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Published in Nature chemical biology (01.02.2018)
Published in Nature chemical biology (01.02.2018)
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Published in Cell chemical biology (21.02.2019)
Published in Cell chemical biology (21.02.2019)
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Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands
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Published in Nature chemical biology (01.04.2018)
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CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation
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Allele-Specific Chromatin Recruitment and Therapeutic Vulnerabilities of ESR1 Activating Mutations
Jeselsohn, Rinath, Bergholz, Johann S., Pun, Matthew, Cornwell, MacIntosh, Liu, Weihan, Nardone, Agostina, Xiao, Tengfei, Li, Wei, Qiu, Xintao, Buchwalter, Gilles, Feiglin, Ariel, Abell-Hart, Kayley, Fei, Teng, Rao, Prakash, Long, Henry, Kwiatkowski, Nicholas, Zhang, Tinghu, Gray, Nathanael, Melchers, Diane, Houtman, Rene, Liu, X. Shirley, Cohen, Ofir, Wagle, Nikhil, Winer, Eric P., Zhao, Jean, Brown, Myles
Published in Cancer cell (12.02.2018)
Published in Cancer cell (12.02.2018)
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Covalent disruptor of YAP-TEAD association suppresses defective Hippo signaling
Fan, Mengyang, Lu, Wenchao, Che, Jianwei, Kwiatkowski, Nicholas P, Gao, Yang, Seo, Hyuk-Soo, Ficarro, Scott B, Gokhale, Prafulla C, Liu, Yao, Geffken, Ezekiel A, Lakhani, Jimit, Song, Kijun, Kuljanin, Miljan, Ji, Wenzhi, Jiang, Jie, He, Zhixiang, Tse, Jason, Boghossian, Andrew S, Rees, Matthew G, Ronan, Melissa M, Roth, Jennifer A, Mancias, Joseph D, Marto, Jarrod A, Dhe-Paganon, Sirano, Zhang, Tinghu, Gray, Nathanael S
Published in eLife (27.10.2022)
Published in eLife (27.10.2022)
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Development of CDK2 and CDK5 Dual Degrader TMX‐2172
Teng, Mingxing, Jiang, Jie, He, Zhixiang, Kwiatkowski, Nicholas P., Donovan, Katherine A., Mills, Caitlin E., Victor, Chiara, Hatcher, John M., Fischer, Eric S., Sorger, Peter K., Zhang, Tinghu, Gray, Nathanael S.
Published in Angewandte Chemie International Edition (10.08.2020)
Published in Angewandte Chemie International Edition (10.08.2020)
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Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13
Zeng, Mei, Kwiatkowski, Nicholas P, Zhang, Tinghu, Nabet, Behnam, Xu, Mousheng, Liang, Yanke, Quan, Chunshan, Wang, Jinhua, Hao, Mingfeng, Palakurthi, Sangeetha, Zhou, Shan, Zeng, Qing, Kirschmeier, Paul T, Meghani, Khyati, Leggett, Alan L, Qi, Jun, Shapiro, Geoffrey I, Liu, Joyce F, Matulonis, Ursula A, Lin, Charles Y, Konstantinopoulos, Panagiotis A, Gray, Nathanael S
Published in eLife (13.11.2018)
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Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype
Olson, Calla M, Liang, Yanke, Leggett, Alan, Park, Woojun D, Li, Lianbo, Mills, Caitlin E, Elsarrag, Selma Z, Ficarro, Scott B, Zhang, Tinghu, Düster, Robert, Geyer, Matthias, Sim, Taebo, Marto, Jarrod A, Sorger, Peter K, Westover, Ken D, Lin, Charles Y, Kwiatkowski, Nicholas, Gray, Nathanael S
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QINGSONG LIU, CHUNXIAO XU, ERCAN, Dalia, NIEPEL, Mario, THOREEN, Carson C, KANG, Seong A, PATRICELLI, Matthew P, YUCHUAN WANG, TUPPER, Tanya, ALTABEF, Abigail, KAWAMURA, Hidemasa, HELD, Kathryn D, KIRUBAKARAN, Sivapriya, CHOU, Danny M, ELLEDGE, Stephen J, JANNE, Pasi A, WONG, Kwok-Kin, SABATINI, David M, GRAY, Nathanael S, XIN ZHANG, HUR, Wooyoung, YAN LIU, KWIATKOWSKI, Nicholas P, JINHUA WANG, WESTOVER, Kenneth D, PENG GAO
Published in Cancer research (Chicago, Ill.) (15.04.2013)
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A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification
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Published in Journal of the American Chemical Society (09.01.2019)
Published in Journal of the American Chemical Society (09.01.2019)
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Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma
Jiang, Baishan, Jiang, Jie, Kaltheuner, Ines H., Iniguez, Amanda Balboni, Anand, Kanchan, Ferguson, Fleur M., Ficarro, Scott B., Seong, Bo Kyung Alex, Greifenberg, Ann Katrin, Dust, Sofia, Kwiatkowski, Nicholas P., Marto, Jarrod A., Stegmaier, Kimberly, Zhang, Tinghu, Geyer, Matthias, Gray, Nathanael S.
