Nickols, Nicholas G. and Yang, Fei and Li, Benjamin C. and Marinov, Georgi K. and Said, Jonathan W. and Dervan, Peter B. (2013) Antitumor activity of a pyrrole-imidazole polyamide in three tumor xenograft models. Cancer Research, 73 (8). Art. No. 1130. ISSN 0008-5472. doi:10.1158/1538-7445.AM2013-1130. https://resolver.caltech.edu/CaltechAUTHORS:20140327-150019475
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Abstract
Background: Pyrrole-imidazole polyamides are synthetic minor groove binders with modular sequence recognition. We developed a polyamide that targets the DNA sequence 5’-WGWWCW-3’ (W=A/T). This molecule is cytotoxic in a number of cancer cell lines including LNCaP (prostate cancer), DU145 (prostate cancer), and A549 (lung cancer). Data in cell culture suggests that this molecule interferes with RNA polymerase 2 activity resulting in proteasome-mediated degradation of the RNA Polymerase 2 large subunit, activation of p53 and induction of p53 target genes, and apoptosis. This polyamide demonstrates no detectable DNA damage by alkaline comet assay nor does it induce detectable phosphorylation of YH2A.X, ATM, DNA-PKcs, p53, or Chk2. This polyamide circulates in mice after intravenous and subcutaneous injection in saline vehicle.
| Item Type: | Article | |||||||||
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| Additional Information: | © 2013 American Association for Cancer Research. | |||||||||
| Issue or Number: | 8 | |||||||||
| DOI: | 10.1158/1538-7445.AM2013-1130 | |||||||||
| Record Number: | CaltechAUTHORS:20140327-150019475 | |||||||||
| Persistent URL: | https://resolver.caltech.edu/CaltechAUTHORS:20140327-150019475 | |||||||||
| Official Citation: | Nicholas G. Nickols, Fei Yang, Benjamin C. Li, Georgi K. Marinov, Jonathan W. Said, Peter B. Dervan. Antitumor activity of a pyrrole-imidazole polyamide in three tumor xenograft models. [abstract]. In: Proceedings of the 104th Annual Meeting of the American Association for Cancer Research; 2013 Apr 6-10; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 1130. doi:10.1158/1538-7445.AM2013-1130 | |||||||||
| Usage Policy: | No commercial reproduction, distribution, display or performance rights in this work are provided. | |||||||||
| ID Code: | 44543 | |||||||||
| Collection: | CaltechAUTHORS | |||||||||
| Deposited By: | Ruth Sustaita | |||||||||
| Deposited On: | 28 Mar 2014 23:07 | |||||||||
| Last Modified: | 10 Nov 2021 16:53 |
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