title: 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 EC50value was 440nM. In addition, the D-peptide possessed inhibition activity to miR-21 processing.
authors.affiliation: Research, Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
authors.forename: Kotaro
authors.initials: K
authors.lastname: Sakamoto
authors.affiliation: Research, Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
authors.forename: Kentaro
authors.initials: K
authors.lastname: Otake
authors.affiliation: Research, Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan. Electronic address: tadashi.umemoto@takeda.com.
authors.forename: Tadashi
authors.initials: T
authors.lastname: Umemoto
mesh_terms: D004797:Enzyme-Linked Immunosorbent Assay; D035683:MicroRNAs / Q000737:chemistry / Q000378:metabolism*; D019151:Peptide Library; D010455:Peptides / Q000737:chemistry / Q000378:metabolism*; D011485:Protein Binding; D012322:RNA Precursors / Q000737:chemistry / Q000378:metabolism; D013237:Stereoisomerism; D020349:Surface Plasmon Resonance
chemical_list: D035683:MicroRNAs; D019151:Peptide Library; D010455:Peptides; D012322:RNA Precursors
keywords: D-amino acid; Mirror image; Peptide; Phage display; miRNA