The concentrations of guanidino compounds in blood are raised in uraemic patients and may have toxic effects. The concentrations of 13 guanidino compounds in serum were measured in 29 patients with chronic renal failure treated by chronic intermittent haemodialysis using liquid cation exchange chromatography with a highly sensitive fluorescence detection method. For taurocyamine we used another column system. Substantial increases in guanidinosuccinic acid, creatine, N-alpha-acetylarginine, creatinine, guanidine and methylguanidine were found. The values obtained for taurocyamine and beta-guanidinoproprionic acid were much lower than those reported by others: a much smaller increase was observed for beta-guanidinoproprionic acid and taurocyamine was only doubled in 4 of 29 uraemic patients. The concentrations of other guanidino compounds such as arginine and guanidinoacetic acid were normal. No differences were found between the polycystic renal disease, the chronic glomerulonephritis and the interstitial nephritis subgroups.
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http://dx.doi.org/10.1016/0009-8981(86)90220-2 | DOI Listing |
Org Biomol Chem
November 2024
Universitat Rovira i Virgili, Departament de Química Analítica i Química Orgànica, Faculty of Chemistry, C/Marcel·lí Domingo 1, 43007 Tarragona, Spain.
This study focuses on the stereoselective syntheses of 1-deoxysphingosine analogues as potential inhibitors of sphingosine kinase (SphK), particularly targeting its isoforms SphK1 and SphK2, which are implicated in cancer progression and therapy resistance. The research builds on previous work by designing a series of analogues featuring systematic structural modifications like the incorporation of a triazole ring, varying degrees of fluorination, and different head groups (, guanidino, -methylamino, and ,-dimethylamino). These modifications aimed to enhance polar and hydrophobic interactions especially with SphK2.
View Article and Find Full Text PDFBioorg Med Chem
December 2024
Lab of Chemical Biology and Molecular Drug Design, College of Pharmaceutical Science, Zhejiang University of Technology, Deqing 313299, China; Institute of Drug Development & Chemical Biology, Zhejiang University of Technology, Deqing 313299, China; Zhejiang Jieyuan Med-Tech Co., Ltd., Hangzhou, 311113, China. Electronic address:
Transmembrane Serine Protease 2 (TMPRSS2) plays a critical role in tumorigenesis and progression, making its degradation a promising therapeutic strategy. In this study, we designed and synthesized TMPRSS2-PROTACs, including VPOT64 and VPOT76, based on camostat. Both compounds exhibited superior inhibitory effects on HT-29 colorectal and Calu-3 lung cancer cells compared to paclitaxel.
View Article and Find Full Text PDFESC Heart Fail
November 2024
Department of Clinical Sciences and Advanced Medicine, University of Pennsylvania, Philadelphia, Pennsylvania, USA.
Background And Aims: The heart is a metabolic organ rich in mitochondria. The failing heart reprograms to utilize different energy substrates, which increase its oxygen consumption. These adaptive changes contribute to increased oxidative stress.
View Article and Find Full Text PDFMethodsX
December 2024
Centre for Microbiology and Environmental Systems Science, Department of Environmental Geosciences, University of Vienna, Josef-Holaubeck-Platz 2, 1090 Vienna, Austria.
The recent discovery of guanidine-dependent riboswitches in many microbes raised interest in the biological function and metabolism of this nitrogen-rich compound. However, very little is known about the concentrations of guanidine in the environment. Several methods have been published for quantifying guanidine and guanidino compounds in human urine and blood, often relying on derivatization followed by fluorescence detection.
View Article and Find Full Text PDFChemistry
December 2024
Inorganic Chemistry, Ruprecht-Karls Universität Heidelberg, Im Neuenheimer Feld 270, 69120, Heidelberg, Germany.
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