Synthesis and biochemical study of N2-(p-n-butylphenyl)-2'-deoxyguanosine 5'-(alpha,beta-imido)triphosphate (BuPdGMPNHPP): a non-substrate inhibitor of B family DNA polymerases
Biochemistry & Molecular Pharmacology
Graduate School of Biomedical Sciences; Department of Pharmacology and Molecular Toxicology
Medical Subject Headings
DNA Polymerase beta; Deoxyguanine Nucleotides; Enzyme Inhibitors; Guanylyl Imidodiphosphate; Humans
Life Sciences | Medicine and Health Sciences
BuPdGMPNHPP was synthesized and assayed as a non-incorporable inhibitor of B family DNA polymerases. The derivative was synthesized by preparation of the imidophosphorane of BuPdG followed by reaction with orthophosphate using the imidazolide method. BuPdGMPNHPP inhibited human DNA polymerase alpha and T4 DNA polymerase 10 and 3.5-times more potently than BuPdGTP, respectively, and was not a substrate for either enzyme. BuPdGMPNHPP acts as an active site affinity probe that could find use in co-crystallization trials of B family DNA polymerases.
Rights and Permissions
Citation: Nucleosides Nucleotides. 1998 Aug;17(8):1505-13.
Nucleosides and nucleotides
Stattel, James Michael Walker; Yanachkov, Ivan; and Wright, George E., "Synthesis and biochemical study of N2-(p-n-butylphenyl)-2'-deoxyguanosine 5'-(alpha,beta-imido)triphosphate (BuPdGMPNHPP): a non-substrate inhibitor of B family DNA polymerases" (1998). GSBS Student Publications. 1162.