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br Conclusion To conclude it would be fair
2022-11-04
Conclusion To conclude, it would be fair to say that the research efforts on FLAP inhibitors for intervening with LT biosynthesis have reached to a considerably advanced state during the last decade as a result of growing interest from both pharmaceutical industry and academia [4], [37], [38]. Du
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A role for YAP in
2022-11-04
A role for YAP in mediating resistance to EGFR inhibition has also been described [28], [29]. In line with these evidences, we observed increased YAP activation in all the generated EGFR TKI–resistant cells, testified by decreased phosphorylation on the inhibitory serine 127, enhanced nuclear locali
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Because of its role in tumor growth proliferation and
2022-11-04
Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t
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br Expression of autotaxin in
2022-11-04
Expression of autotaxin in cancer Autotaxin (ATX) is a member of the family of NPPs (Nucleotides pyrophosphatases phosphodiesterases (NPP) family with a unique lysophospholipase D (lysoPLD) activity, allowing the synthesis of LPA from lysophospholipid precursors such as the lysophosphatidylcholin
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Loss of expression or functional activity of
2022-11-04
Loss of expression or functional activity of cell adhesion is intricately related to advanced stages of tumour progression and invasiveness. Martin-Belmonte and Perez-Moreno recently mentioned that the deregulation of adhesion can alter tumourgenesis in the early stage. We have shown for the first t
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Folinic acid In addition to drawing attention to
2022-11-04
In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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The main function of ATR CHK
2022-11-04
The main function of ATR/CHK1 signaling is activating TC-I 15 checkpoint arrest for S and G2 phases in mammalian cells. There are three checkpoints in response to DNA damage: G1/S, G2/M, and S-phase. The G2/M checkpoint can prevent cells that incur DNA damage in G2 phase or progress into G2 phase fr
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Several structural classes of ASK inhibitors mostly
2022-11-04
Several structural GDC-0941 of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilead revea
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Y-27632 The Nagoya Heart Study enrolled
2022-11-03
The Nagoya Heart Study enrolled patients with hypertension and type 2 diabetes or impaired Y-27632 tolerance (12). Patients were randomized to valsartan- or amlodipine-based regimens with a BP target of ≤130/80 mmHg. The primary outcome was a composite of sudden cardiac death, myocardial infarction
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2-Cl-IB-MECA Akt is another upstream kinase known to phospho
2022-11-03
Akt is another upstream kinase known to phosphorylate AMPK Ser489 in response to high insulin levels [7], [21]. HepG2 2-Cl-IB-MECA show an increase in phosphorylation of AMPK at Ser485 when incubated with either insulin or troglitazone individually (Fig. 5A and C). Despite this concurrent increase,
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br Serine glycine and one
2022-11-03
Serine/glycine and one-carbon metabolism Altered serine metabolism in tumors was noted nearly half a century ago, and elevated flux through the de novo serine synthesis pathway (SSP) is a common phenomenon in cancer ruthenium red [43]. The SSP branches from glycolysis at the point of 3-phosphogl
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A large number of aldose reductase inhibitors have been
2022-11-03
A large number of aldose reductase inhibitors have been prepared synthetically, and a limited number of them are therapeutically used. However, none of them is satisfactory. Here, Cannabis extracts with high content of non-psychotropic phytocannabinoids CBD/CBDA or CBG/CBGA showed statistically sign
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br The AHR functions in the immune system
2022-11-03
The AHR functions in the immune system – a tsunami of exciting findings The research of recent years has convincingly established an important function of the AHR in linking chemical environmental cues to immune responses [21,22], and reviewed in [1,23]. As a side effect, a view of the AHR as “Th
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Implicit in this concept is the
2022-11-03
Implicit in this concept is the idea that the β-adrenoceptors in the detrusor would be activated by adrenergic nerves of the sympathetic system: sympathetic activity promoting relaxation and enhancing bladder capacity. However, it has been demonstrated that there is only a sparse adrenergic innervat
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Renal cell carcinoma RCC accounts for more
2022-11-03
Renal cell carcinoma (RCC) accounts for more than 12,000 cancer deaths in the United States (Jemal et al., 2003). The current treatment includes surgical resection followed by interleukin-2 or Interferon-α treatment. Some patients experience distant metastatic lesions of RCC. In the last 5 years, re
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