| TMS |
Imatinib, daunotubicin, mitoxantrone, vincristine |
Telomere damage |
CHK2, ATM, p21, p27 |
K562, OM9;22 leukaemia cells |
271
|
| TMS |
NSC19630 (WRN helicase inhibitor) |
Stalled replication, DNA damage, cell death |
γH2AX, PCNA |
U2OS |
318
|
| RHSP4 |
Taxol |
Telomere damage, chromosome fusions |
γH2AX/TRF1 |
UXF1138L cells and xenograft |
319
|
| RHPS4 |
Camptothecin (TOP1 inhibitor) then RHPS4 (CI < 0.2), bleomycin (CI ≈ 0.7) |
Apoptosis, tumour growth inhibition |
γH2AX |
M14 melanoma cells, HT29 colon-derived xenograft |
320
|
| RHPS4 |
GPI 15427 (PARP inhibitor) followed by RHPS4, camptothecin |
Telomere damage chromosome aberrations (or PARP1KD sensitisation) |
PARP/telomere colocalisation |
BJ fibroblasts, HT29-derived xenografts |
321
|
| RHPS4 |
SN-38 or ST1484 (TOP1 inhibitors) followed by RHPS4 (CI ≈ 0.1) |
Telomere damage, cell death |
γH2AX, TOP1 accumulation at telomeres |
BJ fibroblasts, HT29 |
322
|
| No synergy with adriamycin and doxorubicin (TOP2a inhibitors) |
| RHSP4 derivates |
SN-38 (CI < 0.5) |
Telomere damage, stalled replication |
γH2AX/TRF1, PCNA |
HT29 |
323
|
| RHPS4 |
Ionising radiation (IR) |
Telomere damage, G2-phase block, chromosomal rearrangements, tumour growth inhibition |
γH2AX and 53BP1/TRF1 colocalisation |
U251MG glioblastoma cells and xenograft |
324 and 325
|
| PDS |
NU7441 (DNA-PK inhibitor) |
Induction of DNA:RNA hybrid structures (R-loops), DNA damage, DSBs and DDR signalling |
γH2AX, 53BP1, ATM, antibody colocalisation: BG4 (G4) and S9.6 (R-loop) |
DNA-PK−/− MO59J vs. DNA-PK+/+ MO59K glioblastoma cells |
309
|
| PDS, FG |
NU7441 (DNA-PK inhibitor) |
DSBs, ATM-dependent DDR |
γH2AX, ATM |
SV40-transformed MRC-5 fibroblasts |
92
|
| PDS, PDSI |
NU7441 (DNA-PK inhibitor) |
DSBs, DDR, apoptosis |
53BP1, RAD51 (or BRCA2−/−) |
HCT116 colon cancer cells |
315
|
| PDS |
MK1775 (WEE1 cell cycle kinase inhibitor) and pimozide (FA repair USP1 inhibitor) |
G4 stabilisation, cell death |
Sensitised to KD of BRCA1&2, POLQ, USP1, TOP1, WEE1 etc.
|
A375 melanoma cells, HT1080 fibrosarcoma cells |
290
|
| PhenDC |
|
G4 stabilisation, cell death |
Sensitised to KD of BRCA1 and TOP1 |
|
|
| PDS, PhenDC |
ME0328 (PARP3 inhibitor), KU0058948 (PARP1 inhibitor) |
Chromosome rearrangements, DSBs, G2-phase block |
γH2AX, 53BP1, G4-binding 1H6 antibody staining, PARP3KO sensitised |
A549 lung adenocarcinoma cells |
114
|
| CX-5461, CX-3543. PDS |
IR, hydroxyurea |
DNA damage |
γH2AX, 53BP1, CHK1/2, RAD51, ATRXKD sensitised |
Murine normal human astrocytes, glioma stem cells |
326
|
| CX-5461 |
BMN-673 (PARP inhibitor) |
Pol1 transcription inhibition, replication stress, DNA damage, G2-phase block, no G4-stabilisation effect |
ATM/ATR, RPA, γH2AX, HR-deficient, BRCA1−/− and MYC−/− cells sensitised |
Ovarian cancer cells and xenografts |
303
|
| EMICORON |
SN-38 then EMICORON; EMICORON then oxaliplatin or 5-FU (all CI < 0.5) |
Telomeric DNA damage |
|
HT29 colon cancer cells and xenografts |
327
|
