Development of cell-penetrating R7 fragment-conjugated helical peptides as inhibitors of estrogen receptor-mediated transcription.
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%.
National Institute of Health Sciences , Tokyo 158-8501, Japan.
Takaya
T
Nagakubo
Yosuke
Y
Demizu
Yasunari
Y
Kanda
Takashi
T
Misawa
Takuji
T
Shoda
Keiichiro
K
Okuhira
Yuko
Y
Sekino
Mikihiko
M
Naito
Masaaki
M
Kurihara
D001120:Arginine; D002460:Cell Line; D057846:Cell-Penetrating Peptides / Q000737:chemistry* / Q000494:pharmacology*; D055808:Drug Discovery; D006801:Humans; D008958:Models, Molecular; D017433:Protein Structure, Secondary; D011960:Receptors, Estrogen / Q000378:metabolism*; D014158:Transcription, Genetic / Q000187:drug effects*
D057846:Cell-Penetrating Peptides; D011960:Receptors, Estrogen; D001120:Arginine