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However although in vitro studies
2024-11-25

However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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In the late s Solvay Pharmaceuticals discontinued the Phase
2024-11-25

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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An alternative approach to the administration of ADO
2024-11-25

An alternative approach to the administration of ADO agonists is to amplify the actions of endogenous ADO by inhibiting the ADO-metabolizing enzyme, ADO kinase (AK). Inhibition of AK has the net effect of potentiating the local concentration and the effects of ADO in the extracellular compartment. T
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br Functional consequences of ADK regulation on astrocyte
2024-11-25

Functional consequences of ADK regulation on astrocyte function As outlined above (see introduction), ADK critically regulates the extracellular adenosine levels in GLP-2 (rat) synthesis (Boison, 2006, Etherington et al., 2009). Changes in the levels of adenosine, as a result of the regulation o
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Since pyrrolopyrimidine dithiolanes and both displayed parti
2024-11-25

Since pyrrolopyrimidine dithiolanes and both displayed particularly excellent levels of ACK1 inhibition, these analogs were viewed as potential candidates for further investigation in tumor xenograft experiments. While in vitro metabolic studies indicated that pyrrolidine was predicted to be sign
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br ACh and ER tests hereafter Spasm
2024-11-25

ACh and ER tests hereafter Spasm provocation tests have self-limitations to document coronary artery spasm during daily life. In the past reports, ST elevation was reproducible in some patients with variant BIO-acetoxime by the administration of ACh or ER. However, we now employ the ER and ACh s
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There is also a literature on the
2024-11-25

There is also a literature on the impact of commodity (consumption) taxation under imperfect competition. Besley (1989) applies a Cournot model, in which production takes place under IRS and in which free entry leads to an excessive number of firms in the market. Introducing a distortive specific co
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Inactivation of the proton pump comes with luminal
2024-11-23

Inactivation of the proton pump comes with luminal alkalinization of the targeted vesicles such as lysosomes (Fig. 2b). Lysosome pH can also be raised stoichiometrically by addition of a membrane-permeable weak uk5099 such as methylamine or chloroquine which accumulates in its protonated, non-membr
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ACY1215 There is little question that as
2024-11-23

There is little question that as we become more proficient in the diagnosis of arginase 1 deficiency individuals with intermediary elevations in arginine on newborn screening and partial defects in enzymatic activity will be found. There are no reliable data to determine a safe level of arginine and
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In addition to attracting immune cells
2024-11-23

In addition to attracting immune cells to the site of injury, ROS also participate in proliferative responses during compensatory proliferation and regeneration. In Xenopus tadpoles, tail amputation induces sustained production of ROS over the span of regeneration, and decreasing ROS levels, especia
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br Application of bamboo in the food and pharmaceutical indu
2024-11-23

Application of bamboo in the food and pharmaceutical industry For decades, the application of antioxidants in the food and pharmaceutical industry has been widespread. In the past, antioxidants were previously used to control oxidation and retard spoilage but today, many are used because of putat
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Recently whey products have been
2024-11-23

Recently, whey products have been added to nutritional beverages to boost their antioxidant capacity. Supplementation of a lemon drink with 1% WP hydrolyzed by subtilisin increased the antioxidant activity of the beverage from 0.75 to 7.79 mmol of TE/L (Athira et al., 2014). In addition, a flavored
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Pathological angiogenesis occurs when an imbalance of
2024-11-23

Pathological angiogenesis occurs when an imbalance of endogenous proangiogenic and antiangiogenic factors occurs. Although the focus of angiogenesis-related drug development has been geared to the discovery of antiangiogenic compounds for use in pathologies where excessive angiogenesis occurs (cance
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The androgen receptor gene AR is located
2024-11-23

The androgen receptor gene (AR) is located on the X-chromosome and consists of eight exons in humans (Brown et al., 1989; Kuiper et al., 1989). The similar gene structure in mice, monotremes and marsupials indicates AR is highly conserved in mammals (Choong et al., 1998; Faber et al., 1991; He et al
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br Materials and methods br Conflict of interest br Acknowle
2024-11-23

Materials and methods Conflict of interest Acknowledgments We thank Christine Heiner (Department of Surgery, University of Pittsburgh) for her critical reading of the manuscript. This work was supported by grants from the US National Institutes of Health (R01GM115366, R01CA160417, and R01CA
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