RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers von Nichols, Robert J., Haderk, Franziska, Stahlhut, Carlos, Schulze, Christopher J., Hemmati, Golzar, Wildes, David, Tzitzilonis, Christos, Mordec, Kasia, Marquez, Abby, Romero, Jason, Hsieh, Tientien, Zaman, Aubhishek, Olivas, Victor, McCoach, Caroline, Blakely, Collin M., Wang, Zhengping, Kiss, Gert, Koltun, Elena S., Gill, Adrian L., Singh, Mallika, Goldsmith, Mark A., Smith, Jacqueline A. M., Bivona, Trever G.

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Automated iterative Csp3–C bond formation von Blair, Daniel J., Chitti, Sriyankari, Trobe, Melanie, Kostyra, David M., Haley, Hannah M. S., Hansen, Richard L., Ballmer, Steve G., Woods, Toby J., Wang, Wesley, Mubayi, Vikram, Schmidt, Michael J., Pipal, Robert W., Morehouse, Greg. F., Palazzolo Ray, Andrea M. E., Gray, Danielle L., Gill, Adrian L., Burke, Martin D.

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Allosteric Inhibition of SHP2 Stimulates Antitumor Immunity by Transforming the Immunosuppressive Environment von Quintana, Elsa, Schulze, Christopher J., Myers, Darienne R., Choy, Tiffany J., Mordec, Kasia, Wildes, David, Shifrin, Nataliya Tobvis, Belwafa, Amira, Koltun, Elena S., Gill, Adrian L., Singh, Mallika, Kelsey, Stephen, Goldsmith, Mark A., Nichols, Robert, Smith, Jacqueline A. M.

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Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS von Schulze, Christopher J., Seamon, Kyle J., Zhao, Yulei, Yang, Yu C., Cregg, Jim, Kim, Dongsung, Tomlinson, Aidan, Choy, Tiffany J., Wang, Zhican, Sang, Ben, Pourfarjam, Yasin, Lucas, Jessica, Cuevas-Navarro, Antonio, Ayala-Santos, Carlos, Vides, Alberto, Li, Chuanchuan, Marquez, Abby, Zhong, Mengqi, Vemulapalli, Vidyasiri, Weller, Caroline, Gould, Andrea, Whalen, Daniel M., Salvador, Anthony, Milin, Anthony, Saldajeno-Concar, Mae, Dinglasan, Nuntana, Chen, Anqi, Evans, Jim, Knox, John E., Koltun, Elena S., Singh, Mallika, Nichols, Robert, Wildes, David, Gill, Adrian L., Smith, Jacqueline A. M., Lito, Piro

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Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy von Holderfield, Matthew, Lee, Bianca J., Jiang, Jingjing, Tomlinson, Aidan, Seamon, Kyle J., Mira, Alessia, Patrucco, Enrico, Goodhart, Grace, Dilly, Julien, Gindin, Yevgeniy, Dinglasan, Nuntana, Wang, Yingyun, Lai, Lick Pui, Cai, Shurui, Jiang, Lingyan, Nasholm, Nicole, Shifrin, Nataliya, Blaj, Cristina, Shah, Harshit, Evans, James W., Montazer, Nilufar, Lai, Oliver, Shi, Jade, Ahler, Ethan, Quintana, Elsa, Chang, Stephanie, Salvador, Anthony, Marquez, Abby, Cregg, Jim, Liu, Yang, Milin, Anthony, Chen, Anqi, Ziv, Tamar Bar, Parsons, Dylan, Knox, John E., Klomp, Jennifer E., Roth, Jennifer, Rees, Matthew, Ronan, Melissa, Cuevas-Navarro, Antonio, Hu, Feng, Lito, Piro, Santamaria, David, Aguirre, Andrew J., Waters, Andrew M., Der, Channing J., Ambrogio, Chiara, Wang, Zhengping, Gill, Adrian L., Koltun, Elena S., Smith, Jacqueline A. M., Wildes, David, Singh, Mallika

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Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth von Lee, Bianca J., Boyer, Jacob A., Burnett, G. Leslie, Thottumkara, Arun P., Tibrewal, Nidhi, Wilson, Stacy L., Hsieh, Tientien, Marquez, Abby, Lorenzana, Edward G., Evans, James W., Hulea, Laura, Kiss, Gert, Liu, Hui, Lee, Dong, Larsson, Ola, McLaughlan, Shannon, Topisirovic, Ivan, Wang, Zhengping, Wang, Zhican, Zhao, Yongyuan, Wildes, David, Aggen, James B., Singh, Mallika, Gill, Adrian L., Smith, Jacqueline A. M., Rosen, Neal

