guanosine-triphosphate and phosphoramidic-acid

guanosine-triphosphate has been researched along with phosphoramidic-acid* in 2 studies

Other Studies

2 other study(ies) available for guanosine-triphosphate and phosphoramidic-acid

Article	Year
β-D-2'-C-Methyl-2,6-diaminopurine Ribonucleoside Phosphoramidates are Potent and Selective Inhibitors of Hepatitis C Virus (HCV) and Are Bioconverted Intracellularly to Bioactive 2,6-Diaminopurine and Guanosine 5'-Triphosphate Forms. Journal of medicinal chemistry, 2015, Apr-23, Volume: 58, Issue:8 The conversion of selected β-D-2,6-diaminopurine nucleosides (DAPNs) to their phosphoramidate prodrug (PD) substantially blocks the conversion to the G-analog allowing for the generation of two bioactive nucleoside triphosphates (NTPs) in human hepatocytes. A variety of 2'-C-methyl DAPN-PDs were prepared and evaluated for inhibition of HCV viral replication in Huh-7 cells, cytotoxicity in various cell lines, and cellular pharmacology in both Huh-7 and primary human liver cells. The DAPN-PDs were pan-genotypic, effective against various HCV resistant mutants, and resistant variants could not be selected. 2'-C-Me-DAPN-TP and 2'-C-Me-GTP were chain terminators for genotype 1b HCV-pol, and single nucleotide incorporation assays revealed that 2'-C-Me-DAPN-TP was incorporated opposite U. No cytotoxicity was observed with our DAPN-PD when tested up to 50 μM. A novel, DAPN-PD, 15c, has been selected for further evaluation because of its good virologic and toxicologic profile and its ability to deliver two active metabolites, potentially simplifying HCV treatment. Topics: 2-Aminopurine; Amides; Antiviral Agents; Cell Line; Cells, Cultured; Guanosine Triphosphate; Hepacivirus; Hepatitis C; Humans; Methylation; Phosphoric Acids; Prodrugs; Ribonucleosides	2015
GTP:GTP guanylyltransferase: trapping procedures for detecting and characterizing chemical nature of enzyme-nucleotide phosphoramidate reaction intermediate. Methods in enzymology, 2002, Volume: 354 Topics: Amides; Amino Acids; Animals; Artemia; Chromatography, High Pressure Liquid; Chromatography, Thin Layer; Dinucleoside Phosphates; Enzyme Inhibitors; Enzyme Stability; Guanosine Triphosphate; Molecular Structure; Nucleotidyltransferases; Phosphoric Acids; Phosphorus Radioisotopes	2002

Article

Year

β-D-2'-C-Methyl-2,6-diaminopurine Ribonucleoside Phosphoramidates are Potent and Selective Inhibitors of Hepatitis C Virus (HCV) and Are Bioconverted Intracellularly to Bioactive 2,6-Diaminopurine and Guanosine 5'-Triphosphate Forms.

Journal of medicinal chemistry, 2015, Apr-23, Volume: 58, Issue:8

The conversion of selected β-D-2,6-diaminopurine nucleosides (DAPNs) to their phosphoramidate prodrug (PD) substantially blocks the conversion to the G-analog allowing for the generation of two bioactive nucleoside triphosphates (NTPs) in human hepatocytes. A variety of 2'-C-methyl DAPN-PDs were prepared and evaluated for inhibition of HCV viral replication in Huh-7 cells, cytotoxicity in various cell lines, and cellular pharmacology in both Huh-7 and primary human liver cells. The DAPN-PDs were pan-genotypic, effective against various HCV resistant mutants, and resistant variants could not be selected. 2'-C-Me-DAPN-TP and 2'-C-Me-GTP were chain terminators for genotype 1b HCV-pol, and single nucleotide incorporation assays revealed that 2'-C-Me-DAPN-TP was incorporated opposite U. No cytotoxicity was observed with our DAPN-PD when tested up to 50 μM. A novel, DAPN-PD, 15c, has been selected for further evaluation because of its good virologic and toxicologic profile and its ability to deliver two active metabolites, potentially simplifying HCV treatment.

Topics: 2-Aminopurine; Amides; Antiviral Agents; Cell Line; Cells, Cultured; Guanosine Triphosphate; Hepacivirus; Hepatitis C; Humans; Methylation; Phosphoric Acids; Prodrugs; Ribonucleosides

2015

GTP:GTP guanylyltransferase: trapping procedures for detecting and characterizing chemical nature of enzyme-nucleotide phosphoramidate reaction intermediate.

Methods in enzymology, 2002, Volume: 354

Topics: Amides; Amino Acids; Animals; Artemia; Chromatography, High Pressure Liquid; Chromatography, Thin Layer; Dinucleoside Phosphates; Enzyme Inhibitors; Enzyme Stability; Guanosine Triphosphate; Molecular Structure; Nucleotidyltransferases; Phosphoric Acids; Phosphorus Radioisotopes

2002