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Donovan, Katherine A., Ferguson, Fleur M., Bushman, Jonathan W., Eleuteri, Nicholas A., Bhunia, Debabrata, Ryu, SeongShick, Tan, Li, Shi, Kun, Yue, Hong, Liu, Xiaoxi, Dobrovolsky, Dennis, Jiang, Baishan, Wang, Jinhua, Hao, Mingfeng, You, Inchul, Teng, Mingxing, Liang, Yanke, Hatcher, John, Li, Zhengnian, Manz, Theresa D., Groendyke, Brian, Hu, Wanyi, Nam, Yunju, Sengupta, Sandip, Cho, Hanna, Shin, Injae, Agius, Michael P., Ghobrial, Irene M., Ma, Michelle W., Che, Jianwei, Buhrlage, Sara J., Sim, Taebo, Gray, Nathanael S., Fischer, Eric S.
Published in Cell (10.12.2020)
Published in Cell (10.12.2020)
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Targeting Pin1 renders pancreatic cancer eradicable by synergizing with immunochemotherapy
Koikawa, Kazuhiro, Kibe, Shin, Suizu, Futoshi, Sekino, Nobufumi, Kim, Nami, Manz, Theresa D., Pinch, Benika J., Akshinthala, Dipikaa, Verma, Ana, Gaglia, Giorgio, Nezu, Yutaka, Ke, Shizhong, Qiu, Chenxi, Ohuchida, Kenoki, Oda, Yoshinao, Lee, Tae Ho, Wegiel, Babara, Clohessy, John G., London, Nir, Santagata, Sandro, Wulf, Gerburg M., Hidalgo, Manuel, Muthuswamy, Senthil K., Nakamura, Masafumi, Gray, Nathanael S., Zhou, Xiao Zhen, Lu, Kun Ping
Published in Cell (02.09.2021)
Published in Cell (02.09.2021)
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Targeting the Dark Lipid Kinase PIP4K2C with a Potent and Selective Binder and Degrader
Teng, Mingxing, Jiang, Jie, Wang, Eric S., Geng, Qixiang, Toenjes, Sean T., Donovan, Katherine A., Mageed, Nada, Yue, Hong, Nowak, Radosław P., Wang, Jinhua, Manz, Theresa D., Fischer, Eric S., Cantley, Lewis C., Gray, Nathanael S.
Published in Angewandte Chemie International Edition (24.04.2023)
Published in Angewandte Chemie International Edition (24.04.2023)
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Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo
Dubiella, Christian, Pinch, Benika J, Koikawa, Kazuhiro, Zaidman, Daniel, Poon, Evon, Manz, Theresa D, Nabet, Behnam, He, Shuning, Resnick, Efrat, Rogel, Adi, Langer, Ellen M, Daniel, Colin J, Seo, Hyuk-Soo, Chen, Ying, Adelmant, Guillaume, Sharifzadeh, Shabnam, Ficarro, Scott B, Jamin, Yann, Martins da Costa, Barbara, Zimmerman, Mark W, Lian, Xiaolan, Kibe, Shin, Kozono, Shingo, Doctor, Zainab M, Browne, Christopher M, Yang, Annan, Stoler-Barak, Liat, Shah, Richa B, Vangos, Nicholas E, Geffken, Ezekiel A, Oren, Roni, Koide, Eriko, Sidi, Samuel, Shulman, Ziv, Wang, Chu, Marto, Jarrod A, Dhe-Paganon, Sirano, Look, Thomas, Zhou, Xiao Zhen, Lu, Kun Ping, Sears, Rosalie C, Chesler, Louis, Gray, Nathanael S, London, Nir
Published in Nature chemical biology (01.09.2021)
Published in Nature chemical biology (01.09.2021)
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Identification of a potent and selective covalent Pin1 inhibitor
Pinch, Benika J, Doctor, Zainab M, Nabet, Behnam, Browne, Christopher M, Seo, Hyuk-Soo, Mohardt, Mikaela L, Kozono, Shingo, Lian, Xiaolan, Manz, Theresa D, Chun, Yujin, Kibe, Shin, Zaidman, Daniel, Daitchman, Dina, Yeoh, Zoe C, Vangos, Nicholas E, Geffken, Ezekiel A, Tan, Li, Ficarro, Scott B, London, Nir, Marto, Jarrod A, Buratowski, Stephen, Dhe-Paganon, Sirano, Zhou, Xiao Zhen, Lu, Kun Ping, Gray, Nathanael S
Published in Nature chemical biology (01.09.2020)
Published in Nature chemical biology (01.09.2020)
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Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors
Sivakumaren, Sindhu Carmen, Shim, Hyeseok, Zhang, Tinghu, Ferguson, Fleur M., Lundquist, Mark R., Browne, Christopher M., Seo, Hyuk-Soo, Paddock, Marcia N., Manz, Theresa D., Jiang, Baishan, Hao, Ming-Feng, Krishnan, Pranav, Wang, Diana G., Yang, T. Jonathan, Kwiatkowski, Nicholas P., Ficarro, Scott B., Cunningham, James M., Marto, Jarrod A., Dhe-Paganon, Sirano, Cantley, Lewis C., Gray, Nathanael S.
