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Items: 1 to 20 of 50

1.
The chemotherapeutic drug CX-5461 is a potent mutagen in cultured human cells
Gene Ching Chiek Koh, Soraya Boushaki, Salome Jingchen Zhao, Andrew Marcel Pregnall, Firas Sadiyah, Cherif Badja, Yasin Memari, Ilias Georgakopoulos-Soares, Serena Nik-Zainal
Nat Genet. 2024; 56(1): 23–26. Published online 2023 Nov 30. doi: 10.1038/s41588-023-01602-9
PMCID:
PMC10786719
AbstractArticlePDF–6.1M
2.
Effects of the G-quadruplex-binding drugs quarfloxin and CX-5461 on the malaria parasite Plasmodium falciparum
Holly M. Craven, Guilherme Nettesheim, Pietro Cicuta, Andrew M. Blagborough, Catherine J. Merrick
Int J Parasitol Drugs Drug Resist. 2023 Dec; 23: 106–119. Published online 2023 Nov 24. doi: 10.1016/j.ijpddr.2023.11.007
PMCID:
PMC10711401
AbstractArticlePDF–3.4M
3.
A G-quadruplex stabilizer, CX-5461 combined with two immune checkpoint inhibitors enhances in vivo therapeutic efficacy by increasing PD-L1 expression in colorectal cancer
Shin-Yi Chung, Yu-Chan Chang, Dennis Shin-Shian Hsu, Ya-Chi Hung, Meng-Lun Lu, Yi-Ping Hung, Nai-Jung Chiang, Chun-Nan Yeh, Michael Hsiao, John Soong, Yeu Su, Ming-Huang Chen
Neoplasia. 2023 Jan; 35: 100856. Published online 2022 Nov 25. doi: 10.1016/j.neo.2022.100856
PMCID:
PMC9709093
AbstractArticlePDF–3.5M
4.
DNA binding preferences of S. cerevisiae RNA polymerase I Core Factor reveal a preference for the GC-minor groove and a conserved binding mechanism
Ashleigh J. Jackobel, Brian J. Zeberl, Danea M. Glover, Aula M. Fakhouri, Bruce A. Knutson
Biochim Biophys Acta Gene Regul Mech. Author manuscript; available in PMC 2022 Nov 28.
Published in final edited form as: Biochim Biophys Acta Gene Regul Mech. 2019 Sep; 1862(9): 194408. Published online 2019 Aug 2. doi: 10.1016/j.bbagrm.2019.194408
PMCID:
PMC9703346
AbstractArticlePDF–2.3M
5.
CX-5461 causes nucleolar compaction, alteration of peri- and intranucleolar chromatin arrangement, an increase in both heterochromatin and DNA damage response
Luc Snyers, Sylvia Laffer, Renate Löhnert, Klara Weipoltshammer, Christian Schöfer
Sci Rep. 2022; 12: 13972. Published online 2022 Aug 17. doi: 10.1038/s41598-022-17923-4
PMCID:
PMC9385865
AbstractArticlePDF–6.1M
6.
Therapeutic efficacy of the novel selective RNA polymerase I inhibitor CX‐5461 on pulmonary arterial hypertension and associated vascular remodelling
Xia Xu, Hua Feng, Chaochao Dai, Weida Lu, Jun Zhang, Xiaosun Guo, Qihui Yin, Jianli Wang, Xiaopei Cui, Fan Jiang
Br J Pharmacol. 2021 Apr; 178(7): 1605–1619. Published online 2021 Mar 1. doi: 10.1111/bph.15385
PMCID:
PMC9328314
AbstractArticlePDF–34M
7.
Results of the phase I CCTG IND.231 trial of CX-5461 in patients with advanced solid tumors enriched for DNA-repair deficiencies
John Hilton, Karen Gelmon, Philippe L. Bedard, Dongsheng Tu, Hong Xu, Anna V. Tinker, Rachel Goodwin, Scott A. Laurie, Derek Jonker, Aaron R. Hansen, Zachary W. Veitch, Daniel J. Renouf, Linda Hagerman, Hongbo Lui, Bingshu Chen, Deb Kellar, Irene Li, Sung-Eun Lee, Takako Kono, Brian Y. C. Cheng, Damian Yap, Daniel Lai, Sean Beatty, John Soong, Kathleen I. Pritchard, Isabel Soria-Bretones, Eric Chen, Harriet Feilotter, Moira Rushton, Lesley Seymour, Samuel Aparicio, David W. Cescon
Nat Commun. 2022; 13: 3607. Published online 2022 Jun 24. doi: 10.1038/s41467-022-31199-2
PMCID:
PMC9232501
AbstractArticlePDF–2.2M
8.
