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3. Repression of PRMT activities sensitize homologous recombination-proficient ovarian and breast cancer cells to PARP inhibitor treatment

Author

Zhang, Youyou, primary, Xu, Mu, additional, Yuan, Jiao, additional, Hu, Zhongyi, additional, Jiang, Junjie, additional, Huang, Jie, additional, Wang, Bingwei, additional, Shen, Jianfeng, additional, Long, Meixiao, additional, Fan, Yi, additional, Montone, Kathleen T., additional, Tanyi, Janos L., additional, Tavana, Omid, additional, Chan, Ho Man, additional, Hu, Xiaowen, additional, and Zhang, Lin, additional

Published
2024
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4. Table S4 from Large-scale Pan-cancer Cell Line Screening Identifies Actionable and Effective Drug Combinations

Author

Bashi, Azadeh C., primary, Coker, Elizabeth A., primary, Bulusu, Krishna C., primary, Jaaks, Patricia, primary, Crafter, Claire, primary, Lightfoot, Howard, primary, Milo, Marta, primary, McCarten, Katrina, primary, Jenkins, David F., primary, van der Meer, Dieudonne, primary, Lynch, James T., primary, Barthorpe, Syd, primary, Andersen, Courtney L., primary, Barry, Simon T., primary, Beck, Alexandra, primary, Cidado, Justin, primary, Gordon, Jacob A., primary, Hall, Caitlin, primary, Hall, James, primary, Mali, Iman, primary, Mironenko, Tatiana, primary, Mongeon, Kevin, primary, Morris, James, primary, Richardson, Laura, primary, Smith, Paul D., primary, Tavana, Omid, primary, Tolley, Charlotte, primary, Thomas, Frances, primary, Willis, Brandon S., primary, Yang, Wanjuan, primary, O'Connor, Mark J., primary, McDermott, Ultan, primary, Critchlow, Susan E., primary, Drew, Lisa, primary, Fawell, Stephen E., primary, Mettetal, Jerome T., primary, and Garnett, Mathew J., primary

Published
2024
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5. Figure 6 from Large-scale Pan-cancer Cell Line Screening Identifies Actionable and Effective Drug Combinations

Author

Bashi, Azadeh C., primary, Coker, Elizabeth A., primary, Bulusu, Krishna C., primary, Jaaks, Patricia, primary, Crafter, Claire, primary, Lightfoot, Howard, primary, Milo, Marta, primary, McCarten, Katrina, primary, Jenkins, David F., primary, van der Meer, Dieudonne, primary, Lynch, James T., primary, Barthorpe, Syd, primary, Andersen, Courtney L., primary, Barry, Simon T., primary, Beck, Alexandra, primary, Cidado, Justin, primary, Gordon, Jacob A., primary, Hall, Caitlin, primary, Hall, James, primary, Mali, Iman, primary, Mironenko, Tatiana, primary, Mongeon, Kevin, primary, Morris, James, primary, Richardson, Laura, primary, Smith, Paul D., primary, Tavana, Omid, primary, Tolley, Charlotte, primary, Thomas, Frances, primary, Willis, Brandon S., primary, Yang, Wanjuan, primary, O'Connor, Mark J., primary, McDermott, Ultan, primary, Critchlow, Susan E., primary, Drew, Lisa, primary, Fawell, Stephen E., primary, Mettetal, Jerome T., primary, and Garnett, Mathew J., primary

Published
2024
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6. Supplementary Figures S1-S16 from Large-scale Pan-cancer Cell Line Screening Identifies Actionable and Effective Drug Combinations

