BibTex format

author = {Xu, H and Di, Antonio M and McKinney, S and Mathew, V and Ho, B and O'Neil, NJ and Dos, Santos N and Silvester, J and Wei, V and Garcia, J and Kabeer, F and Lai, D and Soriano, P and Banath, J and Chiu, DS and Yap, D and Le, DD and Ye, FB and Zhang, A and Thu, K and Soong, J and Lin, S-C and Tsai, AHC and Osako, T and Algara, T and Saunders, DN and Wong, J and Xian, J and Bally, MB and Brenton, JD and Brown, GW and Shah, SP and Cescon, D and Mak, TW and Caldas, C and Stirling, PC and Hieter, P and Balasubramanian, S and Aparicio, S},
doi = {10.1038/ncomms14432},
journal = {Nature Communications},
pages = {1--18},
title = {CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours},
url = {},
volume = {8},
year = {2017}

RIS format (EndNote, RefMan)

AB - 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 inhibition. Exposure to CX-5461, and its related drug CX-3543, blocks replication forks and induces ssDNA gaps or breaks. The BRCA and NHEJ pathways are required for the repair of CX-5461 and CX-3543-induced DNA damage and failure to do so leads to lethality. These data strengthen the concept of G4 targeting as a therapeutic approach, specifically for targeting HR and NHEJ deficient cancers and other tumours deficient for DNA damage repair. CX-5461 is now in advanced phase I clinical trial for patients with BRCA1/2 deficient tumours (Canadian trial, NCT02719977, opened May 2016).
AU - Xu,H
AU - Di,Antonio M
AU - McKinney,S
AU - Mathew,V
AU - Ho,B
AU - O'Neil,NJ
AU - Dos,Santos N
AU - Silvester,J
AU - Wei,V
AU - Garcia,J
AU - Kabeer,F
AU - Lai,D
AU - Soriano,P
AU - Banath,J
AU - Chiu,DS
AU - Yap,D
AU - Le,DD
AU - Ye,FB
AU - Zhang,A
AU - Thu,K
AU - Soong,J
AU - Lin,S-C
AU - Tsai,AHC
AU - Osako,T
AU - Algara,T
AU - Saunders,DN
AU - Wong,J
AU - Xian,J
AU - Bally,MB
AU - Brenton,JD
AU - Brown,GW
AU - Shah,SP
AU - Cescon,D
AU - Mak,TW
AU - Caldas,C
AU - Stirling,PC
AU - Hieter,P
AU - Balasubramanian,S
AU - Aparicio,S
DO - 10.1038/ncomms14432
EP - 18
PY - 2017///
SN - 2041-1723
SP - 1
TI - CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours
T2 - Nature Communications
UR -
UR -
UR -
UR -
VL - 8
ER -