title: A specific substrate-inhibitor, a 2'-deoxy-2'-fluorouridine-containing oligoribonucleotide, against human RNase L.
abstract: We examined the properties of RNA analogues containing 2'-deoxy-2'-alpha-fluorouridine (1) or 2'-O-methyluridine (2) as inhibitors against human RNase L, that cleaves a single-stranded RNA in the presence of 2',5'-linked oligoadenylate (2-5A). The RNA analogue, FF, containing two molecules of 1 in place of uridine efficiently inhibited the RNase L-catalyzed RNA cleavage reaction, whereas the analogue, MM, containing two molecules of 2 was found not to have affinity for the enzyme. The k(cat) value for FF was 1/100 of that for an unmodified RNA, UU, whereas the K(m) value of FF was only twice as great as that of UU. Thus, it was found that the analogue, FF, containing 1 is an efficient inhibitor against human RNase L.
authors: Department of Biomolecular Science, Faculty of Engineering, Gifu University, Yanagido, Gifu, 501-1193, Japan.
authors: Yoshihito
authors: Y
authors: Ueno
authors: Yuuki
authors: Y
authors: Yamada
authors: Masayuki
authors: M
authors: Nakanishi
authors: Yukio
authors: Y
authors: Kitade
mesh_terms: D002384:Catalysis; D004722:Endoribonucleases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004735:Energy Transfer; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D006868:Hydrolysis; D009843:Oligoribonucleotides / Q000737:chemistry / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D009843:Oligoribonucleotides; D011994:Recombinant Proteins; D004722:Endoribonucleases; C031956:2-5A-dependent ribonuclease