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Interestingly hypoxia and an enhanced Warburg effect
2023-10-01
Interestingly, hypoxia and an enhanced Warburg effect ultimately lead to increased lactate production. The accumulation of lactate results in an acidic tumor microenvironment, which induces local inflammation. Lactate also promotes the polarization of macrophages that express immunosuppressive argin
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A high throughput screening campaign led to the
2023-09-28
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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overseas Many coumarin derivatives can be found in
2023-09-28
Many coumarin derivatives can be found in nature. There are more than 1300 types of those purely derived from plants, and if synthetic products are included, their number is immeasurable. According to the earliest existing records extant, herbs containing Psoralen-type compounds, e.g., methoxsalen,
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abnormal lipid metabolism Fig shows a possible scheme of the
2023-09-28
Fig. 8 shows a possible scheme of the generation of AP(+)-exosomes based on this study. In response to inflammatory stimuli, ERAP1 is secreted from ER into the extracellular milieu through the conventional secretion pathway. On the other hand, exosomes are derived from the endosomal pathway, and are
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br Concluding Remarks The effects of point
2023-09-28
Concluding Remarks The effects of point mutations of the four ARs on ligand binding affinities, functional potencies, and efficacies constitute a valuable source of pharmacological information. We analyzed the existing data and mapped it on the collection of available AR crystal structures, allow
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br Conclusions The present data
2023-09-28
Conclusions The present data suggest that homeostatic balance of the cortical/hippocampal adenosinergic tone is necessary for normal working memory function and any deviation appears to impair performance – either as a consequence of A2AR under-activation when adenosine levels are reduced or due
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It is well accepted that PKA is a key enzyme
2023-09-28
It is well accepted that PKA is a key enzyme activated at the beginning of the capacitation process [69]. As mentioned above phosphorylation/inactivation of cofilin in sperm is a PKA dependent process [58]. We could not see any change in cofilin phosphorylation level by adding the PKA activator 8Br-
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On the basis of the
2023-09-28
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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In summary we could identify
2023-09-28
In summary, we could identify and experimentally confirm two novel SBEs within the 5-LO promoter and we were able to demonstrate that TGFβ and SMADs stimulate 5-LO promoter activity. Moreover, an elevated 5-LO expression has been linked to different forms of leukaemia. Therefore, the influence of ML
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The c C T mutation identified in
2023-09-27
The c.286C>T mutation identified in subject K20-1 was also reported in other ethnic groups, including Brazilian, French-Canadian, Italian, and Arabs from the United Arab Emirates [20], [21], [22], whereas c.318A>G mutation in subjects K10-1 was previously reported in Asian and Caucasians [13], [23],
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Moreover our present work suggests that AXL could
2023-09-27
Moreover, our present work suggests that AXL could be a modulator of sunitinib response, at least for cell lines that present high endogenous levels of this RTK activation, since we observed an increased responsiveness to sunitinib in Nivolumab activated with AXL receptor ligand. A role for AXL in
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What can we learn about
2023-09-27
What can we learn about the anticancer therapeutic efficacy of Aurora kinase inhibitors from our experience with the Bcr-Abl inhibitors and the long term clinical consequence of their use in treating leukemias? As discussed, all Aurora kinase inhibitors developed to date are ATP-competitive inhibito
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br Results br Discussion The A nidulans Aurora kinase displa
2023-09-27
Results Discussion The A. nidulans Aurora kinase displays diverse locations during mitosis and we show here that it also locates to hyphal regions where septa subsequently form, to the septal pore region of newly formed septa and displays a depends on specific location to mature septa. To inv
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Fig summarizes the oxidative metabolism
2023-09-27
Fig. 1 summarizes the oxidative metabolism of arachidonic cfse by lipoxygenases cyclooxygenases and cytochrome P450. Lipoxygenases in humans are expressed in a tissue-specific fashion: 5-LOX is mainly expressed in leukocytes, 12-LOX in platelets, and 15-LOX-1 in reticulocytes, eosinophils, and mac
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The allosteric site of class
2023-09-27
The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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