Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor
Bröker, Joachim, Waterson, Alex G., Smethurst, Chris, Kessler, Dirk, Böttcher, Jark, Mayer, Moriz, Gmaschitz, Gerhard, Phan, Jason, Little, Andrew, Abbott, Jason R., Sun, Qi, Gmachl, Michael, Rudolph, Dorothea, Arnhof, Heribert, Rumpel, Klaus, Savarese, Fabio, Gerstberger, Thomas, Mischerikow, Nikolai, Treu, Matthias, Herdeis, Lorenz, Wunberg, Tobias, Gollner, Andreas, Weinstabl, Harald, Mantoulidis, Andreas, Krämer, Oliver, McConnell, Darryl B., W. Fesik, Stephen
Published in Journal of medicinal chemistry (10.11.2022)
Published in Journal of medicinal chemistry (10.11.2022)
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Journal Article
Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS
Hodges, Timothy R, Abbott, Jason R, Little, Andrew J, Sarkar, Dhruba, Salovich, James M, Howes, Jennifer E, Akan, Denis T, Sai, Jiqing, Arnold, Allison L, Browning, Carrie, Burns, Michael C, Sobolik, Tammy, Sun, Qi, Beesetty, Yugandhar, Coker, Jesse A, Scharn, Dirk, Stadtmueller, Heinz, Rossanese, Olivia W, Phan, Jason, Waterson, Alex G, McConnell, Darryl B, Fesik, Stephen W
Published in Journal of medicinal chemistry (11.10.2018)
Published in Journal of medicinal chemistry (11.10.2018)
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Journal Article
High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling
Burns, Michael C., Howes, Jennifer E., Sun, Qi, Little, Andrew J., Camper, DeMarco V., Abbott, Jason R., Phan, Jason, Lee, Taekyu, Waterson, Alex G., Rossanese, Olivia W., Fesik, Stephen W.
Published in Analytical biochemistry (01.05.2018)
Published in Analytical biochemistry (01.05.2018)
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Journal Article
Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling
Abbott, Jason R, Hodges, Timothy R, Daniels, R. Nathan, Patel, Pratiq A, Kennedy, J. Phillip, Howes, Jennifer E, Akan, Denis T, Burns, Michael C, Sai, Jiqing, Sobolik, Tammy, Beesetty, Yugandhar, Lee, Taekyu, Rossanese, Olivia W, Phan, Jason, Waterson, Alex G, Fesik, Stephen W
Published in Journal of medicinal chemistry (26.07.2018)
Published in Journal of medicinal chemistry (26.07.2018)
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Journal Article
Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS
Abbott, Jason R, Patel, Pratiq A, Howes, Jennifer E, Akan, Denis T, Kennedy, J. Phillip, Burns, Michael C, Browning, Carrie F, Sun, Qi, Rossanese, Olivia W, Phan, Jason, Waterson, Alex G, Fesik, Stephen W
Published in ACS medicinal chemistry letters (13.09.2018)
Published in ACS medicinal chemistry letters (13.09.2018)
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Journal Article
Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS G12C Inhibitor
Bröker, Joachim, Waterson, Alex G., Smethurst, Chris, Kessler, Dirk, Böttcher, Jark, Mayer, Moriz, Gmaschitz, Gerhard, Phan, Jason, Little, Andrew, Abbott, Jason R., Sun, Qi, Gmachl, Michael, Rudolph, Dorothea, Arnhof, Heribert, Rumpel, Klaus, Savarese, Fabio, Gerstberger, Thomas, Mischerikow, Nikolai, Treu, Matthias, Herdeis, Lorenz, Wunberg, Tobias, Gollner, Andreas, Weinstabl, Harald, Mantoulidis, Andreas, Krämer, Oliver, McConnell, Darryl B., W. Fesik, Stephen
Published in Journal of medicinal chemistry (10.11.2022)
Published in Journal of medicinal chemistry (10.11.2022)
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Journal Article
Abstract 865: Small molecule-mediated modulation of Ras elicits inhibition of phospho ERK signaling through negative feedback on SOS1
Howes, Jennifer E., Akan, Denis T., Burns, Michael C., Sun, Qi, Little, Andrew J., Camper, DeMarco V., Abbott, Jason R., Phan, Jason, Lee, Taekyu, Rossanese, Olivia W., Waterson, Alex G., Fesik, Stephen W.
