Oxazole-based peptide macrocycles: a new class of G-quadruplex binding ligands |
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Authors: | Jantos Katja Rodriguez Raphaël Ladame Sylvain Shirude Pravin S Balasubramanian Shankar |
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Affiliation: | The University Chemical Laboratory, University of Cambridge, UK. |
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Abstract: | Herein we report on the synthesis and DNA binding properties of a new class of water soluble oxazole-based peptide macrocycles that bind selectively to quadruplex DNA, with no detectable binding to duplex DNA. We have recently identified one quadruplex in the proto-oncogene c-kit that is suspected to act as a regulatory element for the expression of the c-kit gene. Here we provide the first example of a ligand binding to and stabilizing the c-kit quadruplex. Moreover, we show that these macrocycles show a preference for the c-kit quadruplex as compared to the human telomeric quadruplex. |
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