Drugging an undruggable pocket on KRAS von Kesslera, Dirk, Gmachla, Michael, Mantoulidisa, Andreas, Martin, Laetitia J., Zoephel, Andreas, Mayer, Moriz, Gollner, Andreas, Covini, David, Fischer, Silke, Gerstberger, Thomas, Gmaschitz, Teresa, Goodwin, Craig, Greb, Peter, Häring, Daniela, Hela, Wolfgang, Hoffmann, Johann, Karolyi-Oezguer, Jale, Knesl, Petr, Kornigg, Stefan, Koegl, Manfred, Kousek, Roland, Lamarre, Lyne, Moser, Franziska, Munico-Martinez, Silvia, Peinsipp, Christoph, Phan, Jason, Rinnenthal, Jörg, Sai, Jiqing, Salamon, Christian, Scherbantin, Yvonne, Schipany, Katharina, Schnitzer, Renate, Schrenk, Andreas, Sharps, Bernadette, Siszler, Gabriella, Sun, Qi, Waterson, Alex, Wolkerstorfer, Bernhard, Zeeb, Markus, Pearson, Mark, Fesik, Stephen W., McConnell, Darryl B.

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Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange von Burns, Michael C., Qi Sun, Daniels, R. Nathan, Camper, DeMarco, Kennedy, J. Phillip, Phan, Jason, Olejniczak, Edward T., Lee, Taekyu, Waterson, Alex G., Rossanese, Olivia W., Fesik, Stephen W.

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Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor von 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

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Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation von Sun, Qi, Burke, Jason P., Phan, Jason, Burns, Michael C., Olejniczak, Edward T., Waterson, Alex G., Lee, Taekyu, Rossanese, Olivia W., Fesik, Stephen W.

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Discovery of WD Repeat-Containing Protein 5 (WDR5)–MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design von Chacón Simon, Selena, Wang, Feng, Thomas, Lance R, Phan, Jason, Zhao, Bin, Olejniczak, Edward T, Macdonald, Jonathan D, Shaw, J. Grace, Schlund, Caden, Payne, William, Creighton, Joy, Stauffer, Shaun R, Waterson, Alex G, Tansey, William P, Fesik, Stephen W

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Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods von Sarkar, Dhruba, Olejniczak, Edward T, Phan, Jason, Coker, Jesse A, Sai, Jiqing, Arnold, Allison, Beesetty, Yugandhar, Waterson, Alex G, Fesik, Stephen W

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Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS von 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

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Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α von Lee, Ethan, Thorne, Curtis A, Hanson, Alison J, Schneider, Judsen, Tahinci, Emilios, Orton, Darren, Cselenyi, Christopher S, Jernigan, Kristin K, Meyers, Kelly C, Hang, Brian I, Waterson, Alex G, Kim, Kwangho, Melancon, Bruce, Ghidu, Victor P, Sulikowski, Gary A, LaFleur, Bonnie, Salic, Adrian, Lee, Laura A, Miller, David M

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Arrest of mouse preterm labor until term delivery by combination therapy with atosiban and mundulone, a natural product with tocolytic efficacy von Siricilla, Shajila, Hansen, Christopher J., Rogers, Jackson H., De, Debasmita, Simpson, Carolyn L., Waterson, Alex G., Sulikowski, Gary A., Crockett, Stacey L., Boatwright, Naoko, Reese, Jeff, Paria, Bibhash C., Newton, J., Herington, Jennifer L.

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Allosteric antagonism of insect odorant receptor ion channels von Jones, Patrick L, Pask, Gregory M, Romaine, Ian M, Taylor, Robert W, Reid, Paul R, Waterson, Alex G, Sulikowski, Gary A, Zwiebel, Laurence J

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High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling von 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.

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Small Molecule-Mediated Activation of RAS Elicits Biphasic Modulation of Phospho-ERK Levels that Are Regulated through Negative Feedback on SOS1 von Howes, Jennifer E, Akan, Denis T, Burns, Michael C, Rossanese, Olivia W, Waterson, Alex G, Fesik, Stephen W

