Mechanism of acridine-based telomerase inhibition and telomere shortening. Gunaratnam, M., Greciano, O., Martins, C., Reszka, A. P, Schultes, C. M, Morjani, H., Riou, J., & Neidle, S. Biochemical pharmacology, 74(5):679–89, October, 2007. ![Mechanism of acridine-based telomerase inhibition and telomere shortening. [link]](https://bibbase.org/img/filetypes/link.svg "link")
Paper doi abstract bibtex The trisubstituted acridine compound BRACO-19 has been developed as a ligand for stabilising G-quadruplex structures. It is shown here that BRACO-19 produces short- and long-term growth arrest in cancer cell lines, and is significantly less potent in a normal cell line. BRACO-19 reduces telomerase activity and long-term telomere length attrition is observed. It is also shown that BRACO-19 binds to telomeric single-stranded overhang DNA, consistent with quadruplex formation, and the single-stranded protein hPOT1 has been shown to be displaced from the overhang in vitro and in cellular experiments. It is concluded that the cellular activity of BRACO-19 can be ascribed both to the uncapping of 3' telomere ends and to telomere shortening that may preferentially affect cells with short telomeres.
@article{Gunaratnam2007,
title = {Mechanism of acridine-based telomerase inhibition and telomere shortening.},
volume = {74},
issn = {1873-2968},
url = {http://www.ncbi.nlm.nih.gov/pubmed/17631279},
doi = {10.1016/j.bcp.2007.06.011},
abstract = {The trisubstituted acridine compound BRACO-19 has been developed as a ligand for stabilising G-quadruplex structures. It is shown here that BRACO-19 produces short- and long-term growth arrest in cancer cell lines, and is significantly less potent in a normal cell line. BRACO-19 reduces telomerase activity and long-term telomere length attrition is observed. It is also shown that BRACO-19 binds to telomeric single-stranded overhang DNA, consistent with quadruplex formation, and the single-stranded protein hPOT1 has been shown to be displaced from the overhang in vitro and in cellular experiments. It is concluded that the cellular activity of BRACO-19 can be ascribed both to the uncapping of 3' telomere ends and to telomere shortening that may preferentially affect cells with short telomeres.},
number = {5},
journal = {Biochemical pharmacology},
author = {Gunaratnam, Mekala and Greciano, Olga and Martins, Cristina and Reszka, Anthony P and Schultes, Christoph M and Morjani, Hamid and Riou, Jean-Francois and Neidle, Stephen},
month = oct,
year = {2007},
pmid = {17631279},
keywords = {\#nosource, Acridines, Acridines: chemistry, Acridines: pharmacology, Antineoplastic Agents, Antineoplastic Agents: chemistry, Antineoplastic Agents: pharmacology, Cell Line, Dose-Response Relationship, Drug, Humans, Molecular Structure, Telomerase, Telomerase: antagonists \& inhibitors, Telomere, Telomere: metabolism, g-quadruplex ligands},
pages = {679--89},
}
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