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A synthetic lethal drug combination mimics glucose deprivation–induced cancer cell death in the presence of glucose

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Therapeutic Strategies for Targeting CDKN2A Loss in Melanoma

Kreuger, I. Z. M., Slieker, R. C., van Groningen, T., & van Doorn, R. (2022) · Journal of Investigative Dermatology · doi:10.1016/j.jid.2022.07.016 · Cited by 106

The story of protein arginine methylation: characterization, regulation, and function

Peng, C., & Wong, C. C. L. (2017) · Expert Review of Proteomics · doi:10.1080/14789450.2017.1275573 · Cited by 96

Phase 1 Study of JNJ-64619178, a Protein Arginine Methyltransferase 5 Inhibitor, in Advanced Solid Tumors

Vieito, M., Moreno, V., Spreafico, A., Braña, I., Wang, J. S.-Z., Preis, M., Hernández‐Guerrero, T., Genta, S., Hansen, A. R., Doger, B., et al. (2023) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-23-0092 · Cited by 105

FGFR2 Extracellular Domain In-Frame Deletions Are Therapeutically Targetable Genomic Alterations That Function as Oncogenic Drivers in Cholangiocarcinoma

Cleary, J. M., Raghavan, S., Wu, Q., Li, Y. Y., Spurr, L. F., Gupta, H. V., Rubinson, D. A., Fetter, I. J., Hornick, J. L., Nowak, J. A., et al. (2021) · Cancer Discovery · doi:10.1158/2159-8290.cd-20-1669 · Cited by 95

Targeting Arginine Methyltransferase PRMT5 for Cancer Therapy: Updated Progress and Novel Strategies

Zheng, J., Li, B., Wu, Y., Wu, X., & Wang, Y. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00250 · Cited by 97

Molecular basis for substrate recruitment to the PRMT5 methylosome

Mulvaney, K. M., Blomquist, C., Acharya, N., Li, R., Ranaghan, M. J., O’Keefe, M., Rodriguez, D. J., Young, M. J., Kesar, D., Pal, D., et al. (2021) · Molecular Cell · doi:10.1016/j.molcel.2021.07.019 · Cited by 93

SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance

Jensen-Pergakes, K., Tatlock, J., Maegley, K. A., McAlpine, I. J., McTigue, M., Xie, T., Dillon, C. P., Wang, Y., Yamazaki, S., Spiegel, N., et al. (2021) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-21-0620 · Cited by 92

PRMT5 in gene regulation and hematologic malignancies

Zhu, F., & Rui, L. (2019) · Genes & Diseases · doi:10.1016/j.gendis.2019.06.002 · Cited by 93

STC2 activates PRMT5 to induce radioresistance through DNA damage repair and ferroptosis pathways in esophageal squamous cell carcinoma

Jiang, K., Yin, X., Zhang, Q., Yin, J., Tang, Q., Xu, M., Wu, L., Shen, Y., Zhou, Z., Yu, H., et al. (2023) · Redox Biology · doi:10.1016/j.redox.2023.102626 · Cited by 95

Enzymatic Transition States and Drug Design

Schramm, V. L. (2018) · Chemical Reviews · doi:10.1021/acs.chemrev.8b00369 · Cited by 93

AMG 193, a Clinical Stage MTA-Cooperative PRMT5 Inhibitor, Drives Antitumor Activity Preclinically and in Patients with MTAP-Deleted Cancers

Belmontes, B., Slemmons, K. K., Su, C., Liu, S., Policheni, A. N., Moriguchi, J., Tan, H. L. E., Xie, F., Aiello, D. A., Yang, Y., et al. (2024) · Cancer Discovery · doi:10.1158/2159-8290.cd-24-0887 · Cited by 99

A synthetic lethal drug combination mimics glucose deprivation–induced cancer cell death in the presence of glucose

Joly, J. H., Delfarah, A., Phung, P. S., Parrish, S., & Graham, N. A. (2019) · Journal of Biological Chemistry · doi:10.1074/jbc.ra119.011471 · Cited by 88

Blocking methionine catabolism induces senescence and confers vulnerability to GSK3 inhibition in liver cancer

Li, F., Liu, P., Mi, W., Li, L., Anderson, N. M., Lesner, N. P., Burrows, M., Plesset, J. B., Majer, A. D., Wang, G., et al. (2024) · Nature Cancer · doi:10.1038/s43018-023-00671-3 · Cited by 92

Discovery of TNG908: A Selective, Brain Penetrant, MTA-Cooperative PRMT5 Inhibitor That Is Synthetically Lethal with MTAP -Deleted Cancers

Cottrell, K. M., Briggs, K. J., Whittington, D. A., Jahić, H., Ali, J. A., Davis, C. B., Gong, S., Gotur, D., Gu, L., McCarren, P. R., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c00133 · Cited by 91