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Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions
Gao, Yang, Jiang, Baishan, Kim, Hellen, Berberich, Matthew J., Che, Jianwei, Donovan, Katherine A., Hatcher, John M., Huerta, Fidel, Kwiatkowski, Nicholas P., Liu, Yingpeng, Liuni, Peter P., Metivier, Rebecca J., Murali, Vineeth K., Nowak, Radosław P., Zhang, Tinghu, Fischer, Eric S., Gray, Nathanael S., Jones, Lyn H.
Published in Journal of medicinal chemistry (27.04.2023)
Published in Journal of medicinal chemistry (27.04.2023)
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Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13
Liu, Yao, Hao, Mingfeng, Leggett, Alan L, Gao, Yang, Ficarro, Scott B, Che, Jianwei, He, Zhixiang, Olson, Calla M, Marto, Jarrod A, Kwiatkowski, Nicholas P, Zhang, Tinghu, Gray, Nathanael S
Published in Journal of medicinal chemistry (09.07.2020)
Published in Journal of medicinal chemistry (09.07.2020)
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ER Stress Signaling Promotes the Survival of Cancer "Persister Cells" Tolerant to EGFR Tyrosine Kinase Inhibitors
Terai, Hideki, Kitajima, Shunsuke, Potter, Danielle S, Matsui, Yusuke, Quiceno, Laura Gutierrez, Chen, Ting, Kim, Tae-Jung, Rusan, Maria, Thai, Tran C, Piccioni, Federica, Donovan, Katherine A, Kwiatkowski, Nicholas, Hinohara, Kunihiko, Wei, Guo, Gray, Nathanael S, Fischer, Eric S, Wong, Kwok-Kin, Shimamura, Teppei, Letai, Anthony, Hammerman, Peter S, Barbie, David A
Published in Cancer research (Chicago, Ill.) (15.02.2018)
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A kinase-independent role for CDK8 in BCR-ABL1 + leukemia
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Published in Nature communications (18.10.2019)
Published in Nature communications (18.10.2019)
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A Novel HER2-Selective Kinase Inhibitor Is Effective in HER2 Mutant and Amplified Non-Small Cell Lung Cancer
Son, Jieun, Jang, Jaebong, Beyett, Tyler S, Eum, Yoonji, Haikala, Heidi M, Verano, Alyssa, Lin, Mika, Hatcher, John M, Kwiatkowski, Nicholas P, Eser, Pinar Ö, Poitras, Michael J, Wang, Stephen, Xu, Man, Gokhale, Prafulla C, Cameron, Michael D, Eck, Michael J, Gray, Nathanael S, Jänne, Pasi A
Published in Cancer research (Chicago, Ill.) (15.04.2022)
Published in Cancer research (Chicago, Ill.) (15.04.2022)
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Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins
Shirasaki, Ryosuke, Matthews, Geoffrey M., Gandolfi, Sara, de Matos Simoes, Ricardo, Buckley, Dennis L., Raja Vora, Joseline, Sievers, Quinlan L., Brüggenthies, Johanna B., Dashevsky, Olga, Poarch, Haley, Tang, Huihui, Bariteau, Megan A., Sheffer, Michal, Hu, Yiguo, Downey-Kopyscinski, Sondra L., Hengeveld, Paul J., Glassner, Brian J., Dhimolea, Eugen, Ott, Christopher J., Zhang, Tinghu, Kwiatkowski, Nicholas P., Laubach, Jacob P., Schlossman, Robert L., Richardson, Paul G., Culhane, Aedin C., Groen, Richard W.J., Fischer, Eric S., Vazquez, Francisca, Tsherniak, Aviad, Hahn, William C., Levy, Joan, Auclair, Daniel, Licht, Jonathan D., Keats, Jonathan J., Boise, Lawrence H., Ebert, Benjamin L., Bradner, James E., Gray, Nathanael S., Mitsiades, Constantine S.
Published in Cell reports (Cambridge) (05.01.2021)
Published in Cell reports (Cambridge) (05.01.2021)
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THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors
Cayrol, Florencia, Praditsuktavorn, Pannee, Fernando, Tharu M, Kwiatkowski, Nicholas, Marullo, Rosella, Calvo-Vidal, M Nieves, Phillip, Jude, Pera, Benet, Yang, Shao Ning, Takpradit, Kaipol, Roman, Lidia, Gaudiano, Marcello, Crescenzo, Ramona, Ruan, Jia, Inghirami, Giorgio, Zhang, Tinghu, Cremaschi, Graciela, Gray, Nathanael S, Cerchietti, Leandro
Published in Nature communications (30.01.2017)
Published in Nature communications (30.01.2017)
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Chemical genetic strategy identifies histone deacetylase 1 (HDAC1) and HDAC2 as therapeutic targets in sickle cell disease
Bradner, James E., Mak, Raymond, Tanguturi, Shyam K., Mazitschek, Ralph, Haggarty, Stephen J., Ross, Kenneth, Chang, Cindy Y., Bosco, Jocelyn, West, Nathan, Morse, Elizabeth, Lin, Katherine, Shen, John Paul, Kwiatkowski, Nicholas P., Gheldof, Nele, Dekker, Job, DeAngelo, Daniel J., Carr, Steven A., Schreiber, Stuart L., Golub, Todd R., Ebert, Benjamin L.
Published in Proceedings of the National Academy of Sciences - PNAS (13.07.2010)
Published in Proceedings of the National Academy of Sciences - PNAS (13.07.2010)
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