Published in Cell chemical biology (21.05.2020)
Published in Cell chemical biology (21.05.2020)
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Development of potent and selective degraders of PI5P4Kγ
Ji, Wenzhi, Wang, Eric S., Manz, Theresa D., Jiang, Jie, Donovan, Katherine A., Abulaiti, Xianmixinuer, Fischer, Eric S., Cantley, Lewis C., Zhang, Tinghu, Gray, Nathanael S.
Published in European journal of medicinal chemistry (05.02.2023)
Published in European journal of medicinal chemistry (05.02.2023)
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Discovery and Structure–Activity Relationship Study of (Z)‑5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5‑Phosphate 4‑Kinase Inhibitors
Manz, Theresa D, Sivakumaren, Sindhu Carmen, Ferguson, Fleur M, Zhang, Tinghu, Yasgar, Adam, Seo, Hyuk-Soo, Ficarro, Scott B, Card, Joseph D, Shim, Hyeseok, Miduturu, Chandrasekhar V, Simeonov, Anton, Shen, Min, Marto, Jarrod A, Dhe-Paganon, Sirano, Hall, Matthew D, Cantley, Lewis C, Gray, Nathanael S
Published in Journal of medicinal chemistry (14.05.2020)
Published in Journal of medicinal chemistry (14.05.2020)
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Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors
Zhang, Tinghu, Kwiatkowski, Nicholas, Olson, Calla M, Dixon-Clarke, Sarah E, Abraham, Brian J, Greifenberg, Ann K, Ficarro, Scott B, Elkins, Jonathan M, Liang, Yanke, Hannett, Nancy M, Manz, Theresa, Hao, Mingfeng, Bartkowiak, Bartlomiej, Greenleaf, Arno L, Marto, Jarrod A, Geyer, Matthias, Bullock, Alex N, Young, Richard A, Gray, Nathanael S
Published in Nature chemical biology (01.10.2016)
Published in Nature chemical biology (01.10.2016)
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Structure–Activity Relationship Study of Covalent Pan-phosphatidylinositol 5‑Phosphate 4‑Kinase Inhibitors
Manz, Theresa D, Sivakumaren, Sindhu C, Yasgar, Adam, Hall, Matthew D, Davis, Mindy I, Seo, Hyuk-Soo, Card, Joseph D, Ficarro, Scott B, Shim, Hyeseok, Marto, Jarrod A, Dhe-Paganon, Sirano, Sasaki, Atsuo T, Boxer, Matthew B, Simeonov, Anton, Cantley, Lewis C, Shen, Min, Zhang, Tinghu, Ferguson, Fleur M, Gray, Nathanael S
Published in ACS medicinal chemistry letters (12.03.2020)
Published in ACS medicinal chemistry letters (12.03.2020)
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Targeting the Dark Lipid Kinase PIP4K2C with a Potent and Selective Binder and Degrader
Teng, Mingxing, Jiang, Jie, Wang, Eric S., Geng, Qixiang, Toenjes, Sean T., Donovan, Katherine A., Mageed, Nada, Yue, Hong, Nowak, Radosław P., Wang, Jinhua, Manz, Theresa D., Fischer, Eric S., Cantley, Lewis C., Gray, Nathanael S.