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Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH) von Rai, Ganesha, Brimacombe, Kyle R, Mott, Bryan T, Urban, Daniel J, Hu, Xin, Yang, Shyh-Ming, Lee, Tobie D, Cheff, Dorian M, Kouznetsova, Jennifer, Benavides, Gloria A, Pohida, Katie, Kuenstner, Eric J, Luci, Diane K, Lukacs, Christine M, Davies, Douglas R, Dranow, David M, Zhu, Hu, Sulikowski, Gary, Moore, William J, Stott, Gordon M, Flint, Andrew J, Hall, Matthew D, Darley-Usmar, Victor M, Neckers, Leonard M, Dang, Chi V, Waterson, Alex G, Simeonov, Anton, Jadhav, Ajit, Maloney, David J

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Dynamic Imaging of LDH Inhibition in Tumors Reveals Rapid In Vivo Metabolic Rewiring and Vulnerability to Combination Therapy von Oshima, Nobu, Ishida, Ryo, Kishimoto, Shun, Beebe, Kristin, Brender, Jeffrey R., Yamamoto, Kazutoshi, Urban, Daniel, Rai, Ganesha, Johnson, Michelle S., Benavides, Gloria, Squadrito, Giuseppe L., Crooks, Dan, Jackson, Joseph, Joshi, Abhinav, Mott, Bryan T., Shrimp, Jonathan H., Moses, Michael A., Lee, Min-Jung, Yuno, Akira, Lee, Tobie D., Hu, Xin, Anderson, Tamara, Kusewitt, Donna, Hathaway, Helen H., Jadhav, Ajit, Picard, Didier, Trepel, Jane B., Mitchell, James B., Stott, Gordon M., Moore, William, Simeonov, Anton, Sklar, Larry A., Norenberg, Jeffrey P., Linehan, W. Marston, Maloney, David J., Dang, Chi V., Waterson, Alex G., Hall, Matthew, Darley-Usmar, Victor M., Krishna, Murali C., Neckers, Leonard M.

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A fragment‐based approach to discovery of Receptor for Advanced Glycation End products inhibitors von Kozlyuk, Natalia, Gilston, Benjamin A., Salay, Lauren E., Gogliotti, Rocco D., Christov, Plamen P., Kim, Kwangho, Ovee, Mohiuddin, Waterson, Alex G., Chazin, Walter J.

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Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5–MYC Protein–Protein Interaction von Macdonald, Jonathan D, Chacón Simon, Selena, Han, Changho, Wang, Feng, Shaw, J. Grace, Howes, Jennifer E, Sai, Jiqing, Yuh, Joannes P, Camper, Demarco, Alicie, Bethany M, Alvarado, Joseph, Nikhar, Sameer, Payne, William, Aho, Erin R, Bauer, Joshua A, Zhao, Bin, Phan, Jason, Thomas, Lance R, Rossanese, Olivia W, Tansey, William P, Waterson, Alex G, Stauffer, Shaun R, Fesik, Stephen W

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Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: Development of a highly selective and more potent in vitro probe von Delpire, Eric, Baranczak, Aleksandra, Waterson, Alex G., Kim, Kwangho, Kett, Nathan, Morrison, Ryan D., Scott Daniels, J., David Weaver, C., Lindsley, Craig W.

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Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling von 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

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Isoform selective PLD inhibition by novel, chiral 2,8-diazaspiro[4.5]decan-1-one derivatives von Waterson, Alex G., Scott, Sarah A., Kett, Nathan R., Blobaum, Anna L., Alex Brown, H., Lindsley, Craig W.

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Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties von Rai, Ganesha, Urban, Daniel J, Mott, Bryan T, Hu, Xin, Yang, Shyh-Ming, Benavides, Gloria A, Johnson, Michelle S, Squadrito, Giuseppe L, Brimacombe, Kyle R, Lee, Tobie D, Cheff, Dorian M, Zhu, Hu, Henderson, Mark J, Pohida, Katherine, Sulikowski, Gary A, Dranow, David M, Kabir, Md, Shah, Pranav, Padilha, Elias, Tao, Dingyin, Fang, Yuhong, Christov, Plamen P, Kim, Kwangho, Jana, Somnath, Muttil, Pavan, Anderson, Tamara, Kunda, Nitesh K, Hathaway, Helen J, Kusewitt, Donna F, Oshima, Nobu, Cherukuri, Murali, Davies, Douglas R, Norenberg, Jeffrey P, Sklar, Larry A, Moore, William J, Dang, Chi V, Stott, Gordon M, Neckers, Leonard, Flint, Andrew J, Darley-Usmar, Victor M, Simeonov, Anton, Waterson, Alex G, Jadhav, Ajit, Hall, Matthew D, Maloney, David J

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