The DOI matches its Crossref record; 8 of the 8 references it cites were found in a registry or an index.
Structure-based design of selective and potent G quadruplex-mediated telomerase inhibitors
Open accessAbstract
The telomerase enzyme is a potential therapeutic target in many human cancers. A series of potent inhibitors has been designed by computer modeling, which exploit the unique structural features of quadruplex DNA. These 3,6,9-trisubstituted acridine inhibitors are predicted to interact selectively with the human DNA quadruplex structure, as a means of specifically inhibiting the action of human telomerase in extending the length of single-stranded telomeric DNA. The anilino substituent at the 9-position of the acridine chromophore is predicted to lie in a third groove of the quadruplex. Calculated relative binding energies predict enhanced selectivity compared with earlier 3,6-disubstituted compounds, as a result of this substituent. The ranking order of energies is in accord with equilibrium binding constants for quadruplex measured by surface plasmon resonance techniques, which also show reduced duplex binding compared with the disubstituted compounds. The 3,6,9-trisubstututed acridines have potent in vitro inhibitory activity against human telomerase, with EC 50 values of up to 60 nM.
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Cites
Specific Association of Human Telomerase Activity with Immortal Cells and Cancer
Kim, N. W., Piatyszek, M. A., Prowse, K. R., Harley, C. B., West, M. D., Ho, P. L. C., Coviello, G. M., Wright, W. E., Weinrich, S. L., & Shay, J. W. (1994) · Science · doi:10.1126/science.7605428 · Cited by 7,091
Telomeres shorten during ageing of human fibroblasts
Harley, C. B., Futcher, A. B., & Greider, C. W. (1990) · Nature · doi:10.1038/345458a0 · Cited by 5,750
Mammalian Telomeres End in a Large Duplex Loop
Griffith, J. D., Comeau, L., Rosenfield, S., Stansel, R. M., Bianchi, A., Moss, H., & de Lange, T. (1999) · Cell · doi:10.1016/s0092-8674(00)80760-6 · Cited by 2,447
Creation of human tumour cells with defined genetic elements
Hahn, W. C., Counter, C. M., Lundberg, A. S., Beijersbergen, R. L., Brooks, M. W., & Weinberg, R. A. (1999) · Nature · doi:10.1038/22780 · Cited by 2,345
Telomere maintenance by recombination in human cells
Dunham, M. A., Neumann, A. A., Fasching, C. L., & Reddel, R. R. (2000) · Nature Genetics · doi:10.1038/82586 · Cited by 879
Inhibition of Human Telomerase by a G-Quadruplex-Interactive Compound
Sun, D., Thompson, B., Cathers, B. E., Salazar, M., Kerwin, S. M., Trent, J. O., Jenkins, T. C., Neidle, S., & Hurley, L. H. (1997) · Journal of Medicinal Chemistry · doi:10.1021/jm970199z · Cited by 794
Self-citationMcEachern, M. J., Krauskopf, A., & Blackburn, E. H. (2000) · Annual Review of Genetics · doi:10.1146/annurev.genet.34.1.331 · Cited by 716
Herbert, B.-S., Pitts, A. E., Baker, S. I., Hamilton, S. E., Wright, W. E., Shay, J. W., & Corey, D. R. (1999) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.96.25.14276 · Cited by 539
Cited by
Telomere maintenance as a target for anticancer drug discovery
Neidle, S., & Parkinson, G. (2002) · Nature Reviews Drug Discovery · doi:10.1038/nrd793 · Cited by 624
Self-citationBurger, A. M., Dai, F., Schultes, C. M., Reszka, A. P., Moore, M. J., Double, J. A., & Neidle, S. (2005) · Cancer Research · doi:10.1158/0008-5472.can-04-2910 · Cited by 587
Self-citationStructural Basis of DNA Quadruplex Recognition by an Acridine Drug
Campbell, N. H., Parkinson, G. N., Reszka, A. P., & Neidle, S. (2008) · Journal of the American Chemical Society · doi:10.1021/ja8016973 · Cited by 326
Self-citationChemistry in human telomere biology: structure, function and targeting of telomere DNA/RNA
Xu, Y. (2011) · Chemical Society Reviews · doi:10.1039/c0cs00134a · Cited by 323
Metadata
- Authors
- Read, M., Harrison, R. J., Romagnoli, B., Tanious, F. A., Gowan, S. H., Reszka, A. P., Wilson, W. D., Kelland, L. R., & Neidle, S.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2001-04-17
- Volume
- 98
- Issue
- 9
- Pages
- 4844-4849
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2115127516
- Cited by
- 493
- References
- 8
- FWCI
- 6.73
- Type
- journal article
- Language
- en
- Open access
- green
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- Read, M., Harrison, R. J., Romagnoli, B., Tanious, F. A., Gowan, S. H., Reszka, A. P., Wilson, W. D., Kelland, L. R., & Neidle, S. (2001). Structure-based design of selective and potent G quadruplex-mediated telomerase inhibitors. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.081560598
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
