Self-assembled Pt2L2 boxes strongly bind G-quadruplex DNA and influence gene expression in cancer cells

O. Domarco; D. Lötsch; J. Schreiber; C. Dinhof; S. Van Schoonhoven; M. D. García; C. Peinador; B. K. Keppler; W. Berger; A. Terenzi

doi:10.1039/C6DT03876J

Self-assembled Pt₂L₂ boxes strongly bind G-quadruplex DNA and influence gene expression in cancer cells†

O. Domarco,^a D. Lötsch,^b J. Schreiber,^b C. Dinhof,^b S. Van Schoonhoven,^b M. D. García,^a C. Peinador,*^a B. K. Keppler,^cd W. Berger^bd and A. Terenzi

*^cd

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^a Universidade da Coruña, Departamento de Química Fundamental and Centro de Investigacións Científicas Avanzadas, Facultade de Ciencias, E-15071 A Coruña, Spain
E-mail: carlos.peinador@udc.es

^b Medical University Vienna, Department of Medicine I, Institute of Cancer Research and Comprehensive Cancer Center, Borschkegasse 8a, A-1090 Vienna, Austria

^c University of Vienna, Institute of Inorganic Chemistry, Waehringerstrasse 42, A-1090 Vienna, Austria

^d Research Platform “Translational Cancer Therapy Research”, University of Vienna and Medical University of Vienna, Vienna, Austria
E-mail: alessio.terenzi@univie.ac.at

Abstract

Supramolecular Pt(II) quadrangular boxes bind native and G-quadruplex DNA motifs in a size-dependent fashion. Three Pt molecular squares of distinct size show biological activity against cancer cells and heavily influence the expression of genes known to form G-quadruplexes in their promoter regions. The smallest Pt-box displays less activity but more selectivity for a quadruplex formed in the c-Kit gene.

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Self-assembled Pt₂L₂ boxes strongly bind G-quadruplex DNA and influence gene expression in cancer cells†

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Self-assembled Pt₂L₂ boxes strongly bind G-quadruplex DNA and influence gene expression in cancer cells

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