PEPTIDE CONJUGATE USEFUL FOR CELL NUCLEUS MOLECULAR IMAGING AND TUMOR THERAPY

摘要

Described is a conjugate comprising (a) an amphiphilic transport peptide of human origin as a transmembrane module (TPU), (b) a nuclear localization sequence (NLS) and (c) a signalling and/or drug carrying module (SM), preferably comprising Gd, Ga, Fe, Mn, I and/or F as (diagnostic) image creating compound. Said conjugate is' useful for diagnostic purposes, e.g., for cell tracking by MRI, as a contrast agent (e.g., replacing a "biopsy clip") for MRI, or for determining the activity of DNA repair enzymes by MRI. Said conjugate is also useful for therapy, e.g., for chemotherapy or intranuclear Gadolinium Neutron Capture Therapy (GNCT). The transmembrane module (TPU) is selected among peptides of human origin, whose amino acid sequences are similar to the sequence of the antennapedia fragment RQIKIWFQNRRMKWKK. In a specific embodiment, TPU is derived from the human homebox protein HOX-B1. The nuclear localization sequence (NLS) is derived from the simian virus 40-T antigen or from a transcription factor.