Biomaterial Database

Inhibition of reverse transcriptase activity of avian myeloblastosis virus by pyrophosphate analogues. 1982

B Eriksson, and G Stening, and B Oberg

Several pyrophosphate analogues have been studied for their effects on avian myeloblastosis virus reverse transcriptase and on cellular DNA polymerase alpha. Examination of structure-activity relationships for these compounds revealed that two acidic groups connected by a short bridge were necessary, but not sufficient, for inhibition of the enzyme activities. Foscarnet sodium (trisodium phosphonoformate) was the most potent inhibitor of reverse transcriptase, giving non-competitive inhibition of reactions primed by (rA)n . (dT)12-18, (rC)n . (dG)12-18, (dC)n . (dG)12-18, and activated DNA. Carbonyldiphosphonate and 2-hydroxyphosphonoacetate also caused non-competitive inhibition patterns, whereas hypophosphate and imidodiphosphonate inhibited AMV reverse transcriptase in a competitive, non-linear manner. The reverse transcriptase reactions directed by (rA)n . (dT)12-18 and activated DNA were most affected by the non-competitive inhibitors. Hypophosphate and imidodiphosphonate inhibited preferentially reactions primed by (dC)n . (dG)12-18 and activated DNA. In all cases the (rC)n . (dG)12-18 directed reaction was the least affected.

UI	MeSH Term	Description	Entries
D007700	Kinetics	The rate dynamics in chemical or physical systems.
D009189	Avian Myeloblastosis Virus	A species of ALPHARETROVIRUS causing anemia in fowl.	Myeloblastosis Virus, Avian,Avian Myeloblastosis Viruses,Myeloblastosis Viruses, Avian,Virus, Avian Myeloblastosis,Viruses, Avian Myeloblastosis
D010746	Phosphonoacetic Acid	A simple organophosphorus compound that inhibits DNA polymerase, especially in viruses and is used as an antiviral agent.	Phosphonoacetate,Disodium Phosphonoacetate,Fosfonet Sodium,Phosphonacetic Acid,Phosphonoacetate, Disodium
D011089	Polydeoxyribonucleotides	A group of 13 or more deoxyribonucleotides in which the phosphate residues of each deoxyribonucleotide act as bridges in forming diester linkages between the deoxyribose moieties.	Polydeoxyribonucleotide
D011756	Diphosphates	Inorganic salts of phosphoric acid that contain two phosphate groups.	Diphosphate,Pyrophosphate Analog,Pyrophosphates,Pyrophosphate Analogs,Analog, Pyrophosphate
D004164	Diphosphonates	Organic compounds which contain P-C-P bonds, where P stands for phosphonates or phosphonic acids. These compounds affect calcium metabolism. They inhibit ectopic calcification and slow down bone resorption and bone turnover. Technetium complexes of diphosphonates have been used successfully as bone scanning agents.	Bisphosphonate,Bisphosphonates
D004257	DNA Polymerase II	A DNA-dependent DNA polymerase characterized in E. coli and other lower organisms. It may be present in higher organisms and has an intrinsic molecular activity only 5% of that of DNA Polymerase I. This polymerase has 3'-5' exonuclease activity, is effective only on duplex DNA with gaps or single-strand ends of less than 100 nucleotides as template, and is inhibited by sulfhydryl reagents.	DNA Polymerase epsilon,DNA-Dependent DNA Polymerase II,DNA Pol II,DNA Dependent DNA Polymerase II
D001354	Avian Leukosis Virus	The type species of ALPHARETROVIRUS producing latent or manifest lymphoid leukosis in fowl.	Leukosis Virus, Avian,Lymphomatosis Virus, Avian,Rous-Associated Virus,Avian Leukosis Viruses,Avian Lymphomatosis Virus,Avian Lymphomatosis Viruses,Leukosis Viruses, Avian,Lymphomatosis Viruses, Avian,Rous Associated Virus,Virus, Avian Leukosis,Virus, Avian Lymphomatosis,Virus, Rous-Associated,Viruses, Avian Leukosis,Viruses, Avian Lymphomatosis
D013329	Structure-Activity Relationship	The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.	Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D017245	Foscarnet	An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.	Phosphonoformate,Phosphonoformic Acid,Foscarnet Barium (2:3) Salt,Foscarnet Calcium (2:3) Salt,Foscarnet Disodium Salt,Foscarnet Magnesium (2:3) Salt,Foscarnet Manganese (2+) (2:3) Salt,Foscarnet Sodium,Foscarnet Sodium Hexahydrate,Foscarnet Trilithium Salt,Foscarnet Tripotassium Salt,Foscarnet Trisodium Salt,Foscavir,Trisodium Phosphonoformate