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J Med Chem. 2005 Jan 27;48(2):357-9.

Synthesis, characterization, and plasma lipoprotein association of a nucleus-targeted boronated porphyrin.

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  • 1Department of Pharmaceutical Chemistry, University of California, San Francisco, San Francisco, California 94143, USA.


The efficacy of binary cancer therapies such as BNCT and PDT depends critically on the subcellular localization site of the sensitizer. This work presents the synthesis and plasma lipoprotein binding properties of the first reported binary conjugate of a boronated porphyrin with a peptide nuclear localization sequence. The porphyrin-NLS conjugate associates in vitro predominantly with low density lipoproteins. Such association provides a potentially selective entry pathway into malignant cells that overexpress the LDL receptor.

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