2025

Tjeerdsma, R. B., Ng, T. F., Roorda, M., Bianchi, D., Yang, S., Bonnet, C., ... & van Vugt, M. A. (2025). WEE1 inhibitors trigger GCN2-mediated activation of the integrated stress response. bioRxiv, 2025-03.
https://www.biorxiv.org/content/10.1101/2025.03.12.642754v2.full
* AZD1775, A92, AZD7762, VE822, Palcociclib from Axon Medchem

Bertolin, A. P., Canal, B., Yekezare, M., Early, A., Zeng, J., Instrell, R., ... & Diffley, J. F. (2025). The DNA replication checkpoint prevents PCNA/RFC depletion to protect forks from HLTF-induced collapse in human cells. Molecular Cell.
https://www.cell.com/molecular-cell/fulltext/S1097-2765(25)00502-7
* AZD7762, XL-413, MK8776 from Axon Medchem

2024

Chiappa, M., Guffanti, F., Grasselli, C., Panini, N., Corbelli, A., Fiordaliso, F., & Damia, G. (2024). Different patterns of platinum resistance in ovarian cancer cells with homologous recombination proficient and deficient background. International Journal of Molecular Sciences, 25(5), 3049.
https://www.mdpi.com/1422-0067/25/5/3049
* AZD7792 and AZD1775 from Axon Medchem

Bertolin, A. P., Canal, B., Yekezare, M., Zeng, J., Instrell, R., Howell, M., & Diffley, J. F. (2024). The mechanism of checkpoint-dependent DNA replication fork stabilization in human cells. bioRxiv, 2024-11.
https://www.biorxiv.org/content/10.1101/2024.11.01.621514v1.full
* AZD7762 and MK8776 from Axon Medchem

2023

Liu, X. M., Chen, F., Zhang, F., & Zhao, J. Z. (2023). Chk1/2 inhibitor AZD7762 blocks the growth of preantral follicles by inducing apoptosis, suppressing proliferation, and interfering with the cell cycle in granulosa cells.
https://www.hh.um.es/pdf/Vol_38/38_7/Liu-38-779-786-2023.pdf

Zeng, J. (2023). Cyclin E-Induced Replication Stress Drives p53-dependent Mitotic Bypass and Whole Genome Duplication (Doctoral dissertation, UCL (University College London)).
https://discovery.ucl.ac.uk/id/eprint/10176590/3/Zeng_10176590_Thesis_corrected.pdf
* AZD7792 and MK1175 from Axon Medchem

Zeng, J., Hills, S. A., Ozono, E., & Diffley, J. F. (2023). Cyclin E-induced replicative stress drives p53-dependent whole-genome duplication. Cell, 186(3), 528-542.
https://www.sciencedirect.com/science/article/pii/S0092867422015793
* AZD7792 and MK1175 from Axon Medchem

2022

Liu, X. M., Chen, F., Zhang, F., & Zhao, J. Z. (2022). Chk1/2 inhibitor AZD7762 blocks the growth of preantral follicles by inducing apoptosis, suppressing proliferation, and interfering with the cell cycle in granulosa cells.
https://assets.researchsquare.com/files/rs-1275321/v1/e666ba6f-29be-4b36-87cc-7587b28be8c1.pdf

Chiappa, M., Guffanti, F., Anselmi, M., Lupi, M., Panini, N., Wiesmüller, L., & Damia, G. (2022). Combinations of ATR, Chk1 and Wee1 inhibitors with olaparib are active in olaparib-resistant Brca1 proficient and deficient murine ovarian cells. Cancers, 14(7), 1807.
https://www.mdpi.com/2072-6694/14/7/1807
* AZD7762, ADZ1775, KU55939 and AZD6738 from Axon Medchem

2021

Liu, X. M., Chen, F., Wang, L., Zhang, F., & Huo, L. J. (2021). Checkpoint kinases are required for oocyte meiotic progression by the maintenance of normal spindle structure and chromosome condensation. Experimental Cell Research, 405(2), 112657.
https://www.sciencedirect.com/science/article/pii/S0014482721001890

2018

Restelli, V., Lupi, M., Vagni, M., Chilà, R., Bertoni, F., Damia, G., & Carrassa, L. (2018). Combining Ibrutinib with Chk1 Inhibitors Synergistically Targets Mantle Cell Lymphoma Cell Lines. Targeted Oncology, 13(2), 235-245.
https://link.springer.com/article/10.1007/s11523-018-0553-6
* AZD7762, PF-0047736 and Ibrutinib from Axon Medchem

He, L., Kulesskiy, E., Saarela, J., Turunen, L., Wennerberg, K., Aittokallio, T., & Tan, J. (2018). Methods for High-throughput Drug Combination Screening and Synergy Scoring. Cancer Systems Biology, 351-398. Methods in Molecular Biology (MIMB, vol. 1711).
https://link.springer.com/protocol/10.1007/978-1-4939-7493-1_17

