Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds
Horton, John R., Liu, Xu, Gale, Molly, Wu, Lizhen, Shanks, John R., Zhang, Xing, Webber, Philip J., Bell, Joshua S.K., Kales, Stephen C., Mott, Bryan T., Rai, Ganesha, Jansen, Daniel J., Henderson, Mark J., Urban, Daniel J., Hall, Matthew D., Simeonov, Anton, Maloney, David J., Johns, Margaret A., Fu, Haian, Jadhav, Ajit, Vertino, Paula M., Yan, Qin, Cheng, Xiaodong
Published in Cell chemical biology (21.07.2016)
Published in Cell chemical biology (21.07.2016)
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KDM5 Histone Demethylase Activity Links Cellular Transcriptomic Heterogeneity to Therapeutic Resistance
Hinohara, Kunihiko, Wu, Hua-Jun, Vigneau, Sébastien, McDonald, Thomas O., Igarashi, Kyomi J., Yamamoto, Kimiyo N., Madsen, Thomas, Fassl, Anne, Egri, Shawn B., Papanastasiou, Malvina, Ding, Lina, Peluffo, Guillermo, Cohen, Ofir, Kales, Stephen C., Lal-Nag, Madhu, Rai, Ganesha, Maloney, David J., Jadhav, Ajit, Simeonov, Anton, Wagle, Nikhil, Brown, Myles, Meissner, Alexander, Sicinski, Piotr, Jaffe, Jacob D., Jeselsohn, Rinath, Gimelbrant, Alexander A., Michor, Franziska, Polyak, Kornelia
Published in Cancer cell (10.12.2018)
Published in Cancer cell (10.12.2018)
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Loss of function Cbl-c mutations in solid tumors
Daniels, Silvano Rakeem, Liyasova, Mariya, Kales, Stephen C, Nau, Marion M, Ryan, Philip E, Green, Jeffrey E, Lipkowitz, Stanley
Published in PloS one (01.07.2019)
Published in PloS one (01.07.2019)
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Revealing β-TrCP activity dynamics in live cells with a genetically encoded biosensor
Paul, Debasish, Kales, Stephen C., Cornwell, James A., Afifi, Marwa M., Rai, Ganesha, Zakharov, Alexey, Simeonov, Anton, Cappell, Steven D.
Published in Nature communications (26.10.2022)
Published in Nature communications (26.10.2022)
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An Enzymatic TMPRSS2 Assay for Assessment of Clinical Candidates and Discovery of Inhibitors as Potential Treatment of COVID-19
Shrimp, Jonathan H, Kales, Stephen C, Sanderson, Philip E, Simeonov, Anton, Shen, Min, Hall, Matthew D
Published in ACS pharmacology & translational science (09.10.2020)
Published in ACS pharmacology & translational science (09.10.2020)
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Cbl and Human Myeloid Neoplasms: The Cbl Oncogene Comes of Age
KALES, Stephen C, RYAN, Philip E, NAU, Marion M, LIPKOWITZ, Stanley
Published in Cancer research (Chicago, Ill.) (15.06.2010)
Published in Cancer research (Chicago, Ill.) (15.06.2010)
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Journal Article
KDM5B Promotes Drug Resistance by Regulating Melanoma-Propagating Cell Subpopulations
Liu, Xiaoni, Zhang, Shang-Min, McGeary, Meaghan K, Krykbaeva, Irina, Lai, Ling, Jansen, Daniel J, Kales, Stephen C, Simeonov, Anton, Hall, Matthew D, Kelly, Daniel P, Bosenberg, Marcus W, Yan, Qin
Published in Molecular cancer therapeutics (01.03.2019)
Published in Molecular cancer therapeutics (01.03.2019)
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Journal Article
CBL is frequently altered in lung cancers: its relationship to mutations in MET and EGFR tyrosine kinases
Tan, Yi-Hung Carol, Krishnaswamy, Soundararajan, Nandi, Suvobroto, Kanteti, Rajani, Vora, Sapana, Onel, Kenan, Hasina, Rifat, Lo, Fang-Yi, El-Hashani, Essam, Cervantes, Gustavo, Robinson, Matthew, Hsu, Han-Shui, Kales, Stephen C, Lipkowitz, Stanley, Karrison, Theodore, Sattler, Martin, Vokes, Everett E, Wang, Yi-Ching, Salgia, Ravi
Published in PloS one (29.01.2010)
Published in PloS one (29.01.2010)
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Journal Article
High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2
Coussens, Nathan P., Kales, Stephen C., Henderson, Mark J., Lee, Olivia W., Horiuchi, Kurumi Y., Wang, Yuren, Chen, Qing, Kuznetsova, Ekaterina, Wu, Jianghong, Chakka, Sirisha, Cheff, Dorian M., Cheng, Ken Chih-Chien, Shinn, Paul, Brimacombe, Kyle R., Shen, Min, Simeonov, Anton, Lal-Nag, Madhu, Ma, Haiching, Jadhav, Ajit, Hall, Matthew D.
