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.

journal_name

Bioorg Med Chem

authors

Ueno Y,Yamada Y,Nakanishi M,Kitade Y

doi

10.1016/j.bmc.2003.08.025

subject

Has Abstract

pub_date

2003-11-17 00:00:00

pages

5069-73

issue

23

eissn

0968-0896

issn

1464-3391

pii

S0968089603005911

journal_volume

11

pub_type

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