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br Resistance to targeted therapy The idea
2021-09-09

Resistance to targeted therapy The idea of treating HER2 mutant tumors with specific therapies is relatively new and, as a consequence, little is known about the potential mechanisms of resistance to anti-HER2 agents in this setting. Primary resistance may be mediated by the presence of on-target
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In our study we found
2021-09-09

In our study, we found that HER2-mutant lung cancers occurred commonly in female patients with an advanced stage at time of diagnosis and in a relatively younger age group. Previously, Mazières et al. [8] obtained comparable epidemiological findings, including a median age of 60 years, a high propor
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In the previous study concerning HO mediated
2021-09-09

In the previous study concerning HO-1-mediated inhibtion of HCV replication, the mechanism underlying IFN-α/β indcuction by HO-1 involved in HO-1-catalyzed heme metabolic product, biliverdin (Zhu et al., 2010; Lehmann et al., 2010). However, in the present study SnPP, an inhibitor of HO-1 enzymatic
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On the basis of the structure of
2021-09-08

On the basis of the structure of the Rab35/ACAP2 complex, the authors identified Thr76 in switch II of Rab35 as one key specificity determinant (Lin et al., 2019). The crystal structure shows that the hydroxyl group of Thr76 forms a p38 mapk with Asp756 in ACAP2, while the methyl group is a part of
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While the S site has been implicated
2021-09-08

While the S2 site has been implicated in binding, it ML133 HCl is unclear whether the S2 site plays a role in the substrate transport process. Crystal structures have revealed that different drugs and detergents can bind to the S2 site of SERT [8] and LeuT [[13], [14], [15]]. However, there are no
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In contrast to short term
2021-09-08

In contrast to short-term effects, long-term exposure of beta cells to FFAs impairs insulin secretion and triggers apoptosis [13]. The deleterious effects of FFAs have been linked to altered glucose/fatty JTP-74057 australia oxidation cycle [13], decreased NADPH content [14], endoplasmic reticulum
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Pyrogallol is an organic gallic acid converting compound tha
2021-09-08

Pyrogallol is an organic gallic acid-converting compound that has three hydroxyl groups and belongs to the phenol family. Gallic 28170 is obtainable from the galls and barks of various trees, and a simple heating procedure can induce the decarboxylation of gallic acid to produce pyrogallol (alias:
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In order to discover novel small molecule compounds
2021-09-08

In order to discover novel small-molecule compounds with the activity of GLUT4 translocation, we conducted a cell-based phenotype screening in L6-GLUT4-myc myoblasts by measuring appearance of GLUT4 on the plasma membrane (GLUT4 translocation activity). Evaluation of total 183,400 compounds gave sev
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paf receptor br Results br Discussion Using a novel viral
2021-09-08

Results Discussion Using a novel viral vector for norepinephrine-targeted gene deletion, we have shown that glucocorticoid receptor paf receptor from locus coeruleus norepinephrine neurons reduces social interaction specifically in female mice. This effect is not attributable to changes in no
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The MeO CFO phen yl group was then
2021-09-08

The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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Despite the potential promise of
2021-09-08

Despite the potential promise of both of these peptides, such compounds are still susceptible to efficient renal filtration (Emmanouel et al., 1978, Holst, 1991, Deacon et al., 1996). However, numerous studies have demonstrated that fatty TC-H 106 dervatisation of related regulatory peptides result
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While CART increased circulating levels
2021-09-08

While CART increased circulating levels of GIP and GLP-1 in vivo, we were unable to detect any effect of exogenous CART on GIP and GLP-1 mRNA expression or GLP-1 secretion in vitro. There is no ready explanation for this discrepancy. The CART doses used (both in vivo and in vitro) have been shown to
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Although GLP has greater insulin
2021-09-08

Although GLP-1 has greater insulin-releasing effects at pharmacological concentrations [10], it is apparent that the higher circulating concentrations of GIP combined with more pronounced increase in secretion following feeding make GIP the major physiological incretin [7], [11]. The peptide exerts
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br Introduction As a fundamental metal dependent
2021-09-08

Introduction As a fundamental metal-dependent hydrolytic enzyme, inorganic pyrophosphatase (PPase) exhibits a specific catalytic ability, in which one molecule of inorganic pyrophosphate (PPi) can be transformed into two orthophosphate (Pi) ions [1,2]. The process of transformation is extremely e
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A biochemical characterisation of this functionally crucial
2021-09-07

A biochemical characterisation of this functionally crucial LSD1-p53 interaction is the focus of this study. Using several complementary assays [29], [30], [31], [32], we find that a well-defined segment of p53-CTD is capable of binding to LSD1 active site, thereby inhibiting the enzymatic activity
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