Published in The Journal of biological chemistry (31.08.2018)
Published in The Journal of biological chemistry (31.08.2018)
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Journal Article
Immune stimulation of rainbow trout reveals divergent regulation of MH class II-associated invariant chain isoforms
Semple, Shawna L., Heath, George, Christie, Darah, Braunstein, Marsela, Kales, Stephen C., Dixon, Brian
Published in Immunogenetics (New York) (01.05.2019)
Published in Immunogenetics (New York) (01.05.2019)
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Journal Article
Development of a high-throughput dual-stream liquid chromatography-tandem mass spectrometry method to screen for inhibitors of glutamate carboxypeptidase II
Hoxie, Nate, Qiu, Yixuan, Kales, Stephen C, Schneider, Rick, Hu, Xin, Dalal, Anu, Ford-Scheimer, Stephanie L, Wiseman, Robyn, Tsukamoto, Takashi, Wei, Huijun, Slusher, Barbara S, Janiszewski, John S, Hall, Matthew D
Published in Rapid communications in mass spectrometry (12.06.2024)
Published in Rapid communications in mass spectrometry (12.06.2024)
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Journal Article
Enigma prevents Cbl-c-mediated ubiquitination and degradation of RETMEN2A
Kales, Stephen C, Nau, Marion M, Merchant, Anand S, Lipkowitz, Stanley
Published in PloS one (23.01.2014)
Published in PloS one (23.01.2014)
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The AKT modulator A-443654 reduces α-synuclein expression and normalizes ER stress and autophagy
Gandelman, Mandi, Dansithong, Warunee, Kales, Stephen C., Paul, Sharan, Maag, Gentrie, Aoyama, Erika, Zakharov, Alexey, Rai, Ganesha, Dexheimer, Thomas, Whitehill, Brooke M., Sun, Hongmao, Jadhav, Ajit, Simeonov, Anton, Henderson, Mark J., Huynh, Duong P., Pulst, Stefan M., Scoles, Daniel R.
Published in The Journal of biological chemistry (01.10.2021)
Published in The Journal of biological chemistry (01.10.2021)
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A quantitative high-throughput screen identifies compounds that lower expression of the SCA2-and ALS-associated gene ATXN2
Scoles, Daniel R., Gandelman, Mandi, Paul, Sharan, Dexheimer, Thomas, Dansithong, Warunee, Figueroa, Karla P., Pflieger, Lance T., Redlin, Scott, Kales, Stephen C., Sun, Hongmao, Maloney, David, Damoiseaux, Robert, Henderson, Mark J., Simeonov, Anton, Jadhav, Ajit, Pulst, Stefan M.
