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MLN another selective Aurora A
2023-10-07
MLN8237, another selective Aurora-A inhibitor is said to be more potent than MLN8054 and to cause less benzodiazepine-like side effects based on structure modulation by the addition of a methoxy group to either end of the MLN8054 molecule. It was studied [62] in a once daily (QD) schedule for 7 days
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In addition to drawing attention to Ser
2023-10-07
In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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Aromatization of the pyrrole ring after anion capturing
2023-10-07
Aromatization of the pyrrole ring after anion capturing, using acceptor atoms with electron deficiency (B & Be), and substitution of strong electron withdrawing groups such as CN were three strategies used to design a new class of anion receptors. Comparison of the anion affinities of these anion re
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Placental cells also express P
2023-10-07
Placental cells also express P450 aromatase (CYP19A1, encoded by CYP19A1). In the placenta, this enzyme requires an external source of androgens, provided by the adrenal gland of the fetus, to form estrogen. The fetal adrenal gland produces dehydroepiandrosterone (DHEA) [9] and, in the placenta, it
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We made a number of choices in
2023-10-07
We made a number of choices in the original design of our experiments. First, we used only portions of the 5′ and 3′ regulatory elements from S. cerevisiae. The sequences of these regions were known [32] and our goal was to express the Pf-DHFR at low levels. In fact, our choice of only 600 bp of the
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The rescue of the behavioral deficit was associated with a
2023-10-07
The rescue of the behavioral deficit was associated with a significant reduction in the levels of both soluble and insoluble Aβ peptides and their deposition in the Oxaprozin mg of the same animals. In search for the mechanism behind the reduced amyloidosis, we assessed APP metabolism. Confirming pr
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APPL is highly expressed in pancreatic cells but
2023-10-03
APPL1 is highly expressed in pancreatic β cells, but its levels are significantly decreased in several mouse models of obesity and diabetes, including HFD-induced obese mice and db/db mice [6], [73], suggesting that the dysregulation of APPL1 may be associated with malfunction of the pancreas in obe
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The cellular mechanism underlying the CGS
2023-10-03
The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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tachykinin In conclusion the results of this investigation s
2023-10-03
In conclusion, the results of this investigation suggest that the involvement of PGE2 in the pathogenesis of pulpal inflammation and repair may be related to its induction of cAMP production. PGE2-induced cAMP production in dental pulp cells is mediated by binding to the EP2 receptor, activation of
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br Discussion The clinical course of our patient
2023-10-03
Discussion The clinical course of our patient until May 2012 was rather typical of early onset AChR-MG. Later on, the pattern of the disease was more typical of MuSK-MG, as evidenced by the distribution of myasthenic weakness and the unprovoked exacerbations. The cannabinoid receptors of MuSK-MG
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Because of its role in tumor
2023-10-03
Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t
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In this paper we describe the formation of
2023-10-03
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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It was previously demonstrated that dissociation
2023-10-03
It was previously demonstrated that dissociation of the V-ATPase in response to glucose depletion in yeast requires an intact microtubular network [28] and a catalytically active enzyme [29]. Interestingly, mutations in the non-homologous region of the catalytic subunit A are able to block dissociat
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In response to DSB the lesion recognition factor Mre Rad
2023-10-03
In response to DSB, the lesion recognition factor Mre11-Rad50-Nbs1 (MRN) complex helps the recruitment of ATM to the damage site and its activation by phosphorylation [29]. However, whether UV-damage recognition factors directly influence ATR and ATM recruitment and their phosphorylation is not clea
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br Introduction Throughout early prophase I meiotic
2023-10-03
Introduction Throughout early prophase I, meiotic cells intentionally generate DSBs as part of a stringently controlled process to initiate homologous recombination (HR). HR is a critical DSB repair pathway that ultimately permits the exchange of genetic information between homologous chromosomes
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