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In this report the natural compound deguelin potently
2024-08-07

In this report, the natural compound deguelin potently and dose-dependently suppressed Aurora B kinase activity in vitro, indicating that this compound is an effective Aurora B inhibitor. The docking study indicated that deguelin was docked into the ATP-binding pocket of Aurora B and formed hydropho
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br Introduction The process of mitosis is highly complex and
2024-08-07

Introduction The process of mitosis is highly complex and tightly regulated. This phase of the PF-431396 resulted in two identical daughter cells. The aurora kinases (aurora A, B, and C) are a family of three highly homologous serine-threonine protein kinases that play a key role in regulating th
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Lower LDL C mediated by variants in
2024-08-07

Lower LDL-C mediated by variants in the ACL gene is causally associated with the risk of cardiovascular events. Because, genetic variants that mimic the effect of an ACL inhibitor have the same effect on the risk of cardiovascular events per unit change in LDL-C as variants that mimic the effect of
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br Ataxia telangiectasia and Rad related as a
2024-08-07

Ataxia–telangiectasia and Rad3 related as a therapeutic target Several concerns revolving around functional inhibition of ATR have hindered the exploitation of ATR as therapeutic target in cancer therapy and delayed the development of specific ATR kinase inhibitors. It was anticipated that pharma
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Further important evidence for G protein signaling on early
2024-08-07

Further important evidence for G protein signaling on early endosomes has been subsequently obtained for the β2-adrenegic receptor using fluorescently-tagged conformation-sensitive nanobodies selectively recognizing the active receptor and Gs protein [43]. More recently, our group used a combinatio
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Autophagy and apoptosis have a very
2024-08-06

Autophagy and apoptosis have a very complex relationship, and the precise mechanism remains to be determined. At present, a large amount of research has confirmed that autophagy can protect the cell from apoptosis in special conditions such as nutrient deficiency or growth factors deprivation; the e
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br Materials and methods br Results br Discussion In this
2024-08-06

Materials and methods Results Discussion In this study, the orphan receptor GPR25 was cloned from several representative vertebrate species including zebrafish. Although the overall amino UNC0638 sequence identity among these species is not high (38–52%), our synteny analysis clearly indica
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Complementing the effects of ARB
2024-08-06

Complementing the effects of ARB and ACEI on HDL capacity to elicit cholesterol efflux, HDL of ARB- and ACEI-treated groups significantly lessened macrophage production of superoxide (Fig 2). As with efflux, there was no difference in this effect between the ARB and ACEI groups. These data are inter
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parp apoptosis pathway br Conflict of interest statement br
2024-08-06

Conflict of interest statement Introduction Tanshinone IIA (Tan IIA) is a major active component of Salvia miltiorrhiza (S. miltiorrhiza), a well-known Chinese traditional medicine that is used for the treatment of cardiovascular and cerebrovascular diseases [1]. Tan IIA exhibits diverse pharm
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In conclusion we show that HBP is
2024-08-06

In conclusion, we show that HBP1 is phosphorylated on three sites, which control HBP1 transcriptional activity and glioblastoma cell proliferation. This phosphorylation largely depends on AKT, although other kinases may also be involved. In a previous study, we had shown that the PI3K-AKT pathway re
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In the previous study we demonstrated the
2024-08-06

In the previous study, we demonstrated the importance of the mPFC postsynaptic 5-HT1A receptor in the sustained antidepressant effects, because a sustained antidepressant effect was obtained with intra-mPFC injection, but not systemic injection of 8-OH-DPAT, a 5-HT1A receptor agonist (Fukumoto et al
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CHK has been reported to be
2024-08-05

CHK1 has been reported to be the kinase responsible for H3.3S31 phosphorylation in human ALT cancer 9508 . However, in our study, knockdown of CHK1 in HEK293F (Figs. S1c and S6) or HeLa S3 (data not shown) cells did not result in a significant decrease in H3.3S31ph, which is in agreement with an ea
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Earlier studies showed that exposure of cells
2024-08-05

Earlier studies showed that exposure of cells to IR caused ATM-dependent phosphorylation of 53BP1, as judged by electrophoretic mobility shift [24], [25], [26]. To date, the only known in vivo 53BP1 phosphorylation site(s) are Ser25 and possibly Ser29 [27]. In the course of our studies, we noticed t
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A high throughput screening campaign led to the
2024-08-05

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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As aforementioned this study aimed
2024-08-05

As aforementioned, this study aimed to design, synthesize and investigate aromatase inhibitory and anti-breast cancer activities of N,N′-disubstituted thiourea derivatives. Based on the attractive phenotypic molecule 1, the synthetic N,N′-disubstituted thioureas have been designed including monothio
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