use, which may be limited by stereotypies. The hand stereotypies that we have observed are more consistent with self-stimulatory behavior versus the type of hand
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(±)-Bay K 8644 Additionally notice that the Szeg matric
2020-08-05
Additionally, notice that the Szegő matrices (defined in (1.3)) obey In particular, since the spectrum of is given by the closure of the set of at which the Szegő recursion enjoys a polynomially bounded solution [9], (3.10) also suffices to establish (3.5). Beyond that, (3.10) clearly implies for ,
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Although the presence of calcium
2020-08-05
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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Primary renal PNET was first reported by Seemayer
2020-08-05
Primary renal PNET was first reported by Seemayer et al in 1975. The possible etiology of rPNET is based on the theory of neural cell intussusception in the kidney during development that initiates the tumorigenesis. rPNET most commonly affects young adults, with a mean age of 30.4 years and male pr
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Inspired by all these findings and in the
2020-08-04
Inspired by all these findings and in the same direction, we have constructed pyridazinone A and B scaffolds as promising candidates for selective COX-2 inhibition (Fig. 3). Our strategy aims to designing a variety of modifications in the pyridazinone core, targeting exploring the impact of such on
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Sex also influences COMT effects on cognition
2020-08-04
Sex also influences COMT effects on cognition. Women have 20%–30% less COMT activity than men (Chen et al., 2004, Fahndrich et al., 1980). Both Raz et al. (2011)O\'Hara et al. (2006) found that sex interacted with COMT genotype such that older men who had a Val allele showed greater negative effects
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The PEPI trial showed that the
2020-08-04
The PEPI trial showed that the addition of medroxyprogesterone acetate (MPA) for 12 days per month had a stronger effect than CEE alone [32], whilst no such difference was found with a continuous combined regimen. One simple explanation is that a down-regulation of ERs occurs with continuous combine
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An Ubl modification requires several steps that
2020-08-04
An Ubl modification requires several steps that are catalyzed by three enzymes, referred to as E1 (activating enzyme), E2 (conjugation enzyme), and E3 (ligase). The SUMO E1 is a heterodimer of SAE1 and Uba2 (also known as SAE2). In brief, an Ubl is first activated by E1 through ATP hydrolysis and fo
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Interestingly anti inflammatory actions for sPLA V were also
2020-08-04
Interestingly, anti-inflammatory actions for sPLA2-V were also described in mice a few years ago in a model of autoimmune complex mediated arthritis [148]. A novel mechanism was delineated, whereby sPLA2-V promotes phagocytosis of immune complexes by macrophages to ameliorate inflammation in autoimm
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Main Text Post translational modifications by ubiquitin
2020-08-04
Main Text Post-translational modifications by ubiquitin (Ub) and ubiquitin-like proteins (Ubl) regulate a diverse array of cellular and physiological processes including protein degradation, localization, and activation. While ubiquitination has primary responsibility for targeting substrates for p
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