title: 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+).
authors: Department of Bioorganic Medicinal Chemistry, Faculty of Life Sciences, Kumamoto University, Japan.
authors: Yosuke
authors: Y
authors: Kanemaru
authors: Yumi
authors: Y
authors: Momiki
authors: Saori
authors: S
authors: Matsuura
authors: Tatsufumi
authors: T
authors: Horikawa
authors: Jin
authors: J
authors: Gohda
authors: Jun-ichiro
authors: J
authors: Inoue
authors: Yoshinari
authors: Y
authors: Okamoto
authors: Mikako
authors: M
authors: Fujita
authors: Masami
authors: M
authors: Otsuka
mesh_terms: D057846:Cell-Penetrating Peptides / Q000737:chemistry* / Q000494:pharmacology*; D056831:Coordination Complexes / Q000737:chemistry / Q000494:pharmacology; D003300:Copper / Q000737:chemistry* / Q000494:pharmacology*; D006367:HeLa Cells; D006632:Histamine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000276:immunology; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology*; D054322:tat Gene Products, Human Immunodeficiency Virus / Q000737:chemistry / Q000494:pharmacology
chemical_list: D057846:Cell-Penetrating Peptides; D056831:Coordination Complexes; C448824:HPH-Pep; D016328:NF-kappa B; D011725:Pyridines; D054322:tat Gene Products, Human Immunodeficiency Virus; D003300:Copper; D006632:Histamine