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Having established the structural requirements for potency
2024-11-11

Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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In considering the roles of these enzymes in normal physiolo
2024-11-11

In considering the roles of these enzymes in normal physiology, given the importance of GLUT4-dependent glucose uptake and glucose-dependent fatty pfk synthesis for systemic metabolic homeostasis (Herman and Kahn, 2006, Herman et al., 2012), deletion of Acly in adipocytes results in a surprisingly
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br Conclusions A large body of evidence indicates that oxida
2024-11-11

Conclusions A large body of evidence indicates that oxidative stress is involved in the pathogenesis of NDDs. Hence, reducing oxidative stress or suppressing its downstream pathways may be beneficial for the treatment of these diseases, especially such chronic diseases as AD or glaucoma. Here we
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br Conflicts of interest br Introduction Arginase catalyzes
2024-11-11

Conflicts of interest Introduction Arginase catalyzes the reaction in which l-arginine is converted to l-ornithine and urea. In humans, two arginase isoenzymes have been identified, arginase 1 and arginase 2, that differ in cellular location and tissue distribution [1]. Both arginase enzymes a
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Benzoquinonium dibromide synthesis In our previous report sa
2024-11-11

In our previous report, salivary arginase levels were found to be higher in periodontitis patients compared to healthy controls (Ozmeriç, Elgün, & Uraz, 2000). However, only one study has investigated arginase ezyme in saliva in patients with dental implants in which smokers were also included. An i
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br Results and discussion The soil fungus PSU RSPG BCC
2024-11-11

Results and discussion The soil fungus PSU-RSPG37 (BCC56870) was isolated from soil samples collected from Rajjaprabha Dam, Suratthani Province, Thailand. The fungus was deposited at BIOTEC Culture Collection, National Center for Genetic Engineering and Biotechnology (BIOTEC), Thailand Science Pa
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Nanoparticles are submicrometric systems smaller than nm whi
2024-11-11

Nanoparticles are submicrometric systems smaller than 1000 nm which high surface area and composite materials may allow their greater interaction with biological membranes and control of the drug release. These features are directly associated with the efficacy of treatment and the presence of adver
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br HIF Blockade in AA
2024-11-11

HIF-α Blockade in AA Therapy In lieu of the evidence supporting a central role for HIF-α signaling in tumor angiogenesis and CC pathobiology, significant efforts have focused on the discovery of small-molecule HIF-α inhibitors (for exhaustive compendia, see [28,44,45]). In brief, inhibitors vary
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On the contrary Birrel and colleagues observed divergent pro
2024-11-11

On the contrary, Birrel and colleagues observed divergent proliferative responses to androgens in different BC cell lines: DHT and mibolerone were found to inhibit the T47-D and ZR-75-1 324 4 receptor growth, while the proliferation of MCF-7 cells was increased by both the androgens [53]. It is wor
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The first and the best characterized mechanism of receptor
2024-11-11

The first and the best-characterized mechanism of receptor-dependent internalization of Aβ is mediated via the α7-nicotinic cetrimonium bromide receptor [82]. Lipoprotein receptor protein represents the second best-studied route that facilitates the uptake of Aβ by neurons, involving additional mol
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prostaglandin e2 Through an extensive SAR optimization campa
2024-11-11

Through an extensive SAR optimization campaign with the 4-((2-hydroxy-3-methoxybenzyl)amino)-benzenesulfonamide-based scaffold researchers have developed ML355 ((N-benzo[d]thiazol-2-yl)-4((2-hydroxy-3 methoxybenzyl)amino)benzenesulfonamide) [5]. ML355 is a nonreductive, noncompetitive, reversible 12
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AKT has been shown to be
2024-11-11

AKT1 has been shown to be important for G1-S checkpoint transition and proliferation, whereas AKT2 regulates cell-cycle exit through its interaction with p21 (Héron-Milhavet et al., 2006). In a recent study in triple negative breast cancer, AKT3, rather than AKT1 activity was most important for cell
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Mass spectrometry MS analysis and selective enrichment metho
2024-11-09

Mass spectrometry (MS) analysis and selective enrichment methods of phosphorylated proteins are powerful tools that can help address these challenges. Recent advances in MS have made it possible to analyze signaling pathways by facilitating high-throughput identification of phosphorylation sites wit
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br A Rs which were cloned and then pharmacologically identif
2024-11-09

A3Rs, which were cloned and then pharmacologically identified in the early 1990s, are expressed in multiple organs and peripheral tissues including NSC 74859 involved in inflammatory responses (Gessi et al., 2008, Borea et al., 2014). While low levels are expressed in the CNS, A3R agonists produc
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Earlier studies revealed an interaction between HSP and ACK
2024-11-09

Earlier studies revealed an interaction between HSP90β and ACK1 [15]. In the proteomic approach, we show that ACK1 associates with HSP90α and HSP90β. Additionally, we confirm the existence of a HSP90-ACK1 complex with co-IP experiments. We further analysed whether an inhibition of HSP90 affected the
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