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From an historical perspective ligands for GPCRs
2024-10-24
From an historical perspective, ligands for GPCRs (adrenaline, serotonin, gsk3beta or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands were r
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Thirdly and finally multiple studies have analyzed
2024-10-24
Thirdly and finally, multiple studies have analyzed the activation of neurons in the auditory telencephalic areas of songbirds in response to various auditory stimuli. Neuronal activation was identified by the increased expression of immediate early genes such as fos or ZENK (also know as zif-268, e
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Sorafenib was the first small
2024-10-24
Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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In the current investigation we studied the effect of propof
2024-10-23
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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br Perspectives br Acknowledgments This investigation was su
2024-10-23
Perspectives Acknowledgments This investigation was supported by a Research Grant 2010/01385-5 from FAPESP (Sao Paulo Research Foundation, Brazil). P.F.S. was recipient of a CNPq (National Council for Scientific and Technological Development, Brazil) productivity grant. R.F.A. was recipient of
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Recent genome wide association studies have indicated SORL
2024-10-23
Recent genome-wide association studies have indicated SORL1 as a risk factor for AD (Meng et al., 2007, Rogaeva et al., 2007, Wen et al., 2013). SORL1, is expressed in neurons (Yin et al., 2015) and also regulates APP traffic from the cell membrane to the Golgi apparatus. A reduction in its expressi
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Thus we presumed that ALDH A
2024-10-23
Thus, we presumed that ALDH1A3 might play an important role in TMZ-chemoresistance in glioblastoma patients. As we expected, the glioblastoma cell lines and primary glioma Caspase-6, human recombinant protein were more sensitive to TMZ treatment when ALDH1A3 was inhibited or depleted. Consistently,
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Microbe derived ligands can also activate AHR
2024-10-23
Microbe-derived ligands can also activate AHR. Malassezia, a commensal yeast in human skin, can metabolize tryptophan into several AHR activating compounds including FICZ and ICZ [59]. Lactobacillus converts tryptophan into indole-3-aldehyde (IAld), which can activate AHR and promote IL-22 productio
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br Introduction Psychostimulant abuse and
2024-10-23
Introduction Psychostimulant abuse and addiction remain a societal problem in the United States. The latest statistics from the National Survey on Drug Use and Health indicate that slightly less than one million people over the age of 12 report having a cocaine use disorder (NSDUH, 2016). Additio
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br Discussion With recently improved understanding of the
2024-10-23
Discussion With recently improved understanding of the role of βARK1 in the progression of HF and as a potential therapeutic target in HF, we explored the relationship between plasma βARK1, as a marker of chronic sympathetic overactivation, and physical symptoms in HF. Our main findings were 1) e
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Taken together BRP represents a novel chemotype of LT
2024-10-23
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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The obtained results indicate that
2024-10-23
The obtained results indicate that even when the impairment of the same forms of memory are present, amnesia can develop in different ways. Impairment of memory reconsolidation in the conditioned food aversion model through both the serotonin receptor antagonist and the antagonist of NMDA glutamate
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During preparation of this manuscript
2024-10-23
During preparation of this manuscript, some studies investigating effects of Sunitinib on Axl activity in renal cancer have been published [44], [45], [46], [47]. However, there are several important considerations to take into account interpreting results of these studies. First, Sunitinib doses th
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In considering the roles of these enzymes in normal
2024-10-23
In considering the roles of these enzymes in normal physiology, given the importance of GLUT4-dependent glucose uptake and glucose-dependent fatty Fluorescein-12-dUTP receptor synthesis for systemic metabolic homeostasis (Herman and Kahn, 2006, Herman et al., 2012), deletion of Acly in adipocytes r
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H-Lys(Z)-OH br Introduction In addition to ATP production an
2024-10-23
Introduction In addition to ATP production, an important role of mitochondria in the pancreatic beta cell is anaplerosis, which is the net synthesis of citric H-Lys(Z)-OH cycle intermediates that are exported to the cytosol where they are converted to numerous other metabolites that stimulate an
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