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VS strategies have been building momentum
2021-11-26
VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com
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The regulatory effects of NADPH oxidase on ferroptosis might
2021-11-26
The regulatory effects of NADPH oxidase on ferroptosis might also relate to neuroinflammation. Although ferroptosis can trigger inflammatory responses in the brain, neuroinflammation, in turn, can also modify ferroptosis. It has been reported that inflammatory conditions such as those found in neuro
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In this study we followed the fate of Ag
2021-11-26
In this study, we followed the fate of Ag-specific CD8+ T vegfr inhibitor by directly visualizing them using MHC class I tetramers coupled with ovoalubumin (OVA)257–264 following EG.7 inoculation. We also examined the mechanism of apoptosis in exhausted Ag-specific CD8+ T cells during tumor immune
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Following the discovery of diketo compounds S and
2021-11-26
Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent PHA-665752 sale based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase.
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Although epigenetic mechanisms are implicated in the pathoge
2021-11-26
Although epigenetic mechanisms are implicated in the pathogenesis of hematopoietic malignancies, little is known about the role of lysine-specific histone demethylases and whether manipulation of these enzymes can be translated into targeted therapies. KDM6A is the most frequently mutated histone de
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br Conclusion Our data allow
2021-11-26
Conclusion Our data allow pharmacological discrimination of diverse of H3 reductase enzyme antagonists that can be linked to their differential efficacy in preclinical and clinical disease settings (Fig. 6). Moreover, we identify the sigma-1 receptor as a common “off target” for H3 antagonists,
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Whether histamine receptor distribution is altered in canine
2021-11-26
Whether histamine receptor distribution is altered in canine GI diseases remains unknown, but human research has documented altered histamine receptor density in certain GI diseases (Sander et al., 2006, Deiteren et al., 2015, Von Rahden et al., 2011). Additionally, a novel H4 receptor antagonist, J
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Another important outcome of reducing
2021-11-26
Another important outcome of reducing hypothalamic HIF in DIO was the increase in gliosis and hypothalamic inflammation. Both experimental and human studies have shown that hypothalamic inflammation plays an important role in obesity by inducing resistance to anorexigenic signals, such as insulin an
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Most studies of HIF have focused on its transcriptional acti
2021-11-26
Most studies of HIF-1α have focused on its transcriptional activity-dependent functions. However, our results indicate that the oxidative stress-related effects of mtHIF-1α occur independently of its translocation to the nucleus and do not require its transcriptional activity. In fact, several studi
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In addition to lifestyle factors
2021-11-26
In addition to lifestyle factors, genetic factors may also influence the efficacy of antineoplastic drugs in breast cancer patients.16, 17 The HER2 gene contains several single nucleotide polymorphisms (SNPs). Two of the most investigated HER2 SNPs are Ile655Val (rs1136201) and Ala1170Pro (rs1058808
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Initial experiments confirmed that RBC effectively
2021-11-26
Initial experiments confirmed that RBC8 effectively inhibited both RalA and RalB activation in an identical, dose-dependent manner following platelet stimulation with the GPVI-specific ligand, CRP (Fig. 1Ai). Non-specific, upper bands were observed when immunoblotting for activated RalB, with the sp
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The NF B family of transcription factors is involved in
2021-11-26
The NF-κB family of transcription factors is involved in acquisition of resistance to anticancer drugs as well as to apoptosis. NF-κB-mediated mdr1 gene upregulation is part of the anti-apoptotic protection mechanism of proximal tubule (PT) tbtu against cadmium-induced oxidative stress and apoptosi
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Compared to methadone or morphine buprenorphine is
2021-11-25
Compared to methadone or morphine, buprenorphine is a partial mu-opioid agonist, which shows high affinity for, and slow dissociation from, mu-opioid receptors. This maintenance of homeostasis may help to counter the development of an overt withdrawal syndrome, and may explain the lower risk of deve
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br Materials and methods br Results br Discussion To
2021-11-25
Materials and methods Results Discussion To fulfill its role in tissue homeostasis, repair and immunoregulation, MSCs must be able to (i) renew themselves by cell division and proliferation, (ii) migrate to its target end-site in response to chemotaxis signals and (iii) undergo appropriate
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Restless running behavior was first described
2021-11-25
‘Restless running behavior’ was first described in mice after administration of 30mg/kg i.p. ALX-5407 and was thought to be due to an augmentation of NMDA-induced dopamine activity [27]. The motor impairments caused by ALX-5407 were confirmed by Perry et al. [10] and extended to another sarcosine-de
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