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An artificial copper complex incorporating a cell-penetrating peptide inhibits nuclear factor-κB (NF-κB) activation.

Abstract：

:Nuclear factor-κB (NF-κB) is an inducible transcription factor activated by a variety of cytokines, and promotes the transcription of genes involved in cancer, inflammation, autoimmune disease, and viral infection, among others. Because of its involvement in numerous disease processes, considerable research has focused on NF-κB as a potential drug target. We previously reported that cupric ion (Cu(2+)) blocks NF-κB activation. However, Cu(2+) is unsuitable for drug applications. The copper complex of an artificial peptide HPH-Pep (HPH-Pep-Cu(2+)) was a promising alternative, but it did not easily cross the cell membrane. We report the development of a NF-κB inhibiting Cu(2+) complex with improved cell-penetrating activity arising from the coupling of a Tat peptide to HPH-Pep-Cu(2+).

journal_name

Chem Pharm Bull (Tokyo)

journal_title

Chemical & pharmaceutical bulletin

authors

Kanemaru Y,Momiki Y,Matsuura S,Horikawa T,Gohda J,Inoue J,Okamoto Y,Fujita M,Otsuka M

doi

10.1248/cpb.59.1555

subject

Has Abstract

pub_date

2011-01-01 00:00:00

pages

1555-8

issue

12

eissn

0009-2363

issn

1347-5223

pii

JST.JSTAGE/cpb/59.1555

journal_volume

59

pub_type

杂志文章

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