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Gratifyingly compound also demonstrated improved
2023-07-29

Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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The finding that OCT is expressed in the nucleus accumbens
2023-07-29

The finding that OCT3 is expressed in the nucleus accumbens (Gasser et al., 2009) suggests that inhibition of this transporter may underlie previously described effects of glucocorticoids on extracellular DA concentrations and indicates that DA clearance in this region is not mediated exclusively by
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GW9508 Since non lipoprotein derived free cholesterol is rec
2023-07-29

Since non-lipoprotein-derived free cholesterol is recycled from the plasma membrane through the endosomal system through receptor-independent mechanisms, we wanted to determine whether ABCA2 could alter the trafficking of this source of free cholesterol. Our approach was to measure the effect of mob
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Since the cloning of ARs
2023-07-29

Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav
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br Dihydrotestosterone in adult fish and frogs br New perspe
2023-07-28

Dihydrotestosterone in adult fish and frogs New perspectives and next directions Similar to other androgens, DHT can modulate reproductive endpoints in both fish and amphibians. However, predicting the effects of DHT can be challenging, as reproductive homeostasis is dependent upon the balance
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In humans the major LOs are subdivided by their
2023-07-28

In humans, the major LOs are subdivided by their positional specificity into 5-(ALOX5), 12-(ALOX12) and 15-LO (ALOX15) (Kuhn et al., 2015). 5-LO is the key enzyme for LT biosynthesis and mainly found in mature cells from myeloid origin, including neutrophil, eosinophil and basophil granulocytes, mon
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Nemonapride Taken together BRP represents a novel chemotype
2023-07-28

Taken together, BRP-187 represents a novel chemotype of LT biosynthesis inhibitors with outstanding potency in human PMNL and monocytes activated under pathophysiological relevant conditions and with effectiveness in vivo. Using the PLA that visualizes the in situ interaction between 5-LO and FLAP i
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Our previous work fails to
2023-07-28

Our previous work fails to show any maternal effect with blockade of 5-HT2A receptor, as acute and repeated treatment of MDL100907 does not alter maternal behavior at the behaviorally active doses (Chen et al., 2014). In the present study, MDL100907 pretreatment attenuated the maternal disruptive ef
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br Patients and Methods br Results br
2023-07-28

Patients and Methods Results Discussion Gjerdrum et al showed that Axl Spermine NONOate is required to maintain the mesenchymal-like invasiveness of metastatic breast carcinoma cells, but Axl knockdown has no effect on the cell proliferation of MDA-MB-231 cells. Mackiewicz et al also showe
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To test the compounds metabolic
2023-07-28

To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structura
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The elevated levels of intracellular
2023-07-28

The elevated levels of intracellular antioxidant such as reduced glutathione (GSH) are normally oberserved is various tumor GMX1778 which confers the chemoresistant to chemotherapy [59]. Therefore, the induction of oxidative stress via elevation of intracellular ROS and dimunition of intracellular G
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Bran is a byproduct of flour milling typically utilized
2023-07-28

Bran is a byproduct of flour milling, typically utilized as a valuable component of animal feeds. Because of its attractive technological and health-promoting properties, it AH 6809 has also been increasingly used in food manufacturing as a source of dietary fiber. Indeed, with the growing interest
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Cisplatin br STAR Methods br Acknowledgments
2023-07-28

STAR★Methods Acknowledgments We thank Simcere Pharmaceuticals, Nanjing, China, for providing a rabbit anti-VEGF neutralizing monoclonal antibody. We thank Dr. Schlisio in the Ludwig Institute for Cancer Research, Karolinska Institute, for assistance with hypoxia assay. Y.C.’s laboratory is sup
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In the current investigation we studied
2023-07-28

In the current investigation, we studied the effect of propofol on prostate cancer cells. Propofol is one of the most commonly used drugs in the critical care setting and for the induction of general anesthesia and moderate and deep sedation intraoperatively. Recent studies indicated that propofol e
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A phase I trial has
2023-07-28

A phase I trial has recently evaluated enzalutamide, an anti-androgen agent, in patients with ER- and AR-positive advanced BC to estimate safety and tolerability of enzalutamide therapy alone or in association to anastrozole, exemestane or fulvestrant [65]. The results of major clinical trials with
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