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Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors von Burnett, G. Leslie, Yang, Yu C., Aggen, James B., Pitzen, Jennifer, Gliedt, Micah K., Semko, Chris M., Marquez, Abby, Evans, James W., Wang, Gang, Won, Walter S., Tomlinson, Aidan C. A., Kiss, Gert, Tzitzilonis, Christos, Thottumkara, Arun P., Cregg, James, Mellem, Kevin T., Choi, Jong S., Lee, Julie C., Zhao, Yongyuan, Lee, Bianca J., Meyerowitz, Justin G., Knox, John E., Jiang, Jingjing, Wang, Zhican, Wildes, David, Wang, Zhengping, Singh, Mallika, Smith, Jacqueline A. M., Gill, Adrian L.

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Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity von Howard, Steven, Berdini, Valerio, Boulstridge, John A, Carr, Maria G, Cross, David M, Curry, Jayne, Devine, Lindsay A, Early, Theresa R, Fazal, Lynsey, Gill, Adrian L, Heathcote, Michelle, Maman, Sarita, Matthews, Julia E, McMenamin, Rachel L, Navarro, Eva F, O’Brien, Michael A, O’Reilly, Marc, Rees, David C, Reule, Matthias, Tisi, Dominic, Williams, Glyn, Vinković, Mladen, Wyatt, Paul G

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Kinetic efficiency: the missing metric for enhancing compound quality? von Holdgate, Geoffrey A., Gill, Adrian L.

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Author Correction: Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth von Lee, Bianca J., Boyer, Jacob A., Burnett, G. Leslie, Thottumkara, Arun P., Tibrewal, Nidhi, Wilson, Stacy L., Hsieh, Tientien, Marquez, Abby, Lorenzana, Edward G., Evans, James W., Hulea, Laura, Kiss, Gert, Liu, Hui, Lee, Dong, Larsson, Ola, McLaughlan, Shannon, Topisirovic, Ivan, Wang, Zhengping, Wang, Zhican, Zhao, Yongyuan, Wildes, David, Aggen, James B., Singh, Mallika, Gill, Adrian L., Smith, Jacqueline A. M., Rosen, Neal

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Author Correction: Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth von Lee, Bianca J., Boyer, Jacob A., Burnett, G. Leslie, Thottumkara, Arun P., Tibrewal, Nidhi, Wilson, Stacy L., Hsieh, Tientien, Marquez, Abby, Lorenzana, Edward G., Evans, James W., Hulea, Laura, Kiss, Gert, Liu, Hui, Lee, Dong, Larsson, Ola, McLaughlan, Shannon, Topisirovic, Ivan, Wang, Zhengping, Wang, Zhican, Zhao, Yongyuan, Wildes, David, Aggen, James B., Singh, Mallika, Gill, Adrian L., Smith, Jacqueline A. M., Rosen, Neal

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Identification of Novel p38α MAP Kinase Inhibitors Using Fragment-Based Lead Generation von Gill, Adrian L, Frederickson, Martyn, Cleasby, Anne, Woodhead, Steven J, Carr, Maria G, Woodhead, Andrew J, Walker, Margaret T, Congreve, Miles S, Devine, Lindsay A, Tisi, Dominic, O'Reilly, Marc, Seavers, Lisa C. A, Davis, Deborah J, Curry, Jayne, Anthony, Rachel, Padova, Alessandro, Murray, Christopher W, Carr, Robin A. E, Jhoti, Harren

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A general approach to the galanthamine ring system von Parsons, Philip J, Charles, Mark D, Harvey, Darren M, Sumoreeah, L.Ravi, Shell, Adrian, Spoors, Grant, Gill, Adrian L, Smith, Steve

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Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors von Scott, James S., Gill, Adrian L., Godfrey, Linda, Groombridge, Sam D., Rees, Amanda, Revill, John, Schofield, Paul, Sörme, Pernilla, Stocker, Andrew, Swales, John G., Whittamore, Paul R.O.

