Development of cell-penetrating R7 fragment-conjugated helical peptides as inhibitors of estrogen receptor-mediated transcription

Takaya Nagakubo; Yosuke Demizu; Yasunari Kanda; Takashi Misawa; Takuji Shoda; Keiichiro Okuhira; Yuko Sekino; Mikihiko Naito; Masaaki Kurihara

doi:10.1021/bc500480e

Development of cell-penetrating R7 fragment-conjugated helical peptides as inhibitors of estrogen receptor-mediated transcription

Bioconjug Chem. 2014 Nov 19;25(11):1921-4. doi: 10.1021/bc500480e. Epub 2014 Nov 7.

Authors

Takaya Nagakubo¹, Yosuke Demizu, Yasunari Kanda, Takashi Misawa, Takuji Shoda, Keiichiro Okuhira, Yuko Sekino, Mikihiko Naito, Masaaki Kurihara

Affiliation

¹ National Institute of Health Sciences , Tokyo 158-8501, Japan.

PMID: 25375254
DOI: 10.1021/bc500480e

Abstract

The heptaarginine (R7)-conjugated peptide 5 was designed and synthesized as an inhibitor of ER-coactivator interactions and ER-mediated transcription at the cellular level. The R7-conjugated peptide 5 was able to enter ER-positive T47D cells efficiently, and treatment with 3 μM of 5 downregulated the mRNA expression of pS2 (an ER-mediated gene) by 87%.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Arginine*
Cell Line
Cell-Penetrating Peptides / chemistry*
Cell-Penetrating Peptides / pharmacology*
Drug Discovery*
Humans
Models, Molecular
Protein Structure, Secondary
Receptors, Estrogen / metabolism*
Transcription, Genetic / drug effects*

Substances

Cell-Penetrating Peptides
Receptors, Estrogen
Arginine