Author

Bashi, Azadeh C., primary, Coker, Elizabeth A., primary, Bulusu, Krishna C., primary, Jaaks, Patricia, primary, Crafter, Claire, primary, Lightfoot, Howard, primary, Milo, Marta, primary, McCarten, Katrina, primary, Jenkins, David F., primary, van der Meer, Dieudonne, primary, Lynch, James T., primary, Barthorpe, Syd, primary, Andersen, Courtney L., primary, Barry, Simon T., primary, Beck, Alexandra, primary, Cidado, Justin, primary, Gordon, Jacob A., primary, Hall, Caitlin, primary, Hall, James, primary, Mali, Iman, primary, Mironenko, Tatiana, primary, Mongeon, Kevin, primary, Morris, James, primary, Richardson, Laura, primary, Smith, Paul D., primary, Tavana, Omid, primary, Tolley, Charlotte, primary, Thomas, Frances, primary, Willis, Brandon S., primary, Yang, Wanjuan, primary, O'Connor, Mark J., primary, McDermott, Ultan, primary, Critchlow, Susan E., primary, Drew, Lisa, primary, Fawell, Stephen E., primary, Mettetal, Jerome T., primary, and Garnett, Mathew J., primary

Published
2024
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7. Figure 5 from Large-scale Pan-cancer Cell Line Screening Identifies Actionable and Effective Drug Combinations

Author

Bashi, Azadeh C., primary, Coker, Elizabeth A., primary, Bulusu, Krishna C., primary, Jaaks, Patricia, primary, Crafter, Claire, primary, Lightfoot, Howard, primary, Milo, Marta, primary, McCarten, Katrina, primary, Jenkins, David F., primary, van der Meer, Dieudonne, primary, Lynch, James T., primary, Barthorpe, Syd, primary, Andersen, Courtney L., primary, Barry, Simon T., primary, Beck, Alexandra, primary, Cidado, Justin, primary, Gordon, Jacob A., primary, Hall, Caitlin, primary, Hall, James, primary, Mali, Iman, primary, Mironenko, Tatiana, primary, Mongeon, Kevin, primary, Morris, James, primary, Richardson, Laura, primary, Smith, Paul D., primary, Tavana, Omid, primary, Tolley, Charlotte, primary, Thomas, Frances, primary, Willis, Brandon S., primary, Yang, Wanjuan, primary, O'Connor, Mark J., primary, McDermott, Ultan, primary, Critchlow, Susan E., primary, Drew, Lisa, primary, Fawell, Stephen E., primary, Mettetal, Jerome T., primary, and Garnett, Mathew J., primary

Published
2024
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8. Figure 3 from Large-scale Pan-cancer Cell Line Screening Identifies Actionable and Effective Drug Combinations

Author

Bashi, Azadeh C., primary, Coker, Elizabeth A., primary, Bulusu, Krishna C., primary, Jaaks, Patricia, primary, Crafter, Claire, primary, Lightfoot, Howard, primary, Milo, Marta, primary, McCarten, Katrina, primary, Jenkins, David F., primary, van der Meer, Dieudonne, primary, Lynch, James T., primary, Barthorpe, Syd, primary, Andersen, Courtney L., primary, Barry, Simon T., primary, Beck, Alexandra, primary, Cidado, Justin, primary, Gordon, Jacob A., primary, Hall, Caitlin, primary, Hall, James, primary, Mali, Iman, primary, Mironenko, Tatiana, primary, Mongeon, Kevin, primary, Morris, James, primary, Richardson, Laura, primary, Smith, Paul D., primary, Tavana, Omid, primary, Tolley, Charlotte, primary, Thomas, Frances, primary, Willis, Brandon S., primary, Yang, Wanjuan, primary, O'Connor, Mark J., primary, McDermott, Ultan, primary, Critchlow, Susan E., primary, Drew, Lisa, primary, Fawell, Stephen E., primary, Mettetal, Jerome T., primary, and Garnett, Mathew J., primary

Published
2024
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9. Figure 1 from Large-scale Pan-cancer Cell Line Screening Identifies Actionable and Effective Drug Combinations

