Erratum: Identification of novel RHPS4-derivative ligands with improved toxicological profiles and telomere-targeting activities
نویسندگان
چکیده
Acknowledgements Costs of experiments described within this manuscript were funded by Pharminox Ltd. The costs of the biological experiments were funded by Italian Association for Cancer Research (AIRC#11567 to A.B. and AIRC #14337 to C.L). Dr. A. Rizzo and E. Salvati are recipient of fellowships from the Veronesi Foundation. We wish to thank Dr. I. Hutchinson, Dr. Marc Geoffrey Hummersone, Dr D. Cousin and Dr. M. Frigerio for the synthesis of the new compounds 2–10.
منابع مشابه
Identification of novel RHPS4-derivative ligands with improved toxicological profiles and telomere-targeting activities
The pentacyclic acridinium salt RHPS4 (3,11-difluoro-6,8,13-trimethyl-8H-quino [4,3,2-kl] acridinium methosulfate, compound 1) is one of the most interesting DNA G-quadruplex binding molecules due to its high efficacy in tumor cell growth inhibition both in in vitro models and in vivo against human tumor xenografts in combination with conventional chemotherapeutics. Despite compound 1 having de...
متن کاملBiological activity of the G-quadruplex ligand RHPS4 (3,11-difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate) is associated with telomere capping alteration.
This study had two goals: 1) to evaluate the biological effect of the novel pentacyclic acridine 3,11-difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate (RHPS4) on human melanoma lines possessing long telomeres, and 2) to elucidate the relationship between G-quadruplex-based telomerase inhibitor-induced cellular effects and telomere length/dysfunction. The cellular pharmacologi...
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Functional telomeres are required to maintain the replicative ability of cancer cells and represent putative targets for G-quadruplex (G4) ligands. Here, we show that the pentacyclic acridinium salt RHPS4, one of the most effective and selective G4 ligands, triggers damages in cells traversing S phase by interfering with telomere replication. Indeed, we found that RHPS4 markedly reduced BrdU in...
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Purpose: We previously reported that the G-quadruplex (G4) ligand RHPS4 potentiates the antitumor activity of camptothecins both in vitro and in tumor xenografts. The present study aims at investigating the mechanisms involved in this specific drug interaction. Experimental Design: Combination index test was used to evaluate the interaction between G4 ligands and standard or novel Topo I inhibi...
متن کاملOn and off-target effects of telomere uncapping G-quadruplex selective ligands based on pentacyclic acridinium salts
Quadruplexes DNA are present in telomeric DNA as well as in several cancer-related gene promoters and hence affect gene expression and subsequent biological processes. The conformations of G4 provide selective recognition sites for small molecules and thus these structures have become important drug-design targets for cancer treatment. The DNA G-quadruplex binding pentacyclic acridinium salt RH...
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عنوان ژورنال:
دوره 34 شماره
صفحات -
تاریخ انتشار 2015