title: An intracellular targeted NLS peptide inhibitor of karyopherin alpha:NF-kappa B interactions.
abstract: The nuclear import of transcription factors involves proteins termed karyopherins. Previously, we described an intracellular targeted dual nuclear localization sequence (NLS) peptide inhibitor of processes dependent upon the transcription factor NF-kappa B. We have now developed a homogeneous solution based assay and show that NF-kappa B interacts with karyopherin alpha and that the dual NLS peptide inhibits this interaction. We also show that both L- and D-amino acid containing peptides bind well to karyopherin alpha 2, whereas, the L-amino acid peptides bind more efficiently than the D-amino acid peptide to karyopherin alpha1.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA.
authors.forename: Mark D
authors.initials: MD
authors.lastname: Cunningham
authors.forename: Jeffrey
authors.initials: J
authors.lastname: Cleaveland
authors.forename: Steven G
authors.initials: SG
authors.lastname: Nadler
mesh_terms: D000818:Animals; D019556:COS Cells; D003593:Cytoplasm / Q000187:drug effects; D016503:Drug Delivery Systems; D016328:NF-kappa B / Q000378:metabolism*; D019913:Nuclear Localization Signals / Q000378:metabolism / Q000494:pharmacology*; D021381:Protein Transport; D013050:Spectrometry, Fluorescence; D028901:alpha Karyopherins / Q000187:drug effects* / Q000378:metabolism
chemical_list: C423142:KPNA1 protein, human; D016328:NF-kappa B; D019913:Nuclear Localization Signals; D028901:alpha Karyopherins; C087978:karyopherin alpha 2