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In the late s Solvay
2023-08-16
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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adenylate cyclase Targeting the BCR is the
2023-08-16
Targeting the BCR is the ideal strategy to identify the antigen reactive B cells. However, there is concern that B cells could be activated when BCR are bound and cross-linked by antigens, a possibility that is obviously negative for the treatment of autoimmune disease. Proby et al. (2000) tried to
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In summary this study reveals that the stability
2023-08-16
In summary, this study reveals that the stability of rapsyn is critically dependent on HSP90β, highlighting a novel function of HSP90β in NMJ formation and maintenance. It also identifies a mechanism in agrin signaling for AChR clustering, i.e., by upregulating the interaction between HSP90β and rap
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The purpose of the present study
2023-08-16
The purpose of the present study is (1) to characterize AChE from the monogonont B. koreanus and to analyze the modulation of the AChE activity and its transcription level after exposure to six pharmaceuticals, (2) to evaluate the usefulness of AChE as a molecular biomarker upon pharmaceutical expos
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Several tertiary prevention studies are currently underway e
2023-08-16
Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Dut
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The extent to which GPCR oligomerization
2023-08-16
The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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Optimization of the B ring
2023-08-16
Optimization of the B-ring specifically targeted preventing the oxidation of the ring system (). As described above, the 4-position of the phenyl ring provides the appropriate vector towards bulk solvent. - and -linked substitutions at the 4-position of the B-ring from the 4-fluoro-nitrophenyl inter
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RWJ 56110 Because the V ATPase inhibitors that have been emp
2023-08-16
Because the V-ATPase inhibitors that have been employed in these studies (including bafilomycin and concanamycin), are membrane permeant, they inhibit all the V-ATPases in the cell. This is important since it is possible that intracellular V-ATPases, in addition to those present at the plasma membra
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Sennoside D synthesis It was previously demonstrated that
2023-08-16
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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An alternative more rarely used
2023-08-16
An alternative, more rarely used, electron microscopy-based approach exploits labeling of phagosomes with DAMP (3-(2,4-dinitroanilino)-30-amino-N-methyldipropylamine). DAMP is a weakly basic compound which is membrane-impermeable once it has been protonated. This way, DAMPH+ accumulates in acidic in
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br Results br Discussion br
2023-08-15
Results Discussion STAR★Methods Author Contributions Acknowledgments We thank Angela Walker for assistance with the manuscript; Junlin Liu, Xiangxiang Gu, Na Chen, Lu Xue, and the BV Core Facility of iHuman Institute for their support; scientists and colleagues at Amgen Inc., Zhulun W
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Therefore we have further investigated the anti oxidant acti
2023-08-15
Therefore, we have further investigated the anti-oxidant activity of isogarcinol in vitro by measuring the scavenging of 2,2′-diphenyl-1-1picrylhydrazyl (DPPH) and 2,2′-azino-bia (3-ethylben-zothiazoline-6-sulphonicacid) (ABTS), and determining its reducing power and ability to prevent lipid peroxid
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Critically we found that pre
2023-08-15
Critically we found that pre-treatment with Aβ monomer preparations prevented the Aβ oligomer-induced aggregation of PrPC. These preparations contain a mixture of Aβ species and consequently it was not possible to identify the precise form of Aβ that is responsible for this effect. It is possible th
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Another issue is that the vast
2023-08-15
Another issue is that the vast majority of data from PET and CSF are from selected participants recruited through tertiary care dementia centers [176]. It is widely recognized that clinic-based participants differ from community-based studies, for example, the amount, type, and distribution of neuro
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Mass spectrometry MS analysis and selective enrichment metho
2023-08-15
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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