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Tetrazole is one of the most
2022-06-24
1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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br Methods br Results and discussion Protein analysis of com
2022-06-24
Methods Results and discussion Protein analysis of commonly used cell lines (C6, D54-MG, U87, U251 and STTG1) reveals high 6-Aminonicotinamide of SXC (Cho and Bannai, 1990, Ye et al., 1999, de Groot et al., 2005, Lyons et al., 2007, Savaskan et al., 2008). Since protein expression can be alter
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br Acknowledgments br The authors
2022-06-24
Acknowledgments The authors would like to acknowledge the technical assistance of J. Lee. This work was supported by the U.S. National Institute of Health grant HL111206 (to R.A.H.) the Italian Ministry for University and Research (MIUR 2010329EKE). Introduction The liver plays a vital role
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br Experimental br Acknowledgments This
2022-06-24
Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t
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It is increasingly argued that the
2022-06-24
It is increasingly argued that the immunosuppressive effects of GCs are conferred indirectly by GR through the activation of genes encoding proteins that inhibit Gemfibrozil of proinflammatory genes 86, 87, 88. Genomic studies offer another mechanism compatible with the idea that GC-mediated repres
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The vast majority of clinical studies have shown that chroni
2022-06-24
The vast majority of clinical studies have shown that chronic administration of GLP-1R agonists frequently lowers SBP/DBP in diabetic humans, which is consistent with preclinical studies, though the reported reductions are not as potent as those observed in their animal counterparts. In contrast, ac
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In a meta analysis of
2022-06-24
In a meta-analysis of genome-wide association studies, a variant (rs10423928) in the GIPR gene has been found to be associated with elevated postprandial glucose and insulin (Saxena et al., 2010) as well as lean body composition including decreased BMI, lean mass and waist circumference (Lyssenko et
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Here we used a designer receptors activated exclusively by
2022-06-24
Here, we used a designer receptors activated exclusively by designer drugs (DREADD)-based chemogenetic approach in a novel Ghsr-IRES-Cre knock-in mouse line to test whether the activity of MBH GHSR neurons is required for the normal rebound food intake following fasting. We also used the Ghsr-IRES-C
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ETV plays an important role in tumorigenesis and metastasis
2022-06-24
ETV5 plays an important role in tumorigenesis and metastasis. For example, chromosomal rearrangement of ETV5 which results in increased ETV5 level is believed as a common event driving human prostate cancer (Helgeson et al., 2008; Huang and Waknitz, 2009). Ghrelin/acyl-ghrelin also plays an importan
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Dipraglurant br Mechanisms of gap junction internalization d
2022-06-24
Mechanisms of gap junction internalization: disaggregation, endocytosis and annular gap junctions It has been clearly shown that gap junction internalization can occur by a distinctive mechanism where one cell internalizes an entire gap junction via formation of double membrane structure termed a
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AD is an irreversible and progressive neurodegenerative dise
2022-06-24
AD is an irreversible and progressive neurodegenerative disease affecting the sphingosine kinase which insidiously destroys memory, thinking skills and cognition. Originally described in 1906 by German physician Alois Alzheimer, AD is characterized by the presence of intraneuronal neurofibrillary ta
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Recently some researchers working in
2022-06-24
Recently, some researchers working in China Pharmaceutical University developed novel FFA1 agonists some of which were found to be efficacious in the management of type 2 diabetes and with low toxicity. For instance, Zheng et al. [48] in their in vivo study using experimental animals, reported that
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br Rationale The present study was motivated to
2022-06-24
Rationale The present study was motivated to get further insight into the molecular recognition processes of 2-alkyl(amino)ethyl-1,1-bisphosphonates taking compounds 12–14 as reference structures. We have recently demonstrated that TcFPPS inhibitors 12 and 13 bind to the allylic site of the enzym
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br Factor Xa an enzyme in the
2022-06-24
Factor Xa, an enzyme in the coagulation cascade, has recently been identified as having a role in inflammation, generating interest in factor Xa inhibitors as anti-inflammatory agents beyond their established use as anticoagulants [, , , ]. We report sustained clinical and electrophysiologic impro
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br Introduction br Results br Discussion
2022-06-24
Introduction Results Discussion Experimental Acknowledgment Introduction Endocannabinoids, N-arachidonoylethanolamine (AEA) and 2-arachidonoylglycerol (2-AG) have been found in most mammalian tissues and they stimulate cannabinoid CB1 and CB2 receptor activity thereby modulating se
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