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Recognition and discrimination of DNA quadruplexes by acridine-peptide conjugates

Redman, James Edward ORCID:, Granadino-Roldán, J. M., Schouten, James A., Ladame, Sylvain, Reszka, Anthony P., Neidle, Stephen and Balasubramanian, Shankar 2009. Recognition and discrimination of DNA quadruplexes by acridine-peptide conjugates. Organic & Biomolecular Chemistry 7 (1) , pp. 76-84. 10.1039/b814682a

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We have explored a series of trisubstituted acridine-peptide conjugates for their ability to recognize and discriminate between DNA quadruplexes derived from the human telomere, and the c-kit and N-ras proto-oncogenes. Quadruplex affinity was measured as the peptide sequences were varied, together with their substitution position on the acridine, and the identity of the C-terminus (acid or amide). Surface plasmon resonance measurements revealed that all compounds bound to the human telomeric quadruplex with sub-micromolar affinity. Docking calculations from molecular modelling studies were used to model the effects of substituent orientation and peptide sequence. Modelling and experiment were in agreement that placement of the peptide over the face of the acridine is detrimental to binding affinity. The highest degrees of selectivity were observed towards the N-ras quadruplex by compounds capable of forming simultaneous contacts with their acridine and peptide moieties. The ligands that bound best displayed quadruplex affinities in the 1–5 nM range and at least 10-fold discrimination between the quadruplexes studied

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
R Medicine > R Medicine (General)
Publisher: Royal Society of Chemistry
ISSN: 1477-0520
Last Modified: 18 Oct 2022 12:23

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