Article
CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours.
Nature communications - 17 Feb 2017
Xu Hong, Di Antonio Marco, McKinney Steven, Mathew Veena, Ho Brandon, O'Neil Nigel J, Santos Nancy Dos, Silvester Jennifer, Wei Vivien, Garcia Jessica, Kabeer Farhia, Lai Daniel, Soriano Priscilla, Banáth Judit, Chiu Derek S, Yap Damian, Le Daniel D, Ye Frank B, Zhang Anni, Thu Kelsie, Soong John, Lin Shu-Chuan, Tsai Angela Hsin Chin, Osako Tomo, Algara Teresa, Saunders Darren N, Wong Jason, Xian Jian, Bally Marcel B, Brenton James D, Brown Grant W, Shah Sohrab P, Cescon David, Mak Tak W, Caldas Carlos, Stirling Peter C, Hieter Phil, Balasubramanian Shankar, Aparicio Samuel
Abstract excerpt
G-quadruplex DNAs form four-stranded helical structures and are proposed to play key roles in different cellular processes. Targeting G-quadruplex DNAs for cancer treatment is a very promising prospect. Here, we show that CX-5461 is a G-quadruplex stabilizer, with specific toxicity against BRCA deficiencies in cancer cells and polyclonal patient-derived xenograft models, including tumours resistant to PARP...
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