Author

Bashi, Azadeh C., primary, Coker, Elizabeth A., primary, Bulusu, Krishna C., primary, Jaaks, Patricia, primary, Crafter, Claire, primary, Lightfoot, Howard, primary, Milo, Marta, primary, McCarten, Katrina, primary, Jenkins, David F., primary, van der Meer, Dieudonne, primary, Lynch, James T., primary, Barthorpe, Syd, primary, Andersen, Courtney L., primary, Barry, Simon T., primary, Beck, Alexandra, primary, Cidado, Justin, primary, Gordon, Jacob A., primary, Hall, Caitlin, primary, Hall, James, primary, Mali, Iman, primary, Mironenko, Tatiana, primary, Mongeon, Kevin, primary, Morris, James, primary, Richardson, Laura, primary, Smith, Paul D., primary, Tavana, Omid, primary, Tolley, Charlotte, primary, Thomas, Frances, primary, Willis, Brandon S., primary, Yang, Wanjuan, primary, O'Connor, Mark J., primary, McDermott, Ultan, primary, Critchlow, Susan E., primary, Drew, Lisa, primary, Fawell, Stephen E., primary, Mettetal, Jerome T., primary, and Garnett, Mathew J., primary

Published
2024
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10. Supplementary Tables from Large-scale Pan-cancer Cell Line Screening Identifies Actionable and Effective Drug Combinations

Author

Bashi, Azadeh C., primary, Coker, Elizabeth A., primary, Bulusu, Krishna C., primary, Jaaks, Patricia, primary, Crafter, Claire, primary, Lightfoot, Howard, primary, Milo, Marta, primary, McCarten, Katrina, primary, Jenkins, David F., primary, van der Meer, Dieudonne, primary, Lynch, James T., primary, Barthorpe, Syd, primary, Andersen, Courtney L., primary, Barry, Simon T., primary, Beck, Alexandra, primary, Cidado, Justin, primary, Gordon, Jacob A., primary, Hall, Caitlin, primary, Hall, James, primary, Mali, Iman, primary, Mironenko, Tatiana, primary, Mongeon, Kevin, primary, Morris, James, primary, Richardson, Laura, primary, Smith, Paul D., primary, Tavana, Omid, primary, Tolley, Charlotte, primary, Thomas, Frances, primary, Willis, Brandon S., primary, Yang, Wanjuan, primary, O'Connor, Mark J., primary, McDermott, Ultan, primary, Critchlow, Susan E., primary, Drew, Lisa, primary, Fawell, Stephen E., primary, Mettetal, Jerome T., primary, and Garnett, Mathew J., primary

Published
2024
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11. Figure 4 from Large-scale Pan-cancer Cell Line Screening Identifies Actionable and Effective Drug Combinations

Author

Bashi, Azadeh C., primary, Coker, Elizabeth A., primary, Bulusu, Krishna C., primary, Jaaks, Patricia, primary, Crafter, Claire, primary, Lightfoot, Howard, primary, Milo, Marta, primary, McCarten, Katrina, primary, Jenkins, David F., primary, van der Meer, Dieudonne, primary, Lynch, James T., primary, Barthorpe, Syd, primary, Andersen, Courtney L., primary, Barry, Simon T., primary, Beck, Alexandra, primary, Cidado, Justin, primary, Gordon, Jacob A., primary, Hall, Caitlin, primary, Hall, James, primary, Mali, Iman, primary, Mironenko, Tatiana, primary, Mongeon, Kevin, primary, Morris, James, primary, Richardson, Laura, primary, Smith, Paul D., primary, Tavana, Omid, primary, Tolley, Charlotte, primary, Thomas, Frances, primary, Willis, Brandon S., primary, Yang, Wanjuan, primary, O'Connor, Mark J., primary, McDermott, Ultan, primary, Critchlow, Susan E., primary, Drew, Lisa, primary, Fawell, Stephen E., primary, Mettetal, Jerome T., primary, and Garnett, Mathew J., primary

Published
2024
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12. Data from Large-scale Pan-cancer Cell Line Screening Identifies Actionable and Effective Drug Combinations

