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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Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973) von Rice, Kenneth D, Aay, Naing, Anand, Neel K, Blazey, Charles M, Bowles, Owen J, Bussenius, Joerg, Costanzo, Simona, Curtis, Jeffry K, Defina, Steven C, Dubenko, Larisa, Engst, Stefan, Joshi, Anagha A, Kennedy, Abigail R, Kim, Angie I, Koltun, Elena S, Lougheed, Julie C, Manalo, Jean-Claire L, Martini, Jean-Francois, Nuss, John M, Peto, Csaba J, Tsang, Tsze H, Yu, Peiwen, Johnston, Stuart

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Discovery of XL413, a potent and selective CDC7 inhibitor von Koltun, Elena S., Tsuhako, Amy Lew, Brown, David S., Aay, Naing, Arcalas, Arlyn, Chan, Vicky, Du, Hongwang, Engst, Stefan, Ferguson, Kim, Franzini, Maurizio, Galan, Adam, Holst, Charles R., Huang, Ping, Kane, Brian, Kim, Moon H., Li, Jia, Markby, David, Mohan, Manisha, Noson, Kevin, Plonowski, Arthur, Richards, Steven J., Robertson, Scott, Shaw, Kenneth, Stott, Gordon, Stout, Thomas J., Young, Jenny, Yu, Peiwen, Zaharia, Cristiana A., Zhang, Wentao, Zhou, Peiwen, Nuss, John M., Xu, Wei, Kearney, Patrick C.

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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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Tartaric Acid and Tartrates in the Synthesis of Bioactive Molecules von Ghosh, Arun K., Koltun, Elena S., Bilcer, Geoffrey

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The design, synthesis, and biological evaluation of PIM kinase inhibitors von Tsuhako, Amy Lew, Brown, David S., Koltun, Elena S., Aay, Naing, Arcalas, Arlyn, Chan, Vicky, Du, Hongwang, Engst, Stefan, Franzini, Maurizio, Galan, Adam, Huang, Ping, Johnston, Stuart, Kane, Brian, Kim, Moon H., Douglas Laird, A., Lin, Rui, Mock, Lillian, Ngan, Iris, Pack, Michael, Stott, Gordon, Stout, Thomas J., Yu, Peiwen, Zaharia, Cristiana, Zhang, Wentao, Zhou, Peiwen, Nuss, John M., Kearney, Patrick C., Xu, Wei

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Discovery and Characterization of an Inhibitor of Glucosylceramide Synthase von Richards, Steven, Larson, Christopher J, Koltun, Elena S, Hanel, Art, Chan, Vicky, Nachtigall, Jason, Harrison, Amanda, Aay, Naing, Du, Hongwang, Arcalas, Arlyn, Galan, Adam, Zhang, Jeff, Zhang, Wentao, Won, Kwang-Ai, Tam, Danny, Qian, Fawn, Wang, Tao, Finn, Patricia, Ogilvie, Kathy, Rosen, Jon, Aoyama, Ron, Plonowski, Artur, Cancilla, Belinda, Bentzien, Frauke, Yakes, Michael, Mohan, Raju, Lamb, Peter, Nuss, John, Kearney, Patrick

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SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors von Forsyth, Timothy, Kearney, Patrick C., Kim, Byung Gyu, Johnson, Henry W.B., Aay, Naing, Arcalas, Arlyn, Brown, David S., Chan, Vicky, Chen, Jeff, Du, Hongwang, Epshteyn, Sergey, Galan, Adam A., Huynh, Tai P., Ibrahim, Mohamed A., Kane, Brian, Koltun, Elena S., Mann, Grace, Meyr, Lisa E., Lee, Matthew S., Lewis, Gary L., Noguchi, Robin T., Pack, Michael, Ridgway, Brian H., Shi, Xian, Takeuchi, Craig S., Zu, Peiwen, Leahy, James W., Nuss, John M., Aoyama, Ron, Engst, Stefan, Gendreau, Steven B., Kassees, Robert, Li, Jia, Lin, Shwu-Hwa, Martini, Jean-Francois, Stout, Thomas, Tong, Philip, Woolfrey, John, Zhang, Wentao, Yu, Peiwen

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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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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 1322: Maximizing the therapeutic potential of SHP2 inhibition with rational combination strategies in tumors driven by aberrant RAS-MAPK signaling von Lee, Grace J., Stahlhut, Carlos, Evans, James, Reyes, Denise F., Lorenzana, Edward G., Li, Shaoling, Koltun, Elena S., Lee, Dong, Wang, Zhengping, Nichols, Robert J., Smith, Jacqueline A., Singh, Mallika

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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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Abstract 1943: SHP2 inhibition as the backbone of targeted therapy combinations for the treatment of cancers driven by oncogenic mutations in the RAS pathway von Smith, Jacqueline A., Singh, Mallika, Nichols, Robert J., Koltun, Elena S., Yang, Yu C., Wildes, David P., Stahlhut, Carlos, Lee, Dong, Schulze, Chris J., Reyes, Denise, Marquez, Abby, Lee, Grace J., Li, Shaoling, Marcireau, Christophe, Debussche, Laurent, Goldsmith, Mark A., Wang, Zhengping, Gill, Adrian L., Kelsey, Steve M.

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Synthesis and Reactivity of trans-Tricyclo[4.2.0.01,3]oct-4-ene von Koltun, Elena S, Kass, Steven R

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Ring Scission of Diastereomeric 4-Butylspiropentylcarbinyl Radicals as a Chemical Model for Identifying Enzyme-Catalyzed FAD Adducts Resulting from Spiropentylacetyl-CoA von Lis, Lev, Koltun, Elena S, Liu, Hung-wen, Kass, Steven R

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Abstract PR10: Tri-complex inhibitors of the oncogenic, GTP-bound form of KRASG12C overcome RTK-mediated escape mechanisms and drive tumor regressions in vivo von Schulze, Christopher J, Bermingham, Alun, Choy, Tiffany J, Cregg, James J, Kiss, Gert, Marquez, Abby, Reyes, Denise, Saldajeno-Concar, Mae, Weller, Caroline E, Whalen, Daniel M, Yang, Yu C, Koltun, Elena S, Nichols, Robert J, Singh, Mallika, Wildes, David, Gill, Adrian L, Hansen, Richard L, Kelsey, Steve, Goldsmith, Mark A, Smith, Jacqueline A.M.

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Abstract 4877: Allosteric inhibition of SHP2 variants containing cancer-associated activating mutations von Wildes, David, Aay, Naing, Buckl, Andreas, Hsieh, Daphne, Jogalekar, Ashutosh S., Kiss, Gert, Koltun, Elena S., Marquez, Abby, Mellem, Kevin T., Romero, Jason, Saldajeno-Concar, Mae, Schulze, Christopher J., Semko, Chris M., Won, Walter, Nichols, Robert J., Stahlhut, Carlos, Tzitzilonis, Christos, Gill, Adrian L., Smith, Jacqueline A.

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Abstract 4878: RMC-4550, an allosteric inhibitor of SHP2: Synthesis, structure, and anti-tumor activity von Koltun, Elena S., Aay, Naing, Buckl, Andreas, Jogalekar, Ashutosh S., Kiss, Gert, Marquez, Abby, Mellem, Kevin T., Mordec, Kasia, Saldajeno-Concar, Mae, Semko, Chris M., Tibrewal, Nidhi, Tzitzilonis, Christos, Won, Walter, Smith, Jacqueline A., Wilson, Susan E., Nichols, Robert J., Wang, Zhengping, Wilds, David, Singh, Mallika, Gill, Adrian L.

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