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Direct targeting of RAS in pancreatic ductal adenocarcinoma with RMC-6236, a first-in-class, RAS-selective, orally bioavailable, tri-complex RAS MULTI (ON) inhibitor von Gustafson, W. Clay, Wildes, David, Rice, Meghan A., Lee, Bianca J., Jiang, Jingjing, Wang, Zhengping, Chang, Stephanie, Flagella, Mike, Mu, Yunming, Dinglasan, Nuntana, Nasholm, Nicole, Evans, James W., Seamon, Kyle, Cregg, Jim, Bermingham, Alun, Freilich, Rebecca, Gill, Adrian L., Koltun, Elena, Smith, Jacqueline A, Singh, Mallika

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Allosteric Inhibition of SHP2 Stimulates Antitumor Immunity by Transforming the Immunosuppressive Environment von Quintana, Elsa, Schulze, Christopher J., Myers, Darienne R., Choy, Tiffany J., Mordec, Kasia, Wildes, David, Shifrin, Nataliya Tobvis, Belwafa, Amira, Koltun, Elena S., Gill, Adrian L., Singh, Mallika, Kelsey, Stephen, Goldsmith, Mark A., Nichols, Robert, Smith, Jacqueline A. M.

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Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth (Jun, 10.1038/s41589-021-00813-7, 2021) von Lee, Bianca J., Boyer, Jacob A., Burnett, G. Leslie, Thottumkara, Arun P., Tibrewal, Nidhi, Wilson, Stacy L., Hsieh, Tientien, Marquez, Abby, Lorenzana, Edward G., Evans, James W., Hulea, Laura, Kiss, Gert, Liu, Hui, Lee, Dong, Larsson, Ola, McLaughlan, Shannon, Topisirovic, Ivan, Wang, Zhengping, Wang, Zhican, Zhao, Yongyuan, Wildes, David, Aggen, James B., Singh, Mallika, Gill, Adrian L., Smith, Jacqueline A. M., Rosen, Neal

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Abstract 1260: First-in-class, orally bioavailable KRASG12V(ON) tri-complex inhibitors, as single agents and in combinations, drive profound anti-tumor activity in preclinical mode... von Koltun, Elena, Cregg, Jim, Rice, Meghan A., Whalen, Dan M., Freilich, Rebecca, Jiang, Jingjing, Hansen, Richard, Bermingham, Alun, Knox, John E., Dinglasan, Jay, Seamon, Kyle, Blaj, Cristina, Chang, Stephanie S., Liu, Yang, Huang, Jun, Chou, Kang-Jye, McDowell, Laura, Lee, Bianca J., Wildes, David, Wang, Zhengping, Singh, Mallika, Gill, Adrian L., Smith, Jacqueline A.

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Abstract 1261: A next generation tri-complex KRASG12C(ON) inhibitor directly targets the active, GTP-bound state of mutant RAS and may overcome resistance to KRASG12C(OFF) inhibiti... von Nichols, Robert J., Cregg, Jim, Schulze, Christopher J., Wang, Zhican, Yang, Kevin, Jiang, Jingjing, Whalen, Daniel M., Hansen, Rich, Garrenton, Lindsay S., Bermingham, Alun, Knox, John E., Choy, Tiffany, Reyes, Denise, Rios, Mayra, Seamon, Kyle, Longhi, Michael, Chou, Kang-Jye, Li, Shaoling, Wildes, David P., Singh, Mallika, Koltun, Elena S., Gill, Adrian L., Smith, Jacqueline A. M.

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Abstract 1273: Discovery of a potent, selective, and orally bioavailable SOS1 inhibitor, RMC-023, an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1... von Buckl, Andreas, Quintana, Elsa, Lee, Grace J., Shifrin, Nataliya, Zhong, Mengqi, Garrenton, Lindsay S., Montgomery, David C., Stahlhut, Carlos, Zhao, Frances, Whalen, Dan M., Thompson, Severin K., Tambo-ong, Arlyn, Gliedt, Micah, Knox, John E., Cregg, James J., Aay, Naing, Choi, Jong, Nguyen, Bao, Tripathi, Atti, Zhao, Ruiping, Saldajeno-Concar, Mae, Marquez, Abby, Hsieh, Daphne, McDowell, Laura L., Koltun, Elena S., Bermingham, Alun, Wildes, David, Singh, Mallika, Wang, Zhengping, Hansen, Richard, Smith, Jan A., Gill, Adrian L.

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