Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket
Forster, Michael, Chaikuad, Apirat, Bauer, Silke M., Holstein, Julia, Robers, Matthew B., Corona, Cesear R., Gehringer, Matthias, Pfaffenrot, Ellen, Ghoreschi, Kamran, Knapp, Stefan, Laufer, Stefan A.
Published in Cell chemical biology (17.11.2016)
Published in Cell chemical biology (17.11.2016)
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Quantifying CDK inhibitor selectivity in live cells
Wells, Carrow I., Vasta, James D., Corona, Cesear R., Wilkinson, Jennifer, Zimprich, Chad A., Ingold, Morgan R., Pickett, Julie E., Drewry, David H., Pugh, Kathryn M., Schwinn, Marie K., Hwang, Byounghoon (Brian), Zegzouti, Hicham, Huber, Kilian V. M., Cong, Mei, Meisenheimer, Poncho L., Willson, Timothy M., Robers, Matthew B.
Published in Nature communications (02.06.2020)
Published in Nature communications (02.06.2020)
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A Toolbox for the Generation of Chemical Probes for Baculovirus IAP Repeat Containing Proteins
Schwalm, Martin P., Berger, Lena M., Meuter, Maximilian N., Vasta, James D., Corona, Cesear R., Röhm, Sandra, Berger, Benedict-Tilman, Farges, Frederic, Beinert, Sebastian M., Preuss, Franziska, Morasch, Viktoria, Rogov, Vladimir V., Mathea, Sebastian, Saxena, Krishna, Robers, Matthew B., Müller, Susanne, Knapp, Stefan
Published in Frontiers in cell and developmental biology (26.05.2022)
Published in Frontiers in cell and developmental biology (26.05.2022)
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Quantitative Live-Cell Kinetic Degradation and Mechanistic Profiling of PROTAC Mode of Action
Riching, Kristin M, Mahan, Sarah, Corona, Cesear R, McDougall, Mark, Vasta, James D, Robers, Matthew B, Urh, Marjeta, Daniels, Danette L
Published in ACS chemical biology (21.09.2018)
Published in ACS chemical biology (21.09.2018)
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KRAS is vulnerable to reversible switch-II pocket engagement in cells
Vasta, James D., Peacock, D. Matthew, Zheng, Qinheng, Walker, Joel A., Zhang, Ziyang, Zimprich, Chad A., Thomas, Morgan R., Beck, Michael T., Binkowski, Brock F., Corona, Cesear R., Robers, Matthew B., Shokat, Kevan M.
Published in Nature chemical biology (01.06.2022)
Published in Nature chemical biology (01.06.2022)
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Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement
Vasta, James D., Corona, Cesear R., Wilkinson, Jennifer, Zimprich, Chad A., Hartnett, James R., Ingold, Morgan R., Zimmerman, Kristopher, Machleidt, Thomas, Kirkland, Thomas A., Huwiler, Kristin G., Ohana, Rachel Friedman, Slater, Michael, Otto, Paul, Cong, Mei, Wells, Carrow I., Berger, Benedict-Tilman, Hanke, Thomas, Glas, Carina, Ding, Ke, Drewry, David H., Huber, Kilian V.M., Willson, Timothy M., Knapp, Stefan, Müller, Susanne, Meisenheimer, Poncho L., Fan, Frank, Wood, Keith V., Robers, Matthew B.
Published in Cell chemical biology (15.02.2018)
Published in Cell chemical biology (15.02.2018)
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DELs enable the development of BRET probes for target engagement studies in cells
Teske, Kelly A, Su, Wenji, Corona, Cesear R, Wen, Jing, Deng, Jason, Ping, Yan, Zhang, Zaihong, Zhang, Qi, Wilkinson, Jennifer, Beck, Michael T, Nealey, Kendra R, Vasta, James D, Cong, Mei, Meisenheimer, Poncho L, Kuai, Letian, Robers, Matthew B
Published in Cell chemical biology (17.08.2023)
Published in Cell chemical biology (17.08.2023)
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Design of a “Two-in-One” Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites
Wittlinger, Florian, Heppner, David E, To, Ciric, Günther, Marcel, Shin, Bo Hee, Rana, Jaimin K, Schmoker, Anna M, Beyett, Tyler S, Berger, Lena M, Berger, Benedict-Tilman, Bauer, Nicolas, Vasta, James D, Corona, Cesear R, Robers, Matthew B, Knapp, Stefan, Jänne, Pasi A, Eck, Michael J, Laufer, Stefan A
Published in Journal of medicinal chemistry (27.01.2022)
Published in Journal of medicinal chemistry (27.01.2022)
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Journal Article
Small-molecule inhibition of the archetypal UbiB protein COQ8
Murray, Nathan H., Asquith, Christopher R. M., Fang, Zixiang, East, Michael P., Ptak, Naomi, Smith, Robert W., Vasta, James D., Zimprich, Chad A., Corona, Cesear R., Robers, Matthew B., Johnson, Gary L., Bingman, Craig A., Pagliarini, David J.
