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Two parallel branches of the DNA
2024-11-05

Two parallel branches of the DNA damage-dependent S-phase checkpoint are thought to co-operate by inhibiting distinct steps of DNA replication. One branch includes the phosphorylation of structural maintenance of chromosomes 1 (SMC1), a cohesin that is activated by ATM or ATR after IR treatment or r
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Since artemisinin shows low solubility and poor oral bioavai
2024-11-04

Since artemisinin shows low solubility and poor oral bioavailability [8], [9], derivatizations of artemisinin were carried out and yielded different semisynthetic antimalarial drugs such as artemether and sodium artesunate. Artemether (decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano [4.3-
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Thiazole heterocycles constitute an interesting class
2024-11-04

Thiazole heterocycles constitute an interesting class of molecules, which exhibit a broad spectrum of biological activity, including antifungal properties [[16], [17], [18], [19]]. Encouraged by our previous study that describes the activity of hydrazine-thiazole derivatives against C. gattii and C
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br Conclusions and perspectives In view of the
2024-11-04

Conclusions and perspectives In view of the evidences supporting that Silodosin receptor MAS receptors mediate the effects of AT1 antagonists (Iwai et al., 2012, Ohshima et al., 2014, Pernomian et al., 2015, Schuchard et al., 2015), the prime targets from the perspectives on future directions in
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AR Vs are truncated AR proteins lacking the
2024-11-04

AR-Vs are truncated AR proteins lacking the AR ligand-binding domain (AR-LBD) [6]. While AR-Vs have frequently been detected in CRPC, their expression and functional role in benign prostate tissues and primary prostate cancers is not readily apparent. Structural rearrangements in the AR gene and alt
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br Introduction AMPA receptors AMPARs mediate
2024-11-04

Introduction AMPA receptors (AMPARs) mediate the majority of fast excitatory postsynaptic currents (EPSCs) in the herpes simplex virus 1 (Jonas, 2000). The brevity of EPSCs and rapid deactivation of AMPARs depend upon a short lifetime of synaptically released glutamate, estimated to be about 1 ms
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Here we have used transcriptome analysis of primary neonatal
2024-11-04

Here, we have used transcriptome analysis of primary neonatal rat cardiomyocytes treated with either the ETR agonist endothelin-1 or the α1-AR agonist phenylephrine to assess differences in their respective signalling networks, and further probed these differences using a panel of fluorescent resona
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br Experimental section br Results
2024-11-04

Experimental section Results and discussion Conclusions We present a simple, sensitive and selective assay of ADA activity and its inhibitor using the enzyme catalyzed reaction and the different interaction intensity of dye-labeled AD aptamer, aptamer/AD complex with GO. The as-proposed met
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br Conclusion In this brief Letter we
2024-11-01

Conclusion In this brief Letter, we report an easy method for the preparation of the antileukemic natural product 1. Using a biomimetic strategy,1, 8 in which the aromatic residues are attached to a lysine moiety prior to the reduction of the central carboxylate group, a step-economical synthesis
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In fact serotonin is a major
2024-11-01

In fact, serotonin is a major modulator of dopaminergic (DA) neuronal activity through the 5-HT2C receptor. Studies have shown that the selective 5-HT2C receptor agonist Ro60-0175 blocks the burst-firing of mesolimbic DA neurons, which project from the ventral tegmental area (VTA) to the nucleus acc
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Aurora A overexpression is also related to the activation of
2024-11-01

Aurora-A overexpression is also related to the activation of NF-κB, a potent anti-apoptotic effector that may play a role in preventing apoptosis in cancer INT-777 [18]. These data show that we are still at the beginning of unraveling the complex mechanism by which these gene products and proteins
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In addition to pH regulation by
2024-11-01

In addition to pH regulation by ion (counter-) fluxes, acidification is regulated by the abundance of V-ATPase on organelles, by the pumping activity of the complex and by proton leakage. In yeast, the V-ATPase VO subunit a is the only subunit expressed in two isoforms termed Stv1p and Vph1p. V-ATPa
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br Materials and methods br
2024-11-01

Materials and methods Results Discussion Many studies investigate the role of 12/15-LOX in cancer cell,23, 24, 25 however we here first found that host 12/15-LOX also plays an important role in metastasis progression. We have demonstrated that 12(S)-HETE increased melanoma cell adhesion to
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Having demonstrated that Gq coupled mGluR a was necessary
2024-11-01

Having demonstrated that Gq-coupled mGluR1a was necessary for estradiol-induced enhancement of CREB phosphorylation, we hypothesized that activation of a separate G-protein signaling pathway could explain the effect of estradiol on L-type calcium channel signaling (Boulware et al., 2005). Indeed, i
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At the outset of targeting the two
2024-11-01

At the outset of targeting the two Gln756 side-chain rotamers, it was unclear which rotational isomer would lead to more potent ASK1 inhibitors. While such a preference might have been anticipated, the cohort of ASK1 inhibitors in Table 3 did not provide any guidance regarding which of the Gln756 am
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