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Recent data from an investigation conducted with beta cell
2021-09-22
Recent data from an investigation conducted with beta-cell cultures and animals suggest that FFAR1 gene Cell Cycle Compound Library is modulated by stimulation of peroxisome proliferator-activated receptor gamma (PPARG) [10]. Intriguingly, in 2001 we had demonstrated effects of the PPARG Pro12Ala s
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br The hippocampus and spatial
2021-09-22
The hippocampus and spatial memory Numerous lines of evidence have implicated the rodent hippocampus in spatial forms of learning and memory (O’Keefe and Nadel, 1978). For example, hippocampal lesions produce robust and reliable deficits on spatial memory tasks such as the Morris watermaze in bot
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Introduction Glucocorticoids are released in response to
2021-09-22
Introduction Glucocorticoids are released in response to stress and play an important role in inflammation, cellular growth, development, body fluid homeostasis, carbohydrate, lipid, and protein metabolism. However, circulating glucocorticoid excess has been associated with a classical phenotype of
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In summary this study shows that compound d has
2021-09-22
In summary, this study shows that compound 4d has strong clinical potential as an efficient GLP-1/GCGR agonist exhibits weight-lowering, lipid-regulation and diabetes-protective effects and plays an important role in the prevention and therapy of diet induced obesity and dyslipidemia. The present st
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Herein we describe the development of second
2021-09-18
Herein, we describe the development of second generation GSM compounds aimed at improving critical physicochemical properties while maintaining the potent activity of the parent AGSM. Ligand design focused on identifying heterocyclic replacements for the hydrophobic D-ring as a means to improve ADME
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Introduction High mobility group box HMGB is
2021-09-18
Introduction High mobility group box 1 (HMGB1) is a nuclear protein that plays a fundamental role in the regulation of DNA-associated events such as DNA repair, transcription, and replication. HMGB1 can be translocated to the cytosol, plasma membrane, and extracellular space in response to various
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Sperm capacitation was negatively r p related with
2021-09-18
Sperm capacitation was negatively (r = −0.68; p ive but not significant (r = 0.22). No significant relationship was observed between the expression levels of either CB1 receptor or FAAH and any of the sperm quality parameters studied. The scatter plot distribution of spermatozoa expression of CB1 an
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In addition to indoles two additional structural
2021-09-18
In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic EGTA side chain to prepare compound (). The extension of the chain was expec
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In addition to indoles two additional structural
2021-09-18
In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic AS 602801 side chain to prepare compound (). The extension of the chain was
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pkc inhibitors Before discovery of their histone
2021-09-18
Before discovery of their histone demethylase function, the JARID1 isoforms were identified across diverse fields including stem cell biology and congenital disease, as detailed in Box 2. Their observed roles in cancer progression and therapy resistance have led to ongoing pursuit of inhibitors tail
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In summary our results support the model that the
2021-09-18
In summary, our results support the model that the histone demethylase KDM5 is a critical host transcriptional regulator that maintains immune homeostasis and is responsible for preservation of the normal commensal microbial community structure and behavior. Neurodevelopmental disorders such as ID a
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br Discussion In our study the prevalence of severe
2021-09-18
Discussion In our study the prevalence of severe periodontitis in patients with HIV infection was 66%, almost twice as high as in uninfected controls. Our results are in line with the prevalence of severe periodontitis found in HIV-infected patients in London, United Kingdom in the pre-cART era:
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Fig illustrates the different signaling pathways elicited
2021-09-18
Fig. 1 illustrates the different signaling pathways elicited or modulated by H3R activation. Collectively, the modulation of the release of histamine and other neurotransmitters through H3R activation could be linked to several neurological disorders such as sleep disorders like narcolepsy, Alzheime
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br Conclusion br Conflict of interest
2021-09-18
Conclusion Conflict of interest Introduction The human epithelial receptor 2 (HER2 or erbb2) is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases that act through the EGF signaling cascade [1,2]. Approximately 20% of breast cancers overexpress HER2
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Given the role that activation of GC
2021-09-18
Given the role that activation of GC-C has in stimulating fluid secretion in the intestine, attempts have been made to exploit this pathway to relieve symptoms of chronic constipation. Currently, an orally administered synthetic ST mimic, linaclotide [29], has been successfully shown to alleviate co
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