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Journal Article
High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling
Burns, Michael C., Howes, Jennifer E., Sun, Qi, Little, Andrew J., Camper, DeMarco V., Abbott, Jason R., Phan, Jason, Lee, Taekyu, Waterson, Alex G., Rossanese, Olivia W., Fesik, Stephen W.
Published in Analytical biochemistry (01.05.2018)
Published in Analytical biochemistry (01.05.2018)
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Journal Article
Protein tyrosine phosphatase inhibitors and methods of use thereof
Phil KYM, Andrew BOGDAN, Christos ECONOMOU, Geoff HALVORSEN, Xueqing WANG, Zhaoming XIONG, Hongyu ZHAO, Elliot FARNEY, Roohollah Kazem SHIROODI, Qingwei ZHANG, Jason R. ABBOTT, Jennifer M. FROST, Matthew O'CONNOR, Christina BAUMGARTNER
Year of Publication 30.11.2023
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Year of Publication 30.11.2023
Patent
Protein tyrosine phosphatase inhibitors and methods of use thereof
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Year of Publication 24.08.2023
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Year of Publication 24.08.2023
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Quinazoline compounds as modulators of Ras signaling
Fesik, Stephen W, Burns, Michael C, Abbott, Jason R, Patel, Pratiq, Waterson, Alex G, Phan, Jason, Kennedy, J. Phillip, Sun, Qi
Year of Publication 03.05.2022
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Year of Publication 03.05.2022
Patent
PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
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Year of Publication 19.01.2023
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Year of Publication 19.01.2023
Patent
PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
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Year of Publication 26.10.2022
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Year of Publication 26.10.2022
Patent
Protein tyrosine phosphatase inhibitors and methods of use thereof
ZHAO, Hongyu, XIONG, Zhaoming, KYM, Philip R, ZHANG, Qingwei, FARNEY, Elliot P, O'CONNOR, Matthew, ECONOMOU, Christos, HALVORSEN, Geoff T, WANG, Xueqing, ABBOTT, Jason R, SHIROODI, Roohollah Kazem, BOGDAN, Andrew, BAUMGARTNER, Christina, FROST, Jennifer M
Year of Publication 30.06.2022
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Year of Publication 30.06.2022
Patent
Substituted benzimidazoles as modulators of Ras signaling
Waterson, Alex, Abbott, Jason R, Burns, Michael, Little, Andrew, Phan, Jason, Fesik, Steve, Salovich, James M, Sun, Qi
Year of Publication 10.12.2019
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Year of Publication 10.12.2019
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PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
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Year of Publication 16.08.2021
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Year of Publication 16.08.2021
Patent
QUINAZOLINE COMPOUNDS AS MODULATORS OF RAS SIGNALING
Fesik, Stephen W, Burns, Michael C, Abbott, Jason R, Patel, Pratiq, Waterson, Alex G, Phan, Jason, Kennedy, J. Phillip, Sun, Qi
Year of Publication 13.08.2020
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Year of Publication 13.08.2020
Patent
PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
SHIROODI, ROOHOLLAH KAZEM, ZHANG, QINGWEI, KYM, PHILIP R, ECONOMOU, CHRISTOS, HALVORSEN, GEOFF T, BAUMGARTNER, CHRISTINA, FARNEY, ELLIOT P, FROST, JENNIFER M, ZHAO, HONGYU, XIONG, ZHAOMING, O'CONNOR, MATTHEW, WANG, XUEQING, ABBOTT, JASON R, BOGDAN, ANDREW
Year of Publication 24.06.2021
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Year of Publication 24.06.2021
Patent