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In the late s Solvay Pharmaceuticals
2024-05-18

In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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A key step in the ADAR
2024-05-18

A key step in the ADAR reaction is the formation of the adenosine covalent hydrate with a tetrahedral center at C6. The nucleoside analog 8-azanebularine (box in Fig. 6), with its relatively high propensity to form a covalent hydrate, is useful as an adenosine replacement in ADAR2 substrates to trap
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br Acknowledgements MC and PD were funded by
2024-05-18

Acknowledgements MC and PD were funded by the Michael J Fox Foundation (Grant ID 9969). We would like to thank Pierluigi Saba, Francesco Traccis and Barbara Tuveri for their technical assistance. Introduction In the prostate, androgens play a crucial role in normal, BPH and cancerous growth b
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Pompe disease is accompanied by
2024-05-18

Pompe disease is accompanied by the deficiency of the lysosomal α-1,4-glucosidase that makes the I-BET-762 unable to hydrolyze glycogen to glucose, thereby resulting in the accumulation of glycogen in lysosomes, especially in skeletal muscles and cardiac tissues. This accumulation results in the st
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However there are studies revealing
2024-05-18

However, there are studies revealing the “dark side” of autophagy at later stages in cancers, when oncogenes (mainly K-ras and B-raf) are activated and/or tumour suppressors such as PTEN and p53 are inactivated. These studies are based on the use of GEMM and deletions of essential autophagy genes (A
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As cytosolic acetyl CoA levels in hepatocytes descend
2024-05-18

As cytosolic acetyl-CoA levels in hepatocytes descend, cellular production and concentration of cholesterol go down, a change that is known to be sensed by the Sterol response element binding protein (SREBP)/Cleavage-Activating Protein system, leading to SREBP escort to the Golgi apparatus, cleavage
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1 646 In our studies of leucine and
2024-05-18

In our studies of leucine and BCH in pancreatic islets and clonal insulin cell lines, we noticed that leucine was a slightly stronger stimulant of insulin release. Previous studies showed that leucine can be metabolized to CO2[11], [12], [13], [14] and can increase acetoacetate in pancreatic islets
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Telomerase action at the telomere is highly regulated it
2024-05-18

Telomerase action at the telomere is highly regulated; it preferentially elongates the shortest telomeres, and recruitment of the enzyme complex to the telomere occurs in mid-S phase of the cell cycle (Bianchi and Shore, 2007, Britt-Compton et al., 2009, Teixeira et al., 2004, Hemann et al., 2001, T
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br Abbreviations br Acknowledgements This work was supported
2024-05-18

Abbreviations Acknowledgements This work was supported by grants from the National Institutes of Health (R01GM114168) and the Office of Naval Research (N000141210773) awarded to J.C·H and National Cancer Institute (5P30CA16059) Cancer Center Support Grant in support of Massey Cancer Center Pro
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It has been known for a while
2024-05-17

It has been known for a while that oxygenation (the addition of oxygen) of Aβ can inhibit the formation of amyloids and diminish their cytotoxicity. Photo-oxygenation of Aβ started with fullerenes almost a decade ago by Toshima and co-workers. Later, porphyrins and polyoxometalates were used as well
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Aerobic exercise plays an important role in
2024-05-17

Aerobic exercise plays an important role in the regulation of Erismodegib receptor metabolism in the skeletal muscle. It is also associated with increases in AMPK and GLUT4 levels, resulting in the improvement of the glucose uptake signaling pathway [17,18]. Recently, it has been shown that exercise
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In a recent series of studies from
2024-05-17

In a recent series of studies from our laboratory, to characterize the contractile systems within the rat MK-3207 HCl australia wall, three conditions were identified that led to detrusor activity: spontaneous micro-contractions, electrical field stimulated (EFS) contractions and muscarinic agonist
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br There are three types of
2024-05-17

There are three types of 5-HT2 receptors. 5-HT2A, 5-HT2B and 5-HT2C receptors Exhibit 46–50% overall sequence identity and couple preferentially to Gq/11 to increase inositol phosphates and cytosolic [Ca2+] and in agreement with their long known role in muscle contraction and stimulation in the br
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These results from the present study are summarized in Table
2024-05-17

These results from the present study are summarized in Table 1. Eight drugs (doxorubicin, epirubicin, daunorubicin, idarubicin, irinotecan, imatinib, sunitinib and gefitinib) inhibited 5-HT-induced 5-HT3A and 5-HT3AB currents; three (irinotecan, topotecan and mitoxantrone) showed different responses
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br Materials and methods br
2024-05-17

Materials and methods Results Discussion Cdc42 has been implicated in mediating the entry of HCV into hepatocytes, but how Cdc42 affects the response of HCV patients to IFN therapy is unknown. This study therefore examined the genetic association between Cdc42-related genes and efficacy of
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