Author

Bashi, Azadeh C., primary, Coker, Elizabeth A., primary, Bulusu, Krishna C., primary, Jaaks, Patricia, primary, Crafter, Claire, primary, Lightfoot, Howard, primary, Milo, Marta, primary, McCarten, Katrina, primary, Jenkins, David F., primary, van der Meer, Dieudonne, primary, Lynch, James T., primary, Barthorpe, Syd, primary, Andersen, Courtney L., primary, Barry, Simon T., primary, Beck, Alexandra, primary, Cidado, Justin, primary, Gordon, Jacob A., primary, Hall, Caitlin, primary, Hall, James, primary, Mali, Iman, primary, Mironenko, Tatiana, primary, Mongeon, Kevin, primary, Morris, James, primary, Richardson, Laura, primary, Smith, Paul D., primary, Tavana, Omid, primary, Tolley, Charlotte, primary, Thomas, Frances, primary, Willis, Brandon S., primary, Yang, Wanjuan, primary, O'Connor, Mark J., primary, McDermott, Ultan, primary, Critchlow, Susan E., primary, Drew, Lisa, primary, Fawell, Stephen E., primary, Mettetal, Jerome T., primary, and Garnett, Mathew J., primary

Published
2024
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13. Figure 2 from Large-scale Pan-cancer Cell Line Screening Identifies Actionable and Effective Drug Combinations

Author

Bashi, Azadeh C., primary, Coker, Elizabeth A., primary, Bulusu, Krishna C., primary, Jaaks, Patricia, primary, Crafter, Claire, primary, Lightfoot, Howard, primary, Milo, Marta, primary, McCarten, Katrina, primary, Jenkins, David F., primary, van der Meer, Dieudonne, primary, Lynch, James T., primary, Barthorpe, Syd, primary, Andersen, Courtney L., primary, Barry, Simon T., primary, Beck, Alexandra, primary, Cidado, Justin, primary, Gordon, Jacob A., primary, Hall, Caitlin, primary, Hall, James, primary, Mali, Iman, primary, Mironenko, Tatiana, primary, Mongeon, Kevin, primary, Morris, James, primary, Richardson, Laura, primary, Smith, Paul D., primary, Tavana, Omid, primary, Tolley, Charlotte, primary, Thomas, Frances, primary, Willis, Brandon S., primary, Yang, Wanjuan, primary, O'Connor, Mark J., primary, McDermott, Ultan, primary, Critchlow, Susan E., primary, Drew, Lisa, primary, Fawell, Stephen E., primary, Mettetal, Jerome T., primary, and Garnett, Mathew J., primary

Published
2024
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16. Large-scale Pan-cancer Cell Line Screening Identifies Actionable and Effective Drug Combinations

Author

Bashi, Azadeh C., primary, Coker, Elizabeth A., additional, Bulusu, Krishna C., additional, Jaaks, Patricia, additional, Crafter, Claire, additional, Lightfoot, Howard, additional, Milo, Marta, additional, McCarten, Katrina, additional, Jenkins, David F., additional, van der Meer, Dieudonne, additional, Lynch, James T., additional, Barthorpe, Syd, additional, Andersen, Courtney L., additional, Barry, Simon T., additional, Beck, Alexandra, additional, Cidado, Justin, additional, Gordon, Jacob A., additional, Hall, Caitlin, additional, Hall, James, additional, Mali, Iman, additional, Mironenko, Tatiana, additional, Mongeon, Kevin, additional, Morris, James, additional, Richardson, Laura, additional, Smith, Paul D., additional, Tavana, Omid, additional, Tolley, Charlotte, additional, Thomas, Frances, additional, Willis, Brandon S., additional, Yang, Wanjuan, additional, O'Connor, Mark J., additional, McDermott, Ultan, additional, Critchlow, Susan E., additional, Drew, Lisa, additional, Fawell, Stephen E., additional, Mettetal, Jerome T., additional, and Garnett, Mathew J., additional

Published
2024
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18. NSD2 is a requisite subunit of the AR/FOXA1 neo-enhanceosome in promoting prostate tumorigenesis

