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The cellular mechanism underlying the CGS mediated inhibitio
2022-12-01
The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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Extracellular adenosine acts as a local
2022-12-01
Extracellular adenosine acts as a local modulator of cell function via four adenosine receptor subtypes (A1Rs A2AR, A2BR, and A3R) that are involved in numerous physiological and pathophysiological processes [31]. Each is encoded by a separate gene and has different functions, although with some ove
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Our initial approach to identify hits was two pronged
2022-12-01
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI JP 1302 dihydrochloride mg library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein
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br Materials and methods br Results br
2022-12-01
Materials and methods Results Discussion Prostate cancer represents an ideal candidate for chemoprevention because of its high incidence and long latency to clinically significant disease [17]. The precancerous lesion PIN may also be a suitable target for ablation in chemoprevention strateg
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br Funding br Introduction The interest in the effects of
2022-12-01
Funding Introduction The interest in the effects of endocrine disrupting chemicals (EDCs) in the aquatic environment continues to increase over the past decade, specifically those that act on steroidogenic pathways. EDCs that include synthetic androgenic and estrogenic compounds can severely a
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The extent to which GPCR oligomerization
2022-12-01
The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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The consensus amino acid recognition sequence for p
2022-12-01
The consensus amino eph receptor recognition sequence for p38α substrates is (Ser/Thr)Pro (Cuadrado and Nebreda, 2010), typically assisted by upstream docking motifs (Remenyi et al, 2005, Sharrocks et al, 2000). P450c17 has 32 Ser and 25 Thr residues, of which only Thr 341 and Ser 427 are immediate
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br Introduction Human esophageal carcinoma is one
2022-12-01
Introduction Human esophageal carcinoma is one of the most frequently diagnosed cancers, ranked as the eighth leading causes of cancer-related mortality worldwide. Esophagus squamous cell carcinoma (ESCC) is the most common histological type of esophageal carcinomas, especially with a higher inci
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Available data thus indicate that there are at
2022-12-01
Available data thus indicate that there are at least two ways that HMGA proteins can induce localized changes in the chromatin structure of inducible gene promoters, both of which involve positioned nucleosomes that must be “remodeled” before gene transcription can occur. The first mechanism is exem
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br Introduction Alcohol i e ethanol is absorbed into the
2022-11-30
Introduction Alcohol, i.e., ethanol, is absorbed into the blood from the stomach to the small intestine, then distributed throughout the body. The metabolism of alcohol converting to acetic caspofungin basically involves two enzymes; alcohol dehydrogenase converting ethanol to acetaldehyde and a
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COPD is almost unheard of in individuals less than years
2022-11-30
COPD is almost unheard of in individuals less than 40 years of age (even among heavy smokers), 1 in 10 lifetime never-smokers and 1 in 3 develop COPD by age 75 [26], unquestionably, COPD is an age-related disorder. This notion of accelerated ageing of COPD is supported by animal models, which demons
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br AHR expression in cancer Perhaps the earliest
2022-11-30
AHR expression in cancer Perhaps the earliest indicator that the AHR might play an ongoing role in tumorigenesis, independent of its role in generating mutations, was the demonstration that non-genotoxic 2,3,7,8-tetrachlorodibenzo(p)dioxin (TCDD) is a carcinogen in animals and humans [7]. Althoug
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In fact serotonin is a major modulator of dopaminergic
2022-11-30
In fact, serotonin is a major modulator of dopaminergic (DA) neuronal activity through the 5-HT2C receptor. Studies have shown that the selective 5-HT2C receptor agonist Ro60-0175 blocks the burst-firing of mesolimbic DA neurons, which project from the ventral tegmental area (VTA) to the nucleus acc
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br Conflicts of interest br Acknowledgments br
2022-11-30
Conflicts of interest Acknowledgments Significance Introduction Androgen receptor (AR) plays a paramount role in the onset and progression of prostate cancer (PC) (Burnstein, 2005, Lonergan and Tindall, 2011, Watson et al., 2015). This very facet underlies androgen deprivation therapy (A
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br Acknowledgments This work was supported by the Swiss Nati
2022-11-29
Acknowledgments This work was supported by the Swiss National Science Foundation. 15-Lipoxygenase 1 (15-LOX-1) is a nonheme, iron-containing enzyme predominantly expressed in reticulocytes, eosinophils, macrophages, mast cells, and bronchial epithelial cells . 15-LOX-1 is a key enzyme involved
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