2017

Díaz-Muñoz, M. D., Kiselev, V. Y., Le Novère, N., Curk, T., Ule, J., & Turner, M. (2017). Tia1-dependent regulation of mRNA subcellular location and translation controls p53 expression in B cells. Nature Communications, 8, 530. doi:10.1038/s41467-017-00454-2
https://www.nature.com/articles/s41467-017-00454-2

2016

Prince, E. W., Balakrishnan, I., Shah, M., Levy, J. M. M., Griesinger, A. M., Alimova, I., ... & Remke, M. (2016). Checkpoint kinase 1 expression is an adverse prognostic marker and therapeutic target in MYC-driven medulloblastoma. Oncotarget, 7(33), 53881.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5288228/

2015

Rocca, C. J., Soares, D. G., Bouzid, H., Henriques, J. A. P., Larsen, A. K., & Escargueil, A. E. (2015). BRCA2 is needed for both repair and cell cycle arrest in mammalian cells exposed to S23906, an anticancer monofunctional DNA binder. Cell Cycle, DOI:10.1080/15384101.2015.1042632.
https://pubmed.ncbi.nlm.nih.gov/25945522/

2014

Agarwal, A. (2014). Novel Role of CHK2 in the Intrinsic and Extrinsic Apoptosis Pathway. PhD Thesis, Washington University in St. Louis.
https://openscholarship.wustl.edu/cgi/viewcontent.cgi?article=2276&context=etd

Bryant, C., Rawlinson, R., & Massey, A. J. (2014). Chk1 Inhibition as a novel therapeutic strategy for treating triple-negative breast and ovarian cancers. BMC Cancer, 14, 570.
https://pubmed.ncbi.nlm.nih.gov/25104095/

Itamochi, H., Nishimura, M., Oumi, N., Kato, M., Oishi, T., Shimada, M., ... & Harada, T. (2014). Checkpoint Kinase Inhibitor AZD7762 Overcomes Cisplatin Resistance in Clear Cell Carcinoma of the Ovary. International Journal of Gynecological Cancer, 24(1), 61-69.
https://pubmed.ncbi.nlm.nih.gov/24362713/

2013

Breindel, J. L., Haskins, J. W., Cowell, E. P., Zhao, M., Nguyen, D. X., & Stern, D. F. (2013). EGF Receptor activates MET through MAP kinases to enhance non-small cell lung carcinoma invasion and brain metastasis. Cancer Research, DOI: 10.1158/0008-5472.CAN-12-3775.
https://pubmed.ncbi.nlm.nih.gov/23794705/

Huh, J., & Piwnica-Worms, H. (2013). CRL4_CDT2 Targets CHK1 for PCNA-Independent Destruction. Molecular and Cellular Biology, 33(2), 213-226. doi: 10.1128/MCB.00847-12.
https://pubmed.ncbi.nlm.nih.gov/23109433/

Palii, S. S., Cui, Y., Innes, C. L., & Paules, R. S. (2013). Dissecting cellular responses to irradiation via targeted disruptions of the ATM-CHK1-PP2A circuit. Cell Cycle, 12(7), 1105-1108.
https://pubmed.ncbi.nlm.nih.gov/23462183/

Williams, T. M., Galbán, S., Li, F., Heist, K. A., Galbán, C. J., Lawrence, T. S., ... & Ross, B. D. (2013). DW-MRI as a Predictive Biomarker of Radiosensitization of GBM through Targeted Inhibition of Checkpoint Kinases. Translational Oncology, 6(2), 133–142. PMCID: PMC3610547.
https://pubmed.ncbi.nlm.nih.gov/23544166/

Booth, L., Cruickshanks, N., Ridder, T., Dai, Y., Grant, S., & Dent, P. (2013). PARP and CHK inhibitors interact to cause DNA damage and cell death in mammary carcinoma cells. Landes Bioscience, 14(5), 458-465.
https://pubmed.ncbi.nlm.nih.gov/23917378/

Origanti, S., Cai, S., Munir, A. Z., White, L. S., & Piwnica-Worms, H. (2013). Synthetic lethality of Chk1 inhibition combined with p53 and/or p21 loss during a DNA damage response in normal and tumor cells. Oncogene, 32, 577-588; doi: 10.1038/onc.2012.84.
https://pubmed.ncbi.nlm.nih.gov/22430210/

Pemovska, T., Kontro, M., Yadav, B., Edgren, H., Eldfors, S., Szwajda, A., ... & Wennerberg, K. (2013). Individualized Systems Medicine (ISM) strategy to tailor treatments for patients with chemorefractory acute myeloid leukemia. Cancer Discovery, DOI: 10.1158/2159-8290.CD-13-0350.
https://pubmed.ncbi.nlm.nih.gov/24056683/

2012

Ricci, F., Bernasconi, S., Perego, P., Ganzinelli, M., Russo, G., Bono, F., ... & Damia, G. (2012). Ovarian carcinoma tumor-initiating cells have a mesenchymal phenotype. Cell Cycle, 11(10), 1966-1976.
https://pubmed.ncbi.nlm.nih.gov/22544328/