Published in The Journal of biological chemistry (01.08.2022)
Published in The Journal of biological chemistry (01.08.2022)
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Journal Article
Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A
Horton, John R, Woodcock, Clayton B, Chen, Qin, Liu, Xu, Zhang, Xing, Shanks, John, Rai, Ganesha, Mott, Bryan T, Jansen, Daniel J, Kales, Stephen C, Henderson, Mark J, Cyr, Matthew, Pohida, Katherine, Hu, Xin, Shah, Pranav, Xu, Xin, Jadhav, Ajit, Maloney, David J, Hall, Matthew D, Simeonov, Anton, Fu, Haian, Vertino, Paula M, Cheng, Xiaodong
Published in Journal of medicinal chemistry (13.12.2018)
Published in Journal of medicinal chemistry (13.12.2018)
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Auranofin targets UBA1 and enhances UBA1 activity by facilitating ubiquitin trans-thioesterification to E2 ubiquitin-conjugating enzymes
Yan, Wenjing, Zhong, Yongwang, Hu, Xin, Xu, Tuan, Zhang, Yinghua, Kales, Stephen, Qu, Yanyan, Talley, Daniel C., Baljinnyam, Bolormaa, LeClair, Christopher A., Simeonov, Anton, Polster, Brian M., Huang, Ruili, Ye, Yihong, Rai, Ganesha, Henderson, Mark J., Tao, Dingyin, Fang, Shengyun
Published in Nature communications (09.08.2023)
Published in Nature communications (09.08.2023)
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Journal Article
Balancing Protein Stability and Activity in Cancer: A New Approach for Identifying Driver Mutations Affecting CBL Ubiquitin Ligase Activation
Li, Minghui, Kales, Stephen C, Ma, Ke, Shoemaker, Benjamin A, Crespo-Barreto, Juan, Cangelosi, Andrew L, Lipkowitz, Stanley, Panchenko, Anna R
Published in Cancer research (Chicago, Ill.) (01.02.2016)
Published in Cancer research (Chicago, Ill.) (01.02.2016)
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Journal Article
KDM5 histone demethylases repress immune response via suppression of STING
Wu, Lizhen, Cao, Jian, Cai, Wesley L, Lang, Sabine M, Horton, John R, Jansen, Daniel J, Liu, Zongzhi Z, Chen, Jocelyn F, Zhang, Meiling, Mott, Bryan T, Pohida, Katherine, Rai, Ganesha, Kales, Stephen C, Henderson, Mark J, Hu, Xin, Jadhav, Ajit, Maloney, David J, Simeonov, Anton, Zhu, Shu, Iwasaki, Akiko, Hall, Matthew D, Cheng, Xiaodong, Shadel, Gerald S, Yan, Qin
Published in PLoS biology (06.08.2018)
Published in PLoS biology (06.08.2018)
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Journal Article
Comparative Analysis of Drug-like EP300/CREBBP Acetyltransferase Inhibitors
Crawford, McKenna C., Tripu, Deepika R., Barritt, Samuel A., Jing, Yihang, Gallimore, Diamond, Kales, Stephen C., Bhanu, Natarajan V., Xiong, Ying, Fang, Yuhong, Butler, Kamaria A. T., LeClair, Christopher A., Coussens, Nathan P., Simeonov, Anton, Garcia, Benjamin A., Dibble, Christian C., Meier, Jordan L.
Published in ACS chemical biology (20.10.2023)
Published in ACS chemical biology (20.10.2023)
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Journal Article
KDM5 Histone Demethylase Activity Links Cellular Transcriptomic Heterogeneity to Therapeutic Resistance
Hinohara, Kunihiko, Wu, Hua-Jun, Sébastien Vigneau, McDonald, Thomas O., Igarashi, Kyomi J., Yamamoto, Kimiyo N., Madsen, Thomas, Fassl, Anne, Egri, Shawn B., Papanastasiou, Malvina, Ding, Lina, Peluffo, Guillermo, Cohen, Ofir, Kales, Stephen C., Lal-Nag, Madhu, Rai, Ganesha, Maloney, David J., Jadhav, Ajit, Simeonov, Anton, Wagle, Nikhil, Brown, Myles, Meissner, Alexander, Sicinski, Piotr, Jaffe, Jacob D., Jeselsohn, Rinath, Gimelbrant, Alexander A., Michor, Franziska, Polyak, Kornelia
Published in Cancer cell (11.02.2019)
Published in Cancer cell (11.02.2019)
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