Metabolite sensing and signaling in cancer

Wang, Y.-P., Li, J., Qu, J., Yin, M., & Lei, Q. (2020) · Journal of Biological Chemistry · doi:10.1074/jbc.rev119.007624 · Cited by 87

MTAP deficiency creates an exploitable target for antifolate therapy in 9p21-loss cancers

Alhalabi, O., Chen, J., Zhang, Y., Lü, Y., Wang, Q., Ramachandran, S., Tidwell, R. S. S., Han, G., Yan, X., Meng, J., et al. (2022) · Nature Communications · doi:10.1038/s41467-022-29397-z · Cited by 83

Loss of MAT2A compromises methionine metabolism and represents a vulnerability in H3K27M mutant glioma by modulating the epigenome

Golbourn, B. J., Halbert, M. E., Halligan, K. E., Varadharajan, S., Krug, B., Mbah, N. E., Kabir, N., Stanton, A.-C. J., Locke, A. L., Casillo, S. M., et al. (2022) · Nature Cancer · doi:10.1038/s43018-022-00348-3 · Cited by 80

Protein arginine methyltransferase 5: A novel therapeutic target for triple‐negative breast cancers

Vinet, M., Suresh, S., Maire, V., Monchecourt, C., Némati, F., Lesage, L., Pierre, F., Ye, M., Lescure, A., Brisson, A., et al. (2019) · Cancer Medicine · doi:10.1002/cam4.2114 · Cited by 79

Synthetic lethal strategies for the development of cancer therapeutics

Ngoi, N. Y. L., Gallo, D., Torrado, C., Nardo, M., Durocher, D., & Yap, T. A. (2024) · Nature Reviews Clinical Oncology · doi:10.1038/s41571-024-00966-z · Cited by 81

ERG signaling in prostate cancer is driven through PRMT5-dependent methylation of the Androgen Receptor

Mounir, Z., Korn, J. M., Westerling, T., Lin, F., Kirby, C. A., Schirle, M., McAllister, G., Hoffman, G., Ramadan, N., Hartung, A., et al. (2016) · eLife · doi:10.7554/elife.13964 · Cited by 80

New Horizons of Synthetic Lethality in Cancer: Current Development and Future Perspectives

Previtali, V., Bagnolini, G., Ciamarone, A., Ferrandi, G., Rinaldi, F., Myers, S. H., Roberti, M., & Cavalli, A. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c00113 · Cited by 84

A Ubiquitination Cascade Regulating the Integrated Stress Response and Survival in Carcinomas

Cervia, L. D., Shibue, T., Borah, A. A., Gaeta, B., He, L., Leung, L., Li, N., Moyer, S. M., Shim, B. H., Dumont, N., et al. (2022) · Cancer Discovery · doi:10.1158/2159-8290.cd-22-1230 · Cited by 77

Targeting Histone Methylation in Cancer

McCabe, M. T., Mohammad, H. P., Barbash, O., & Kruger, R. G. (2017) · The Cancer Journal · doi:10.1097/ppo.0000000000000283 · Cited by 76

Abstract LB-017: Disordered methionine metabolism in MTAP/CDKN2A-deleted cancers leads to marked dependence on PRMT5

Mavrakis, K. J., McDonald, E. R., Schlabach, M. R., Billy, É., Hoffman, G. R., de Weck, A., Ruddy, D. A., Venkatesan, K., McAllister, G., deBeaumont, R. S., et al. (2016) · Cancer Research · doi:10.1158/1538-7445.am2016-lb-017 · Cited by 3

Methylthioadenosine phosphorylase deficiency in tumors: A compelling therapeutic target

Fan, N., Zhang, Y., & Zou, S. (2023) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2023.1173356 · Cited by 42

Abstract LB-307: MTAP deletions in cancer create vulnerability to a MAT2A/PRMT5/RIOK1 axis

Marks, K. M. (2016) · Cancer Research · doi:10.1158/1538-7445.am2016-lb-307

MTAP deletion confers enhanced dependency on the PRMT5 arginine methyltransferase in cancer cells

Kryukov, G. V., Wilson, F. H., Ruth, J. R., Paulk, J., Tsherniak, A., Marlow, S. E., Vazquez, F., Weir, B. A., Fitzgerald, M. E., Tanaka, M., et al. (2016) · Science · doi:10.1126/science.aad5214 · Cited by 688

544 DNA methylation: an epigenetic pathway to cancer and a promising target for anticancer therapy in breast cancer

Martinez-Galán, J., Delgado, J. R., Ávila, R. D. M., Torres, B. T., Núñez, M., Valdivia, J., Luque, R., Peñalver, J., Ríos-Arrabal, S., & de Almodóvar, M. R. (2010) · European Journal of Cancer Supplements · doi:10.1016/s1359-6349(10)72251-5 · Cited by 1