Bartucci, M., Svensson, S., Romania, P., Dattilo, R., Patrizii, M., Signore, M., ... & De Maria, R. (2012). Therapeutic targeting of Chk1 in NSCLC stem cells during chemotherapy. Cell Death & Differentiation, 19, 768–778. DOI:10.1038/cdd.2011.170.
https://pubmed.ncbi.nlm.nih.gov/22117197/

Duxin, J. P., Moore, H. R., Sidorova, J., Karanja, K., Honaker, Y., Dao, B., ... & Stewart, S. A. (2012). Okazaki Fragment Processing-independent Role for Human Dna2 Enzyme during DNA Replication. Journal of Biological Chemistry, 287, 21980-21991. DOI: 10.1074/jbc.M112.359018.
https://pubmed.ncbi.nlm.nih.gov/22570476/

Tang, Y., Hamed, H. A., Poklepovic, A., Dai, Y., Grant, S., & Dent, P. (2012). Poly(ADP-ribose) Polymerase 1 Modulates the Lethality of CHK1 Inhibitors in Mammary Tumors. Molecular Pharmacology, 82(2), 322-332. DOI: 10.1124/mol.112.078907.
https://pubmed.ncbi.nlm.nih.gov/22596349/

Ma, C. X., Cai, S., Li, S., Ryan, C. E., Guo, Z., Schaiff, W. T., ... & Piwnica-Worms, H. (2012). Targeting Chk1 in p53-deficient triple-negative breast cancer is therapeutically beneficial in human-in-mouse tumor models. Journal of Clinical Investigation, 122(4), 1541–1552. doi: 10.1172/JCI58765.
https://pubmed.ncbi.nlm.nih.gov/22446188/

2011

Yang, H., Yoon, S. J., Jin, J., Choi, S. H., Seol, H. J., Lee, J. I., ... & Yoo, H. Y. (2011). Inhibition of checkpoint kinase 1 sensitizes lung cancer brain metastases to radiotherapy. Biochemical and Biophysical Research Communications, 406(1), 53–58.
https://pubmed.ncbi.nlm.nih.gov/21291864/

Lee, J. H., Choy, M. L., Ngo, L., Venta-Perez, G., & Marks, P. A. (2011). Role of checkpoint kinase 1 (Chk1) in the mechanisms of resistance to histone deacetylase inhibitors. PNAS, 108(49), 19629-19634. DOI: 10.1073/pnas.1117544108.
https://pubmed.ncbi.nlm.nih.gov/22106282/

Soares, D. G., Battistella, A., Rocca, C. J., Matuo, R., Henriques, J. A. P., Larsen, A. K., & Escargueil, A. E. (2011). Ataxia telangiectasia mutated- and Rad3-related kinase drives both the early and late DNA-damage response to the monofunctional antitumour alkylator S23906. Biochemical Journal, 437, 63–73.
https://pubmed.ncbi.nlm.nih.gov/21470188/

Höglund, A., Strömvall, K., Li, Y., Forshell, L. P., & Nilsson, J. A. (2011). Chk2 deficiency in Myc-overexpressing lymphoma cells elicits a synergistic lethal response in combination with PARP inhibition. Cell Cycle, 10(20), 3598–3607. DOI: 10.4161/cc.10.20.17887.
https://pubmed.ncbi.nlm.nih.gov/22030621/

Ullah, Z., de Renty, C., & DePamphilis, M. L. (2011). Checkpoint Kinase 1 Prevents Cell Cycle Exit Linked to Terminal Cell Differentiation. Molecular and Cellular Biology, 31(19), 4129–4143. DOI: 10.1128/MCB.05723-11.
https://pubmed.ncbi.nlm.nih.gov/21791608/

2010

Honaker, Y., & Piwnica-Worms, H. (2010). Casein kinase 1 functions as both penultimate and ultimate kinase in regulating Cdc25A destruction. Oncogene, 29, 3324–3334. DOI:10.1038/onc.2010.96.
https://pubmed.ncbi.nlm.nih.gov/20348946/

Mitchell, C., Park, M., Eulitt, P., Yang, C., Yacoub, A., & Dent, P. (2010). Poly(ADP-Ribose) Polymerase 1 Modulates the Lethality of CHK1 Inhibitors in Carcinoma Cells. Molecular Pharmacology, 78(5), 909–917. DOI: 10.1124/mol.110.067199.
https://pubmed.ncbi.nlm.nih.gov/20696794/

Carrassa, L., Montelatici, E., Lazzari, L., Zangrossi, S., Simone, M., Broggini, M., & Damia, G. (2010). Role of Chk1 in the differentiation program of hematopoietic stem cells. Cellular and Molecular Life Sciences, 67(10), 1713–1722. DOI: 10.1007/s00018-010-0274-1.
https://pubmed.ncbi.nlm.nih.gov/20146081/

2009

Wagner, J. M., & Karnitz, L. M. (2009). Cisplatin-induced DNA damage activates replication checkpoint signaling components that differentially affect tumor cell survival. Molecular Pharmacology, 76(1), 208–214. DOI: 10.1124/mol.109.055178.
https://pubmed.ncbi.nlm.nih.gov/19403702/