Author

Parolia, Abhijit, primary, Eyunni, Sanjana, additional, Verma, Brijesh Kumar, additional, Young, Eleanor, additional, Liu, Lianchao, additional, George, James, additional, Aras, Shweta, additional, Das, Chandan Kanta, additional, Mannan, Rahul, additional, ur Rasool, Reyaz, additional, Luo, Jie, additional, Carson, Sandra E., additional, Mitchell-Velasquez, Erick, additional, Liu, Yihan, additional, Xiao, Lanbo, additional, Gajjala, Prathibha R., additional, Jaber, Mustapha, additional, He, Tongchen, additional, Qiao, Yuanyuan, additional, Pang, Matthew, additional, Zhang, Yuping, additional, Alhusayan, Mohammed, additional, Cao, Xuhong, additional, Tavana, Omid, additional, Hou, Caiyun, additional, Wang, Zhen, additional, Ding, Ke, additional, Chinnaiyan, Arul M., additional, and Asangani, Irfan A., additional

Published
2024
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21. Abstract 5321: Large scale pan cancer drug combination screening to identify effective and actionable combinations and biomarker hypothesis

Author

Bashi, Azadeh, primary, Coker, Elizabeth A., additional, Bulusu, Krishna, additional, Milo, Marta, additional, Crafter, Claire, additional, Lynch, James, additional, Jenkins, David, additional, Lightfoot, Howard, additional, Willis, Brandon, additional, Andersen, Courtney, additional, Tavana, Omid, additional, Mongeon, Kevin, additional, Gordon, Jacob, additional, Smith, Paul, additional, Barry, Simon, additional, McDermott, Ultan, additional, Drew, Lisa, additional, Critchlow, Susan, additional, Garnett, Mathew J., additional, and Mettetal, Jerome, additional

Published
2023
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22. Figure S3 from AZD4320, A Dual Inhibitor of Bcl-2 and Bcl-xL, Induces Tumor Regression in Hematologic Cancer Models without Dose-limiting Thrombocytopenia

Author

Balachander, Srividya B., primary, Criscione, Steven W., primary, Byth, Kate F., primary, Cidado, Justin, primary, Adam, Ammar, primary, Lewis, Paula, primary, Macintyre, Terry, primary, Wen, Shenghua, primary, Lawson, Deborah, primary, Burke, Kathleen, primary, Lubinski, Tristan, primary, Tyner, Jeffrey W., primary, Kurtz, Stephen E., primary, McWeeney, Shannon K., primary, Varnes, Jeffrey, primary, Diebold, R. Bruce, primary, Gero, Thomas, primary, Ioannidis, Stephanos, primary, Hennessy, Edward J., primary, McCoull, William, primary, Saeh, Jamal C., primary, Tabatabai, Areya, primary, Tavana, Omid, primary, Su, Nancy, primary, Schuller, Alwin, primary, Garnett, Mathew J., primary, Jaaks, Patricia, primary, Coker, Elizabeth A., primary, Gregory, Gareth P., primary, Newbold, Andrea, primary, Johnstone, Ricky W., primary, Gangl, Eric, primary, Wild, Martin, primary, Zinda, Michael, primary, Secrist, J. Paul, primary, Davies, Barry R., primary, Fawell, Stephen E., primary, and Gibbons, Francis D., primary

Published
2023
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28. NSD2 is a requisite subunit of the AR/FOXA1 neo-enhanceosome in promoting prostate tumorigenesis

Author

Parolia, Abhijit, Eyunni, Sanjana, Verma, Brijesh Kumar, Young, Eleanor, Liu, Yihan, Liu, Lianchao, George, James, Aras, Shweta, Das, Chandan Kanta, Mannan, Rahul, ur Rasool, Reyaz, Mitchell-Velasquez, Erick, Mahapatra, Somnath, Luo, Jie, Carson, Sandra E., Xiao, Lanbo, Gajjala, Prathibha R., Venkatesh, Sharan, Jaber, Mustapha, Wang, Xiaoju, He, Tongchen, Qiao, Yuanyuan, Pang, Matthew, Zhang, Yuping, Tien, Jean Ching-Yi, Louw, Micheala, Alhusayan, Mohammed, Cao, Xuhong, Su, Fengyun, Tavana, Omid, Hou, Caiyun, Wang, Zhen, Ding, Ke, Chinnaiyan, Arul M., and Asangani, Irfan A.