The therapeutic potential of RNA Polymerase I transcription inhibitor, CX-5461, in uterine leiomyosarcoma
Chang-Won Kang, Katherine M. Hannan, Anneke C. Blackburn, Amos H. P. Loh, Kuick Chik Hong, Goh Jian Yuan, Nadine Hein, Denis Drygin, Ross D. Hannan, Lucy A. Coupland
Invest New Drugs. 2022; 40(3): 529–536. Published online 2022 Feb 24. doi: 10.1007/s10637-022-01222-w
PMCID:
PMC9098598
AbstractArticlePDF–3.0M
9.
CX-5461 induces radiosensitization through modification of the DNA damage response and not inhibition of RNA polymerase I
Stacey L. Lehman, Kayla R. Schwartz, Shrankhla Maheshwari, Kevin Camphausen, Philip J. Tofilon
Sci Rep. 2022; 12: 4059. Published online 2022 Mar 8. doi: 10.1038/s41598-022-07928-4
PMCID:
PMC8904802
AbstractArticlePDF–1.2M
10.
p53 induces a survival transcriptional response after nucleolar stress
Han Liao, Anushri Gaur, Claire Mauvais, Catherine Denicourt
Mol Biol Cell. 2021 Oct 1; 32(20): ar3. doi: 10.1091/mbc.E21-05-0251
PMCID:
PMC8684752
AbstractArticlePDF–5.1M
11.
The chemotherapeutic CX-5461 primarily targets TOP2B and exhibits selective activity in high-risk neuroblastoma
Min Pan, William C. Wright, Richard H. Chapple, Asif Zubair, Manbir Sandhu, Jake E. Batchelder, Brandt C. Huddle, Jonathan Low, Kaley B. Blankenship, Yingzhe Wang, Brittney Gordon, Payton Archer, Samuel W. Brady, Sivaraman Natarajan, Matthew J. Posgai, John Schuetz, Darcie Miller, Ravi Kalathur, Siquan Chen, Jon Patrick Connelly, M. Madan Babu, Michael A. Dyer, Shondra M. Pruett-Miller, Burgess B. Freeman, III, Taosheng Chen, Lucy A. Godley, Scott C. Blanchard, Elizabeth Stewart, John Easton, Paul Geeleher
Nat Commun. 2021; 12: 6468. Published online 2021 Nov 9. doi: 10.1038/s41467-021-26640-x
PMCID:
PMC8578635
AbstractArticlePDF–7.1M
12.
Transcription-associated topoisomerase 2α (TOP2A) activity is a major effector of cytotoxicity induced by G-quadruplex ligands
Madeleine Bossaert, Angélique Pipier, Jean-Francois Riou, Céline Noirot, Linh-Trang Nguyên, Remy-Felix Serre, Olivier Bouchez, Eric Defrancq, Patrick Calsou, Sébastien Britton, Dennis Gomez
eLife. 2021; 10: e65184. Published online 2021 Jun 28. doi: 10.7554/eLife.65184
PMCID:
PMC8279764
AbstractArticlePDF–6.1M
13.
CX-5461 Enhances the Efficacy of APR-246 via Induction of DNA Damage and Replication Stress in Triple-Negative Breast Cancer
Ashwini Makhale, Devathri Nanayakkara, Prahlad Raninga, Kum Kum Khanna, Murugan Kalimutho
Int J Mol Sci. 2021 Jun; 22(11): 5782. Published online 2021 May 28. doi: 10.3390/ijms22115782
PMCID:
PMC8198831
AbstractArticlePDF–2.7M
14.
Ubiquitin-mediated DNA damage response is synthetic lethal with G-quadruplex stabilizer CX-5461
Tehmina Masud, Charles Soong, Hong Xu, Justina Biele, Saelin Bjornson, Steven McKinney, Samuel Aparicio
Sci Rep. 2021; 11: 9812. Published online 2021 May 7. doi: 10.1038/s41598-021-88988-w
PMCID:
PMC8105411
AbstractArticlePDF–2.8M
15.
