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To our knowledge BAY has
2023-07-24
To our knowledge, BAY 60-6583 has not progressed to clinical development and remains to be the only ADORA2B agonist that has been developed.33, 34 Further development of similar compounds would be beneficial in future fibrosis research. One of the limitations of our study is being limited to in vit
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The potential use of derivatives
2023-07-24
The potential use of derivatives belonging to this series as therapeutic agents mostly depends on their pharmacokinetics and pharmacodynamics. The pharmacokinetic phase includes absorption, distribution, metabolism and excretion (ADME) of the studied compounds. Therefore, preliminary data for theore
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br Introduction Adenosine deaminase ADA also known as adenos
2023-07-24
Introduction Adenosine deaminase (ADA), also known as adenosine aminohydrolase, is a key enzyme involved in the purine metabolism that converts adenosine to inosine irreversibly (Lupidi et al., 1997). It is a zinc containing metalloenzyme present in both prokaryotes and eukaryotes. In humans ADA
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On the basis of the above information
2023-07-24
On the basis of the above information, we designed a new series of benzothiazole–piperazine derivatives (–) that have the aforementioned structural requirements (). Benzothiazole is an important ring system in the drug discovery studies of AD. There are several benzothiazole compounds that show pote
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Halopemide The AChR is composed of five
2023-07-24
The AChR is composed of five homologous, membrane-spanning subunits. AChRs containing two α, one β, one δ and one γ subunit (AChRγ) predominate during embryonic development and mice lacking AChRγ die at birth (Takahashi et al., 2002). After birth, the AChRγs are replaced during the first 2 postnatal
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Most studies on d penicillamine
2023-07-24
Most studies on d-penicillamine-induced MG were performed before the discovery that some MG patients have anti-MuSK antibodies. After the identification of the present case, we retrospectively tested the stored frozen sera of ten earlier identified d-penicillamine MG patients with anti-AChR Phosphor
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Furthermore our lab previously reported that cadmium treatme
2023-07-24
Furthermore, our lab previously reported that cadmium treatment increased AChE-S and decreased AChE-R variants gene expression, which mediates the cell death observed on basal forebrain cholinergic neurons (Del Pino et al., 2016b). AChE-R decreased expression, which presents a neuroprotective role i
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A variety of quinazoline or fused
2023-07-21
A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and
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Nivolumab Drug resistance development often involves structu
2023-07-21
Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 Nivolumab are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream activator of ERK1/2, associated
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br Methods br Results br Discussion Autotaxin
2023-07-21
Methods Results Discussion Autotaxin has been shown to have effects on major cell types implicated in OA, notably chondrocytes, osteoblasts, osteoclasts, and synoviocytes, through its enzymatic product LPA [20]. However, a paucity of research exists on the involvement of autotaxin in OA. Fi
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Based on these findings the
2023-07-21
Based on these findings, the time point for manipulating autophagy may also determine its role, whereby autophagy induction performed before ischemia could play a protective role but have an opposite effect once ischemia/reperfusion has occurred. This hypothesis is further supported by the protectiv
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MLN another selective Aurora A inhibitor is
2023-07-21
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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FPS-ZM1 TLX may promote survival and prevent apoptosis
2023-07-21
TLX may promote survival and prevent apoptosis in NB FPS-ZM1 [12]. Here, we ask whether the survival-promoting effects of TLX are mediated by Apoptosis Signal-regulating Kinase-1 (ASK1, MAP3K5). ASK1 is a member of the Mitogen-Activated Protein (MAP) kinase family and it preferentially activates th
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br Abbreviations br Acknowledgements This work was
2023-07-21
Abbreviations Acknowledgements This work was supported by grants from the National Institutes of Health (R01GM114168) and the Office of Naval Research (N000141210773) awarded to J.C·H and National Cancer Institute (5P30CA16059) Cancer Center Support Grant in support of Massey Cancer Center Pro
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br Implications for cancer ROS have
2023-07-21
Implications for cancer ROS have a long history of being involved in the development and progression of cancer and increased ROS level is considered as a hallmark of many tumors [76], [77]. Initially, it was thought that ROS would serve as chemical mutagens that would indiscriminately damage cell
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