Abstract

Androgen receptor (AR) is a ligand-responsive transcription factor that drives terminal differentiation of the prostatic luminal epithelia. By contrast, in tumors originating from these cells, AR chromatin occupancy is extensively reprogrammed to activate malignant phenotypes, the molecular mechanisms of which remain unknown. Here, we show that tumor-specific AR enhancers are critically reliant on H3K36 dimethyltransferase activity of NSD2. NSD2 expression is abnormally induced in prostate cancer, where its inactivation impairs AR transactivation potential by disrupting over 65% of its cistrome. NSD2-dependent AR sites distinctively harbor the chimeric FOXA1:AR half-motif, which exclusively comprise tumor-specific AR enhancer circuitries defined from patient specimens. NSD2 inactivation also engenders increased dependency on the NSD1 paralog, and a dual NSD1/2 PROTAC degrader is preferentially cytotoxic in AR-dependent prostate cancer models. Altogether, we characterize NSD2 as an essential AR neo-enhanceosome subunit that enables its oncogenic activity, and position NSD1/2 as viable co-targets in advanced prostate cancer.

Published
2024
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29. HAUSP deubiquitinates and stabilizes N-Myc in neuroblastoma

Author

Tavana, Omid, Li, Dawei, Dai, Chao, Lopez, Gonzalo, Banerjee, Debarshi, Kon, Ning, Chen, Chao, Califano, Andrea, Yamashiro, Darrell J, Sun, Hongbin, and Gu, Wei

Subjects
Ubiquitin -- Research, Proteases -- Research, Neuroblastoma -- Genetic aspects -- Research, Biological sciences, Health
Abstract

Author(s): Omid Tavana [1, 2]; Dawei Li [1, 2]; Chao Dai [1, 2]; Gonzalo Lopez [1, 2, 3, 4]; Debarshi Banerjee [2, 5]; Ning Kon [1, 2]; Chao Chen [6, [...]

Published
2016
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34. Systematic illumination of druggable genes in cancer genomes

Author

Jiang, Junjie, primary, Yuan, Jiao, additional, Hu, Zhongyi, additional, Zhang, Youyou, additional, Zhang, Tianli, additional, Xu, Mu, additional, Long, Meixiao, additional, Fan, Yi, additional, Tanyi, Janos L., additional, Montone, Kathleen T., additional, Tavana, Omid, additional, Vonderheide, Robert H., additional, Chan, Ho Man, additional, Hu, Xiaowen, additional, and Zhang, Lin, additional

Published
2022
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35. Systematic Pan-Cancer Characterization of Nuclear Receptors Identifies Potential Cancer Biomarkers and Therapeutic Targets

Author

Jiang, Junjie, primary, Yuan, Jiao, additional, Hu, Zhongyi, additional, Xu, Mu, additional, Zhang, Youyou, additional, Long, Meixiao, additional, Fan, Yi, additional, Montone, Kathleen T., additional, Tanyi, Janos L., additional, Tavana, Omid, additional, Chan, Ho Man, additional, Zhang, Lin, additional, and Hu, Xiaowen, additional

Published
2022
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36. SETD1B mutations confer apoptosis resistance and BCL2 independence in B cell lymphoma

Author

Portelinha, Ana, Wang, Shenqiu, Parsa, Sara, Jiang, Man, Gorelick, Alexander N., Mohanty, Sagarajit, Sharma, Soumya, de Stanchina, Elisa, Berishaj, Marjan, Zhao, Chunying, Heward, James, Aryal, Neeraj K., Tavana, Omid, Wen, Jiayu, Fitzgibbon, Jude, Dogan, Ahmet, Younes, Anas, Melnick, Ari M., and Wendel, Hans-Guido

