Table 2

Cleavage Rate constants for cleavage of S-30 by Chemically Modified Mrz-12/12.

Miniribozyme (Mrz-12/12)

C₃

U₄

U₇

C_15.2

3' end

Cleavage rate constant (min^-1)

Relative Stability

A

-

-

-

-

-

4.2 ± 0.3

1

B

F

NH₂

NH₂

F

-

0.30 ± 0.05

-

C

-

NH₂

NH₂

-

-

0.18 ± 0.01

-

D

-

NH₂

-

-

-

0.30 ± 0.03

-

E

-

-

NH₂

-

-

7.7 ± 0.8

-

F

-

dT

-

-

-

0.014 ± 0.005

-

G

-

dU

-

-

-

0.024 ± 0.007

-

H

-

OMe

-

-

-

0.01 ± 0.007

-

I

-

ps

-

-

-

3.9 ± 0.06

-

J

OMe

ps

OMe

OMe

psps

7.3 ± 0.7

1400

K

OMe

NH₂

OMe

OMe

-

0.6 ± 0.1

8600

Rz-12/12-L

-

NH₂

-

-

-

0.05 ± 0.009

-

Cleavage conditions; 37°C, pH 7.6, 10 mM MgCl_2. [Rz] = 1 μM, [S30] = 5 nM. (- = unmodified, ie 2'OH). F = 2'-fluoro, NH₂ = 2'-amino, dT = 2'-deoxythymidine, dU = 2'-deoxyuridine, OMe = 2'-O-methyl, ps = 3' phosphorothioate linkage. Stability is defined as the time required in 10% human serum to degrade 75% of full-length ribozyme, relative to unmodified miniribozyme A.

Hendry et al. BMC Chemical Biology 2004 4:1   doi:10.1186/1472-6769-4-1