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To improve the preferential GalR binding
2022-04-07
To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollenb
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LXRs are physiological regulators of cholesterol
2022-04-07
LXRs are physiological regulators of cholesterol and lipid metabolism and influence glucose metabolism. In addition, they have been shown to repress transcription of certain pro-inflammatory genes (Jakobsson et al., 2012; Ogawa et al., 2005; Terasaka et al., 2005). Thus, LXRs can either activate or
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During the course of our optimization of the diarylsulfonami
2022-04-07
During the course of our optimization of the diarylsulfonamide chemotype as FFA4 agonists, we identified xanthene as a potent and selective antagonist of FFA4 (). Xanthene was able to block the agonist induced intracellular Ca response elicited by both linoleic 5-moUTP and compound in competition st
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br Material and methods br Results
2022-04-07
Material and methods Results Discussion In the present study, we attempted to unravel the mechanism underlying the statin-mediated inhibition of FGFR3 signaling in chondrocytes, reported earlier by Yamashita and colleagues. We evaluated the role of statins in four different experimental sys
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Till date the first line treatment
2022-04-07
Till date, the first line treatment of T2DM is oral metformin followed by oral sulfonylureas, dipeptidyl peptidase-IV-inhibitors, and TZDs. As the disease progresses, injectable glucagon-like peptide-I analogues or ultimately insulin become necessary to maintain glycaemic control. Despite the establ
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ci-1033 br Nanoscale Cortical Actin Remodeling in Regulated
2022-04-07
Nanoscale Cortical Actin Remodeling in Regulated Exocytosis The network of cortical ci-1033 is formed by numerous fine actin filaments, which are only about 10nm in diameter [52]. Although the microscale role of the cortical actin network in vesicle exocytosis is well established, the function of
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bupropion hydrochloride The initial hyperproliferation phase
2022-04-07
The initial hyperproliferation phase during crypt regeneration is reminiscent of the effects of Apc loss during tumour initiation and genetic studies show Yap and Taz are also required for adenoma formation in mice [10••, 12•, 13]. Furthermore, Yap activation by Mst1/2 or Sav deletion increases cry
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br Materials and methods br Results Heterologous expression
2022-04-07
Materials and methods Results Heterologous expression of P. locustae Hxk in methylotrophic yeast P. pastoris was not accompanied by nuclear localization of parasite protein (Fig. 1). The addition of leptomycin B, a specific inhibitor of nuclear export in fission yeast Schizosaccharomyces pombe
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V5 Epitope br Resistance to targeted therapy The idea of
2022-04-07
Resistance to targeted therapy The idea of treating HER2 mutant tumors with specific therapies is relatively new and, as a consequence, little is known about the potential mechanisms of resistance to anti-HER2 agents in this setting. Primary resistance may be mediated by the presence of on-target
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br Parkinson disease Idiopathic PD
2022-04-07
Parkinson disease Idiopathic PD is a hypodopaminergic movement disorder of uncertain etiology that affects 3% of persons over age 65 (Dexter and Jenner, 2013). Cardinal signs of this common neurodegenerative condition include bradykinesia, rigidity, rest tremor and postural instability. Autonomic
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br Mechanism of HH pathway activation in NSCLC Despite
2022-04-07
Mechanism of HH pathway activation in NSCLC Despite the role of the HH pathway in basal cell carcinoma and medulloblastoma, it has been postulated that epithelial tumors do not demonstrate cell autonomous HH ligand activity. The main evidence comes from the study by Yauch et al showing no correla
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Introduction Cancer has been a significant public health
2022-04-07
Introduction Cancer has been a significant public health problem in the world with more patients being diagnosed every year. However, chemotherapy from non-specific cytotoxic agents that as an effective means of cancer treatment is limited by severe side effects and poor selectivity. Thus, the deve
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br Conclusion The addition of cellulose to natural substrate
2022-04-07
Conclusion The addition of AY 9944 dihydrochloride to natural substrate increases the number of H-bonds which indicates an increase in the stability of the docking systems. The investigated compounds are more stable than natural substrate in docking systems, where the natural substrate has two H
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Substrate affinity and specificity can be enhanced by dockin
2022-04-07
Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of perifosine receptor bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognitio
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A number of in vivo studies
2022-04-06
A number of in vivo studies have investigated the antitumor activity of distinct GSK-3 inhibitors in a variety of cancer cell line-derived tumor xenograft models [14], [21], [22], [24], [33], [39], [40]. These studies utilized toolkit GSK-3 inhibitors as monotherapies. Although inhibition of tumor g
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