Abstract

The translocation t(14;18) activates BCL2 and is considered the initiating genetic lesion in most follicular lymphomas (FL). Surprisingly, FL patients fail to respond to the BCL2 inhibitor, Venetoclax. We show that mutations and deletions affecting the histone lysine methyltransferase SETD1B (KMT2G) occur in 7% of FLs and 16% of diffuse large B cell lymphomas (DLBCL). Deficiency in SETD1B confers striking resistance to Venetoclax and an experimental MCL-1 inhibitor. SETD1B also acts as a tumor suppressor and cooperates with the loss of KMT2D in lymphoma development in vivo. Consistently, loss of SETD1B in human lymphomas typically coincides with loss of KMT2D. Mechanistically, SETD1B is required for the expression of several proapoptotic BCL2 family proteins. Conversely, inhibitors of the KDM5 histone H3K4 demethylases restore BIM and BIK expression and synergize with Venetoclax in SETD1B-deficient lymphomas. These results establish SETD1B as an epigenetic regulator of cell death and reveal a pharmacological strategy to augment Venetoclax sensitivity in lymphoma.

Published
2024
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37. Discovery of PROTAC molecules that selectively degrade the IRAK3 pseudokinase.

Author

Degorce, Sebastien L, Tavana, Omid, Banks, Erica, Crafter, Claire, Gingipalli, Lakshmaiah, Kouvchinov, David, Mao, Yumeng, Pachl, Fiona, Solanki, Anisha, Valge-Archer, Viia, Yang, Bin, Edmondson, Scott, Degorce, Sebastien L, Tavana, Omid, Banks, Erica, Crafter, Claire, Gingipalli, Lakshmaiah, Kouvchinov, David, Mao, Yumeng, Pachl, Fiona, Solanki, Anisha, Valge-Archer, Viia, Yang, Bin, and Edmondson, Scott

Abstract

We report the first disclosure of IRAK3 degraders in the scientific literature. Taking advantage of an opportune by-product obtained during our efforts to identify IRAK4 inhibitors, we identified ready to use, selective IRAK3 ligands in our compound collection with the required properties for conversion into PROTAC degraders. This work culminated with the discovery of PROTAC 23, which we demonstrated to be a potent and selective degrader of IRAK3. 23 induced proteasome-dependent degradation of IRAK3 and required both CRBN and IRAK3 binding for activity. We conclude that PROTAC 23 constitutes an excellent in vitro tool with which to interrogate the biology of IRAK3.

Published
2020
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38. AZD4320, A Dual Inhibitor of Bcl-2 and Bcl-xL, Induces Tumor Regression in Hematologic Cancer Models without Dose-limiting Thrombocytopenia

Author

Balachander, Srividya B., primary, Criscione, Steven W., additional, Byth, Kate F., additional, Cidado, Justin, additional, Adam, Ammar, additional, Lewis, Paula, additional, Macintyre, Terry, additional, Wen, Shenghua, additional, Lawson, Deborah, additional, Burke, Kathleen, additional, Lubinski, Tristan, additional, Tyner, Jeffrey W., additional, Kurtz, Stephen E., additional, McWeeney, Shannon K., additional, Varnes, Jeffrey, additional, Diebold, R. Bruce, additional, Gero, Thomas, additional, Ioannidis, Stephanos, additional, Hennessy, Edward J., additional, McCoull, William, additional, Saeh, Jamal C., additional, Tabatabai, Areya, additional, Tavana, Omid, additional, Su, Nancy, additional, Schuller, Alwin, additional, Garnett, Mathew J., additional, Jaaks, Patricia, additional, Coker, Elizabeth A., additional, Gregory, Gareth P., additional, Newbold, Andrea, additional, Johnstone, Ricky W., additional, Gangl, Eric, additional, Wild, Martin, additional, Zinda, Michael, additional, Secrist, J. Paul, additional, Davies, Barry R., additional, Fawell, Stephen E., additional, and Gibbons, Francis D., additional

Published
2020
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40. Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase

Author

Degorce, Sébastien L., primary, Tavana, Omid, additional, Banks, Erica, additional, Crafter, Claire, additional, Gingipalli, Lakshmaiah, additional, Kouvchinov, David, additional, Mao, Yumeng, additional, Pachl, Fiona, additional, Solanki, Anisha, additional, Valge-Archer, Viia, additional, Yang, Bin, additional, and Edmondson, Scott D., additional

Published
2020
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