To evaluate the possible variations of adenosine receptor (AR) profile together with TNF-α and IL-6 mRNA in cardiac tissue of obese Zucker rats (OZR) during fasting conditions (fc) and during the induction of acute hyperglycemia (AH). OZR (O, n=21) and age-matched lean control rats (CO, n=18) were studied during fc (COfc, n=8; Ofc, n=13) and during the induction of AH (COAH, n=10; OAH, n=8). The histopathologic analysis performed on O and CO heart samples did not show abnormalities of myocardial structure. The AR transcriptomic profile was analyzed in O and CO by real-time polymerase chain reaction (PCR) and a significantly lower mRNA expression was observed for A2AR in O with respect to CO (p=0.047), while a significant upregulation was observed for A3R in O with respect to CO (p=0.002). No significant differences between O and CO were observed for TNF-α or IL-6. Correlations were found between glycemia and A1R (p=0.03) and A2BR (p=0.002); total cholesterol and A2BR (p=0.02) and A3R (p=0.0002), as well as between IL-6 and A1R (p=0.05) and TNF-α and A2AR (p<0.0001). The modulation of ARs in these settings could represent a promising approach to pharmacological treatment, which must be supported by diet restrictions and physical exercise.
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http://dx.doi.org/10.1089/dna.2014.2770 | DOI Listing |
Curr Med Chem
January 2025
Laboratory of Pharmaceutical Biotechnology and Bioinformatics, Department of Genetic Engineering and Biotechnology, Jashore University of Science and Technology, Jashore, 7408, Bangladesh.
Background: Breast cancer is a frequently diagnosed malignant disease and the primary cause of mortality among women with cancer worldwide. The therapy options are influenced by the molecular subtype due to the intricate nature of the condition, which consists of various subtypes. By focusing on the activation of receptors, Epidermal Growth Factor Receptor (EGFR) tyrosine kinase can be utilized as an effective drug target for therapeutic purposes of breast cancer.
View Article and Find Full Text PDFACS Pharmacol Transl Sci
January 2025
Pharmaceutical Institute, Pharmacology and Toxicology, University of Bonn, Gerhard-Domagk-Str. 3, 53121 Bonn, Germany.
Lipopolysaccharide (LPS)-neutralizing peptides are emerging as new potential therapeutic modalities to treat sepsis and skin infections. Purinergic ligand-gated ion channels (P2X receptors) play a critical role in various biological processes, including inflammation. Recent drug development efforts have significantly focused on the modulation of P2X receptors.
View Article and Find Full Text PDFPharmacol Ther
January 2025
Laboratório de Neuroimunologia, Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil. Electronic address:
The purinergic P2Y receptors comprise eight G-coupled receptor (GPCR) subtypes already identified (P2Y, P2Y, P2Y, P2Y, P2Y, P2Y). P2Y receptor physiological agonists are extracellular purine and pyrimidine nucleotides such as ATP (Adenosine triphosphate), ADP (Adenosine diphosphate), UTP (Uridine triphosphate), UDP (Uridine diphosphate), and UDP-glucose. These receptors are expressed in almost all cells.
View Article and Find Full Text PDFBiomed Pharmacother
January 2025
College of Veterinary Medicine, Konkuk University, 120, Neungdong-ro, Gwangjin-gu, Seoul 05029, Republic of Korea. Electronic address:
Rett syndrome (RTT) is a neurological disorder caused by a mutation in the X-linked methyl-CpG binding protein 2 (MECP2), leading to cognitive and motor skill regression. Therapeutic strategies aimed at increasing brain-derived neurotrophic factor (BDNF) levels have been reported; however, BDNF treatment has limitations, including the inability to penetrate the blood-brain barrier, a short half-life, and potential for adverse effects when administered via intrathecal injection, necessitating novel therapeutic approaches. In this study, we focused on the adenosine A receptor (AR), which modulates BDNF and its downstream pathways, and investigated the therapeutic potential of CGS21680, an AR agonist, through in vitro and in vivo studies using R106W RTT model.
View Article and Find Full Text PDFChempluschem
January 2025
Kaiserslautern University of Technology: Rheinland-Pfalzische Technische Universitat Kaiserslautern-Landau, Chemistry, 67663, Kaiserslautern, GERMANY.
We report the synthesis of a series of detergents with a lactobionamide polar head group and a tail containing four to seven perfluorinated carbon atoms. Critical micellar concentrations (CMCs) were determined using isothermal titration calorimetry (ITC) and surface tension (SFT) measurements, showing a progressive decrease from 27 mM to about 0.2 mM across the series.
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