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Optimization of the B ring specifically targeted
2025-01-17

Optimization of the B-ring specifically targeted preventing the oxidation of the ring system (). As described above, the 4-position of the phenyl ring provides the appropriate vector towards bulk solvent. - and -linked substitutions at the 4-position of the B-ring from the 4-fluoro-nitrophenyl inter
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Chronic inflammation is associated with
2025-01-17

Chronic inflammation is associated with both initiation and progression of many neoplastic conditions [149], and ATX may be a player in the process. ATX/LPA signaling is positively correlated with the invasive and metastatic potential of several cancers including melanoma, breast cancer, ovarian can
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Over the past decade extensive research has been directed to
2025-01-17

Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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Evidences have suggested that impairment of CK activity cont
2025-01-17

Evidences have suggested that impairment of CK activity contributes to inhibition of Na+, K+-ATPase and H+-ATPase activities during infectious diseases, since these ATPases are dependent of ATP, as observed by Baldissera et al. [31] in fish experimentally infected by Aeromonas caviae. We observed th
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Acknowledgments br Introduction Prostate cancer is the first
2025-01-17

Acknowledgments Introduction Prostate cancer is the first leading cause of cancer-related deaths among males in the UK and the second in the US. Despite recent advances in surgery, radiation, medical management and screening, prostate cancer patients suffer high morbidity and mortality and signi
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Activated MAP kinases transform the stimulus into the pathop
2025-01-17

Activated MAP kinases transform the stimulus into the pathophysiological responses by phosphorylating downstream substrates, including transcription factors, cytoskeletal proteins involved in mRNA translation (Li et al., 2015). Among the numerous effectors that intervene in the TNF-α action is an ac
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br Experimental EPR spectra of probes
2025-01-16

Experimental EPR spectra of probes 1a–f were recorded on a Bruker EMX-1572 operating at X-band (9.0–9.9 GHz), at 21 ± 1 °C. The EPR parameters were the same in all experiments: microwave power, 1 mW; modulation amplitude, 5 G; time constant, 10.24 ms; and conversion time, 40.96 ms. Reduced gluta
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To the best of our
2025-01-16

To the best of our knowledge, there have been only a few reports on antiangiogenic activities about C. sanki, and its antiangiogenic constituents as well as its mechanism of action are worthy of further exploring and studying. Therefore, we carried out a bioassay-guided investigation of C. sanki in
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Based on the general structure function principle in
2025-01-16

Based on the general structure-function principle in biology [[19], [20], [21]], toxic oligomers are expected to have well-defined three-dimensional structures to carry out their pathological functions. A common amyloid toxicity mechanism also suggests that toxic oligomers of different amyloid prote
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The AMP Activated Protein Kinase AMPK
2025-01-16

The 5′AMP-Activated Protein Kinase (AMPK) has evolved as an important cellular sensor of reduced energy status that can subsequently phosphorylate its target proteins, slowing the rates of key biosynthetic processes and promoting energy producing pathways; for these reasons AMPK has been proposed as
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The functional significance of the
2025-01-16

The functional significance of the cap residues with regard to the established role of PfA-M1 in hemoglobin catabolism in the food vacuole is a key question that is difficult to address with in vitro studies. We note that three of the dipeptide substrates used in our study are found in the sequences
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br cDNA cloning gene structure and chromosomal
2025-01-16

cDNA cloning, gene structure and chromosomal localization The cDNA for the leukocyte-type 12S-lipoxygenase was first cloned from porcine leukocytes [9], and later from mouse [10], [11], rat [12], [13], bovine [14] and rabbit [15] sources. The cDNA for the platelet-type 12S-lipoxygenase cDNA has b
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The second evidence comes from
2025-01-16

The second evidence comes from the results obtained by patch-clamp recordings carried out at the endplate region of isolated mouse FDB fibers, where adenosine and the P1R agonist NECA significantly affected the NPo, the open frequency and the time constant τ of the adult nAChR channels. It is genera
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In this article we have outlined the increasing
2025-01-16

In this article, we have outlined the increasing, as yet still circumstantial evidence that the 6TM domains of bacterial ACs might operate as receptors for as yet unknown ligands. Intriguingly, several architectural arguments are also applicable to the 6TM domains of mammalian membrane-bound ACs (mA
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Endogenous adenosine systems have largely been implicated in
2025-01-16

Endogenous adenosine systems have largely been implicated in drug actions by the demonstration that caffeine (non-selective A1R and A2AR antagonist) (see Section The issue of caffeine), in doses up to 7.5–10mg/kg, inhibits antinociception, and when this occurs, it DAPI hydrochloride is generally al
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