CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours

CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours

Stabilization of DNA quadruplex structures (G4) is lethal for cells with a compromised DNA repair pathway. Here, the authors show that CX-5461, a small molecule in clinical trials as RNA polymerase inhibitor, has G4-stablization properties and can be repurposed to target DNA repair-defective cancers...

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Autores principales: Hong Xu, Marco Di Antonio, Steven McKinney, Veena Mathew, Brandon Ho, Nigel J. O’Neil, Nancy Dos Santos, Jennifer Silvester, Vivien Wei, Jessica Garcia, Farhia Kabeer, Daniel Lai, Priscilla Soriano, Judit Banáth, Derek S. Chiu, Damian Yap, Daniel D. Le, Frank B. Ye, Anni Zhang, Kelsie Thu, John Soong, Shu-chuan Lin, Angela Hsin Chin Tsai, Tomo Osako, Teresa Algara, Darren N. Saunders, Jason Wong, Jian Xian, Marcel B. Bally, James D. Brenton, Grant W. Brown, Sohrab P. Shah, David Cescon, Tak W. Mak, Carlos Caldas, Peter C. Stirling, Phil Hieter, Shankar Balasubramanian, Samuel Aparicio
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2017
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Science
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Acceso en línea:https://doaj.org/article/5b722e62084b4032919682ab16257e1a
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Sumario:Stabilization of DNA quadruplex structures (G4) is lethal for cells with a compromised DNA repair pathway. Here, the authors show that CX-5461, a small molecule in clinical trials as RNA polymerase inhibitor, has G4-stablization properties and can be repurposed to target DNA repair-defective cancers cells.

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