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Whether similar mechanisms play a role in adiponectin signal
2024-03-20
Whether similar mechanisms play a role in adiponectin signal transduction and whether additional proteins are recruited to adiponectin receptors via APPL1 has not been analysed so far. Although it has been clearly established that APPL1 is a downstream adaptor protein in adiponectin signal transduct
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Since pyrrolopyrimidine dithiolanes and both displayed parti
2024-03-20
Since pyrrolopyrimidine dithiolanes and both displayed particularly excellent levels of ACK1 inhibition, these analogs were viewed as potential candidates for further investigation in tumor xenograft experiments. While in vitro metabolic studies indicated that pyrrolidine was predicted to be sign
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Our initial approach to identify
2024-03-20
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI calcium sensing receptor library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein fl
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The ATX LPA signaling axis has been implicated
2024-03-18
The ATX–LPA signaling “axis” [5] has been implicated in a perplexing variety of physiological and pathophysiological processes, including vascular and neural development [5], [26], [27], [28], [29], tumor progression and metastasis [30], [31], lymphocyte trafficking [22], bone development [32], neur
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A third motif involves the toggle switch and consists
2024-03-18
A third motif involves the toggle switch and consists of the conserved FxxCWxP sequence in TM6 of class A GPCRs (Hofmann et al., 2009, Rosenbaum et al., 2009). Rotamerization of Trp in combination with a kink caused by Pro facilitates the outward movement of TM6 upon activation (Hofmann et al., 2009
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br Regulatory mechanisms of ASK activity br
2024-03-18
Regulatory mechanisms of ASK1 activity The functions of ASK1 in disease ASK1 inhibitor As mentioned above, ASK1 plays a pivotal role in the pathogenesis of various diseases; hence, an ASK1 inhibitor has therapeutic potential. Although inhibitors of the ASK1 downstream kinases p38 and JNK ar
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Despite these conflicting data about COX ER
2024-03-18
Despite these conflicting data about COX-2/ER correlations, a large body of evidence supports that elevated COX-2 expression in breast cancer is a constant feature of high stage disease and a predictor of worse outcome. Upregulation of COX-2 protein has been identified in approximately 40% of cases
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br Introduction Natural antioxidants in vegetables have gain
2024-03-18
Introduction Natural antioxidants, in vegetables, have gained the attention of both researchers and consumers. Vegetable amaranth (Amaranthus tricolor) is a good source of minerals, vitamins, phenolics, and carotenoids; it also contains betalains, a nitrogen containing group of natural pigments,
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F is an orotomide a novel
2024-03-18
F901318 is an orotomide, a novel class of antifungals, which inhibits pyridine biosynthesis by blocking dihydroorotate dehydrogenase (URA1) activity [137]. Although this pathway is conserved in humans, human URA1 is only 20% identical to its fungal homolog and it is inhibited 2000-fold less effectiv
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Another possible scenario is that the same pathologic proces
2024-03-18
Another possible scenario is that the same pathologic process has different effects in different people. It might be that the pathway outlined in Fig. 6A is operative in some individuals, but other individuals have a factor Q (which could be genetic or environmental) that blocks the effect of A on T
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Globally the total number of
2024-03-18
Globally, the total number of patients included in the meta-analysis was 1885, ranging from 40 to 442 patients per study. All eligible studies reported the association between ALDH1 expression and patients' OS [24-26, 3241], whereas nine studies evaluated the relationship between ALDH1 expression an
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The macrophage is the major cell type responsible for
2024-03-18
The macrophage is the major cell type responsible for cholesterol uptake and metabolism associated with the initiation and progression of atherosclerosis in focal areas of the arterial subendothelial space. In advanced atherosclerotic lesions of cardiovascular disease, cholesterol-induced macrophage
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br A Rs which were cloned and then pharmacologically identif
2024-03-18
A3Rs, which were cloned and then pharmacologically identified in the early 1990s, are expressed in multiple organs and peripheral tissues including Torcetrapib involved in inflammatory responses (Gessi et al., 2008, Borea et al., 2014). While low levels are expressed in the CNS, A3R agonists produ
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Metformin s pluripotent roles are alluded to
2024-03-16
Metformin's pluripotent roles are alluded to in terms of its antitumorigenic, glucose-lowering, and cardioprotective effects, which are due in part to its upregulation of AMPK activity [39,40]. Metformin's glucose-lowering effect is a result of reduced hepatic gluconeogenesis, whereas improved insul
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Oxidative stress has recently been reported
2024-03-16
Oxidative stress has recently been reported as one of the important mechanisms of toxic effect of Cd2+[43]. The mechanism of Cd2+-induced oxidative stress involves an imbalance between generation and removal of ROS in tissues and cellular components, causing damage to membranes, DNA, and proteins [4
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