Development of Cell-Penetrating R7 Fragment-Conjugated Helical Peptides as Inhibitors of Estrogen Receptor-Mediated Transcription

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 th...

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Veröffentlicht in:Bioconjugate chemistry 2014-11, Vol.25 (11), p.1921-1924
Hauptverfasser: Nagakubo, Takaya, Demizu, Yosuke, Kanda, Yasunari, Misawa, Takashi, Shoda, Takuji, Okuhira, Keiichiro, Sekino, Yuko, Naito, Mikihiko, Kurihara, Masaaki
Format: Artikel
Sprache:eng
Schlagworte:
Arginine
Biosynthesis
Cell Line
Cell-Penetrating Peptides - chemistry
Cell-Penetrating Peptides - pharmacology
Cellular biology
Drug Discovery
Estrogens
Gene expression
Humans
Models, Molecular
Peptides
Pharmacology
Protein Structure, Secondary
Receptors, Estrogen - metabolism
Transcription, Genetic - drug effects
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Zusammenfassung: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%.
ISSN:1043-1802
1520-4812
DOI:10.1021/bc500480e