Published in Nature chemical biology (01.02.2023)
Published in Nature chemical biology (01.02.2023)
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Discovery of Two Highly Selective Structurally Orthogonal Chemical Probes for Activin Receptor-like Kinases 1 and 2
Němec, Václav, Remeš, Marek, Beňovský, Petr, Böck, Michael C., Šranková, Eliška, Wong, Jong Fu, Cros, Julien, Williams, Eleanor, Tse, Lap Hang, Smil, David, Ensan, Deeba, Isaac, Methvin B., Al-Awar, Rima, Gomolková, Regina, Ursachi, Vlad-Constantin, Fafílek, Bohumil, Kahounová, Zuzana, Víchová, Ráchel, Vacek, Ondřej, Berger, Benedict-Tilman, Wells, Carrow I., Corona, Cesear R., Vasta, James D., Robers, Matthew B., Krejci, Pavel, Souček, Karel, Bullock, Alex N., Knapp, Stefan, Paruch, Kamil
Published in Journal of medicinal chemistry (08.08.2024)
Published in Journal of medicinal chemistry (08.08.2024)
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Quantitative, Real-Time Measurements of Intracellular Target Engagement Using Energy Transfer
Robers, Matthew B, Vasta, James D, Corona, Cesear R, Ohana, Rachel Friedman, Hurst, Robin, Jhala, Manisha A, Comess, Kenneth M, Wood, Keith V
Published in Methods in molecular biology (Clifton, N.J.) (2019)
Published in Methods in molecular biology (Clifton, N.J.) (2019)
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Discovery of a selective inhibitor of doublecortin like kinase 1
Ferguson, Fleur M., Nabet, Behnam, Raghavan, Srivatsan, Liu, Yan, Leggett, Alan L., Kuljanin, Miljan, Kalekar, Radha L., Yang, Annan, He, Shuning, Wang, Jinhua, Ng, Raymond W. S., Sulahian, Rita, Li, Lianbo, Poulin, Emily J., Huang, Ling, Koren, Jost, Dieguez-Martinez, Nora, Espinosa, Sergio, Zeng, Zhiyang, Corona, Cesear R., Vasta, James D., Ohi, Ryoma, Sim, Taebo, Kim, Nam Doo, Harshbarger, Wayne, Lizcano, Jose M., Robers, Matthew B., Muthaswamy, Senthil, Lin, Charles Y., Look, A. Thomas, Haigis, Kevin M., Mancias, Joseph D., Wolpin, Brian M., Aguirre, Andrew J., Hahn, William C., Westover, Kenneth D., Gray, Nathanael S.
Published in Nature chemical biology (01.06.2020)
Published in Nature chemical biology (01.06.2020)
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Journal Article
Design of a “two-in-one” mutant-selective EGFR inhibitor that spans the orthosteric and allosteric sites
Wittlinger, Florian, Heppner, David E., To, Ciric, Günther, Marcel, Shin, Bo Hee, Rana, Jaimin K., Schmoker, Anna M., Beyett, Tyler S., Berger, Lena M., Berger, Benedict-Tilman, Bauer, Nicolas, Vasta, James D., Corona, Cesear R., Robers, Matthew B., Knapp, Stefan, Jänne, Pasi A., Eck, Michael J., Laufer, Stefan A.
Published in Journal of medicinal chemistry (20.10.2021)
Published in Journal of medicinal chemistry (20.10.2021)
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Journal Article
KRAS is vulnerable to reversible switch-II pocket engagement in cells
Vasta, James D, Peacock, D Matthew, Zheng, Qinheng, Walker, Joel A, Zhang, Ziyang, Zimprich, Chad A, Thomas, Morgan R, Beck, Michael T, Binkowski, Brock F, Corona, Cesear R, Robers, Matthew B, Shokat, Kevan M
Published in bioRxiv (15.10.2021)
Published in bioRxiv (15.10.2021)
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Small Molecule Modulation of the Archetypal UbiB protein COQ8
Murray, Nathan H, Lewis, Adam, Asquith, Christopher R M, Rincon Pabon, Juan P, Fang, Zixiang, Ptak, Naomi, Smith, Robert W, Vasta, James D, Zimprich, Chad A, Corona, Cesear R, Robers, Matthew B, Bingman, Craig A, Gross, Michael L, Henzler-Wildman, Katherine, Pagliarini, David J
Published in bioRxiv (23.03.2022)
Published in bioRxiv (23.03.2022)
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