MODIFIED CYCLIC PENTAPEPTIDES FOR TARGETING CXCR4 CHEMOKINE RECEPTOR EXPRESSION

摘要

Several diseases like HIV-1 infection, cancer metastasis, rheumatoid arthritis, and chronic lymphocytic B-cell leukaemia are linked to the CXCR4-chemokine receptor. Antagonising its natural ligand SDF-1α, is a promising way of treating these diseases. Fujii et al. developed the highly affine peptide cyclof-Arg~1-Arg~2-Nal~3-Gly~4D-Tyr~5]. Herein we describe further enhancement towards metabolic stability, oral bioavailability and chemical versatility to attach radiolabels for tumour diagnosis via PET imaging.