The RNA polymerase I transcription inhibitor CX-5461 cooperates with topoisomerase 1 inhibition by enhancing the DNA damage response in homologous recombination-proficient high-grade serous ovarian cancer
Shunfei Yan, Jiachen Xuan, Natalie Brajanovski, Madeleine R. C. Tancock, Piyush B. Madhamshettiwar, Kaylene J. Simpson, Sarah Ellis, Jian Kang, Carleen Cullinane, Karen E. Sheppard, Katherine M. Hannan, Ross D. Hannan, Elaine Sanij, Richard B. Pearson, Keefe T. Chan
Br J Cancer. 2021 Feb 2; 124(3): 616–627. Published online 2020 Nov 11. doi: 10.1038/s41416-020-01158-z
PMCID:
PMC7851142
AbstractArticlePDF–4.4M
16.
Reprogrammed mRNA translation drives resistance to therapeutic targeting of ribosome biogenesis
Eric P Kusnadi, Anna S Trigos, Carleen Cullinane, David L Goode, Ola Larsson, Jennifer R Devlin, Keefe T Chan, David P De Souza, Malcolm J McConville, Grant A McArthur, George Thomas, Elaine Sanij, Gretchen Poortinga, Ross D Hannan, Katherine M Hannan, Jian Kang, Richard B Pearson
EMBO J. 2020 Nov 2; 39(21): e105111. Published online 2020 Sep 18. doi: 10.15252/embj.2020105111
PMCID:
PMC7604608
AbstractArticlePDF–3.2M
17.
A Multimodal Genotoxic Anticancer Drug Characterized by Pharmacogenetic Analysis in Caenorhabditis elegans
Frank B. Ye, Akil Hamza, Tejomayee Singh, Stephane Flibotte, Philip Hieter, Nigel J. O’Neil
Genetics. 2020 Jul; 215(3): 609–621. Published online 2020 May 15. doi: 10.1534/genetics.120.303169
PMCID:
PMC7337070
AbstractArticlePDF–1.5M
18.
Discovery of novel inhibitors of ribosome biogenesis by innovative high throughput screening strategies
Catherine E. Scull, Yinfeng Zhang, Nichole Tower, Lynn Rasmussen, Indira Padmalayam, Robert Hunter, Ling Zhai, Robert Bostwick, David A. Schneider
Biochem J. Author manuscript; available in PMC 2020 Jun 8.
Published in final edited form as: Biochem J. 2019 Aug 9; 476(15): 2209–2219. Published online 2019 Aug 9. doi: 10.1042/BCJ20190207
PMCID:
PMC7278283
AbstractArticlePDF–511K
19.
CX-5461 activates the DNA damage response and demonstrates therapeutic efficacy in high-grade serous ovarian cancer
Elaine Sanij, Katherine M. Hannan, Jiachen Xuan, Shunfei Yan, Jessica E. Ahern, Anna S. Trigos, Natalie Brajanovski, Jinbae Son, Keefe T. Chan, Olga Kondrashova, Elizabeth Lieschke, Matthew J. Wakefield, Daniel Frank, Sarah Ellis, Carleen Cullinane, Jian Kang, Gretchen Poortinga, Purba Nag, Andrew J. Deans, Kum Kum Khanna, Linda Mileshkin, Grant A. McArthur, John Soong, Els M. J. J. Berns, Ross D. Hannan, Clare L. Scott, Karen E. Sheppard, Richard B. Pearson
Nat Commun. 2020; 11: 2641. Published online 2020 May 26. doi: 10.1038/s41467-020-16393-4
PMCID:
PMC7251123
AbstractArticlePDF–8.5M
20.
The primary mechanism of cytotoxicity of the chemotherapeutic agent CX-5461 is topoisomerase II poisoning
Peter M. Bruno, Mengrou Lu, Kady A. Dennis, Haider Inam, Connor J. Moore, John Sheehe, Stephen J. Elledge, Michael T. Hemann, Justin R. Pritchard
Proc Natl Acad Sci U S A. 2020 Feb 25; 117(8): 4053–4060. Published online 2020 Feb 10. doi: 10.1073/pnas.1921649117
PMCID:
PMC7049172
AbstractArticlePDF–1.0M

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