Discovery of peptidic miR-21 processing inhibitor by mirror image phage display: A novel method to generate RNA binding D-peptides.

Abstract:

:A novel method to generate RNA binding D-peptide has been developed. To achieve the screening method, phage display was applied to "Mirrored" RNA (L-enantiomer of RNA). We have selected pre-miR21 as an initial screening target to demonstrate the method. The mirrored pre-miR-21 binding peptide sequences were successfully obtained, and were chemically synthesized using D-amino acids. D-peptide is expected to have favorable properties as a drug candidate such as protease resistance and low immunogenicity. As a result of binding evaluation of the D-peptide to pre-miR-21, the EC50 value was 440nM. In addition, the D-peptide possessed inhibition activity to miR-21 processing.

journal_name

Bioorg Med Chem Lett

authors

Sakamoto K,Otake K,Umemoto T

doi

10.1016/j.bmcl.2017.01.023

subject

Has Abstract

pub_date

2017-02-15 00:00:00

pages

826-828

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(17)30035-5

journal_volume

27

pub_type

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