Published in Angewandte Chemie (24.04.2023)
Published in Angewandte Chemie (24.04.2023)
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Journal Article
Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors
Zhang, Tinghu, Kwiatkowski, Nicholas, Olson, Calla M, Dixon-Clarke, Sarah E, Abraham, Brian J, Greifenberg, Ann K, Ficarro, Scott B, Elkins, Jonathan M, Liang, Yanke, Hannett, Nancy M, Manz, Theresa, Hao, Mingfeng, Bartkowiak, Bartlomiej, Greenleaf, Arno L, Marto, Jarrod A, Geyer, Matthias, Bullock, Alex N, Young, Richard A, Gray, Nathanael S
Published in Nature chemical biology (01.10.2016)
Published in Nature chemical biology (01.10.2016)
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Abstract 2757: Discovery and characterization of covalent Pin1 inhibitors targeted to an active site cysteine
Pinch, Benika, Doctor, Zainab, Browne, Christopher M., Seo, Hyuk-Soo, Nabet, Behnam, Kozono, Shingo, Lian, Xiaolan, Zaidman, Daniel, Daitchman, Dina, London, Nir, Gong, Lu, Manz, Theresa, Chun, Yujin, Tan, Li, Marto, Jarrod, Buratowski, Stephen, Dhe-Paganon, Sirano, Zhou, Xiao, Lu, Kun Ping, Gray, Nathanael S.
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Covalent targeting of remote cysteine residues to develop CDK12 and 13 inhibitors
Zhang, Tinghu, Kwiatkowski, Nicholas, Olson, Calla M, Dixon-Clarke, Sarah E, Abraham, Brian J, Greifenberg, Ann K, Ficarro, Scott B, Elkins, Jonathan M, Liang, Yanke, Hannett, Nancy M, Manz, Theresa, Hao, Mingfeng, Bartkowiak, Bartlomiej, Greenleaf, Arno L, Marto, Jarrod A, Geyer, Matthias, Bullock, Alex N, Young, Richard A, Gray, Nathanael S
Published in Nature chemical biology (29.08.2016)
Published in Nature chemical biology (29.08.2016)
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SMALL MOLECULE DEGRADERS OF PHOSPHATIDYLINOSITOL-5-PHOSPHATE 4-KINASE TYPE 2 AND USES THEREOF
Wang, Eric, Cantley, Lewis C, Gray, Nathanael S, Sivakumaren, Sindhu Carmen, Manz, Theresa, Zhang, Tinghu, Fischer, Eric S, Ji, Wenzhi, Donovan, Katherine
Year of Publication 25.07.2024
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Year of Publication 25.07.2024
Patent
Targeting the PI5P4K lipid kinase family in cancer using novel covalent inhibitors
Sindhu Carmen Sivakumaren, Shim, Hyeseok, Zhang, Tinghu, Ferguson, Fleur M, Lundquist, Mark R, Browne, Christopher M, Hyuk-Soo Seo, Paddock, Marcia N, Manz, Theresa D, Jiang, Baishan, Ming-Feng, Hao, Krishnan, Pranav, Wang, Diana G, Yang, T Jonathan, Kwiatkowski, Nicholas P, Ficarro, Scott B, Cunningham, James M, Marto, Jarrod A, Dhe-Paganon, Sirano, Cantley, Lewis C, Gray, Nathanael S
Published in bioRxiv (25.10.2019)
Published in bioRxiv (25.10.2019)
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Paper
Sulfopin, a selective covalent inhibitor of Pin1, blocks Myc-driven tumor initiation and growth in vivo
Dubiella, Christian, Pinch, Benika J, Zaidman, Daniel, Manz, Theresa D, Poon, Evon, He, Shuning, Resnick, Efrat, Langer, Ellen M, Daniel, Colin J, Hyuk-Soo Seo, Chen, Ying, Ficarro, Scott B, Jamin, Yann, Lian, Xiaolan, Kibe, Shin, Kozono, Shingo, Koikawa, Kazuhiro, Doctor, Zainab M, Nabet, Behnam, Browne, Christopher M, Annan Yang, Stoler-Barak, Liat, Shah, Richa B, Vangos, Nicholas E, Geffken, Ezekiel A, Oren, Roni, Sidi, Samuel, Shulman, Ziv, Chu, Wang, Marto, Jarrod A, Dhe-Paganon, Sirano, Look, Thomas, Zhou, Xiao Zhen, Lu, Kun Ping, Sears, Rosalie C, Chesler, Louis, Gray, Nathanael S, London, Nir
Published in bioRxiv (21.03.2020)
Published in bioRxiv (21.03.2020)
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Paper