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
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Publicado: Nature Portfolio 2017
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Acceso en línea:https://doaj.org/article/5b722e62084b4032919682ab16257e1a
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spelling oai:doaj.org-article:5b722e62084b4032919682ab16257e1a2021-12-02T15:37:04ZCX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours10.1038/ncomms144322041-1723https://doaj.org/article/5b722e62084b4032919682ab16257e1a2017-02-01T00:00:00Zhttps://doi.org/10.1038/ncomms14432https://doaj.org/toc/2041-1723Stabilization 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.Hong XuMarco Di AntonioSteven McKinneyVeena MathewBrandon HoNigel J. O’NeilNancy Dos SantosJennifer SilvesterVivien WeiJessica GarciaFarhia KabeerDaniel LaiPriscilla SorianoJudit BanáthDerek S. ChiuDamian YapDaniel D. LeFrank B. YeAnni ZhangKelsie ThuJohn SoongShu-chuan LinAngela Hsin Chin TsaiTomo OsakoTeresa AlgaraDarren N. SaundersJason WongJian XianMarcel B. BallyJames D. BrentonGrant W. BrownSohrab P. ShahDavid CesconTak W. MakCarlos CaldasPeter C. StirlingPhil HieterShankar BalasubramanianSamuel AparicioNature PortfolioarticleScienceQENNature Communications, Vol 8, Iss 1, Pp 1-18 (2017)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
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
CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours
description 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.
format article
author 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
author_facet 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
author_sort Hong Xu
title CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours
title_short CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours
title_full CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours
title_fullStr CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours
title_full_unstemmed CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours
title_sort cx-5461 is a dna g-quadruplex stabilizer with selective lethality in brca1/2 deficient tumours
publisher Nature Portfolio
publishDate 2017
url https://doaj.org/article/5b722e62084b4032919682ab16257e1a
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