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Imatinib was first approved for
2024-09-29
Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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In our previous study we found that
2024-09-29
In our previous study we found that the total activity of aldehyde dehydrogenase in cancer HQNO of RCC is at the same level as in normal renal tissue [10]. These findings are similar to our results in serum patients with renal cancer. There is no significant difference between ALDH activity in seru
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WM-2474 Introduction Mammalian cells express the
2024-09-29
Introduction Mammalian WM-2474 express the seven STAT family members STAT1, −2, −3, −4, −5A, −5B, and −6 [1], [2]. All STATs exert physiologically important roles as homo- and heterodimers [2], [3], [4]. Cytokines and growth factors activate STATs through the activation of kinases that phosphorylat
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The first rationally designed dual mPGES
2024-09-29
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic bioactive mg - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synth
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In an effort to determine if one ARI was
2024-09-29
In an effort to determine if one 5ARI was more effective than the other, the Enlarged Prostate International Comparator Study (EPICS) [17] compared treatment with finasteride and dutasteride in 1630 men over the age of 50 and concluded that after one year of treatment, both groups had statistically
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The benzimidazole group seems to be a key
2024-09-29
The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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Moreover showed reduction in fibroblast growth
2024-09-29
Moreover, showed 73% reduction in fibroblast growth factor–induced neovascularization in a mouse corneal micropocket assay at a dose of 100mg/kg and 50% reduction at 50mg/kg. Both results were highly statistically significant (PMilrinone synthesis have recently shown only moderate efficacy (40% inhi
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Matthew et al synthesized and carried
2024-09-28
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that AG-126 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pHH3), EC50
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Hypoxia induced replication arrest has
2024-09-28
Hypoxia-induced replication arrest has been demonstrated in a variety of organisms in addition to mammals; including Zebrafish , , and (brine shrimp) which have been shown to survive for 4 years and longer in anoxic conditions . Despite this breadth of study, little is known about the mechanism of h
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Why do glutamate and glycine bind
2024-09-28
Why do glutamate and glycine bind to the endothelin receptor antagonist in such different ways? Given the overall structural similarity between the GluN2A and GluN1 LBDs, one might conclude that the LBDs also bind ligands via similar processes. NMDA receptors with engineered disulfide linkages that
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Findings of the present study provide a molecular
2024-09-28
Findings of the present study provide a molecular mechanism for the elevated ASK1 expression in obesity and how it may be functionally linked to whole-body insulin resistance. The role our findings assign to increased E2F1 in upregulating ASK1 parallels the capacity of this transcription factor to r
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br Antioxidant polymers conjugates Natural antioxidants are
2024-09-28
Antioxidant-polymers conjugates Natural antioxidants are usually used as a substitute for synthetics but some degradation phenomena could influence their applications. For example, ascorbic T7 High Yield RNA Synthesis as a natural antioxidant undergoes yellowish coloration as a result of oxidati
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However from our meta analysis
2024-09-28
However, from our meta-analysis emerge some strategic considerations for the continued use of antiangiogenic drugs for glioblastoma patients: Conflict of interest Funding Introduction Angiogenesis is a physiological process involving the formation of new blood vessels from pre-existing blo
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Prostate cell growth and prostate carcinogenesis are not onl
2024-09-28
Prostate cell growth and prostate carcinogenesis are not only mediated by androgens, they are also dependent on functional insulin receptor (IR) and insulin-like growth factor-1 (IGF-1) receptor (IGF1R) signaling. Previous studies addressed this issue and reported a correlation between high insulin
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Another issue is that the
2024-09-28
Another issue is that the vast majority of data from PET and CSF are from selected participants recruited through tertiary care dementia centers [176]. It is widely recognized that clinic-based participants differ from community-based studies, for example, the amount, type, and distribution of neuro
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