Drugging an undruggable pocket on KRAS
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.
Published in Proceedings of the National Academy of Sciences - PNAS (06.08.2019)
Published in Proceedings of the National Academy of Sciences - PNAS (06.08.2019)
Get full text
Journal Article
Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange
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.
Published in Proceedings of the National Academy of Sciences - PNAS (04.03.2014)
Published in Proceedings of the National Academy of Sciences - PNAS (04.03.2014)
Get full text
Journal Article
Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation
Sun, Qi, Burke, Jason P., Phan, Jason, Burns, Michael C., Olejniczak, Edward T., Waterson, Alex G., Lee, Taekyu, Rossanese, Olivia W., Fesik, Stephen W.
Published in Angewandte Chemie International Edition (18.06.2012)
Published in Angewandte Chemie International Edition (18.06.2012)
Get full text
Journal Article
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)
Get full text
Journal Article
Discovery of WD Repeat-Containing Protein 5 (WDR5)–MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design
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
Published in Journal of medicinal chemistry (23.04.2020)
Published in Journal of medicinal chemistry (23.04.2020)
Get full text
Journal Article
Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods
Sarkar, Dhruba, Olejniczak, Edward T, Phan, Jason, Coker, Jesse A, Sai, Jiqing, Arnold, Allison, Beesetty, Yugandhar, Waterson, Alex G, Fesik, Stephen W
Published in Journal of medicinal chemistry (13.08.2020)
Published in Journal of medicinal chemistry (13.08.2020)
Get full text
Journal Article
Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α
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
Published in Nature chemical biology (01.11.2010)
Published in Nature chemical biology (01.11.2010)
Get full text
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)
Get full text
Journal Article
Small Molecule-Mediated Activation of RAS Elicits Biphasic Modulation of Phospho-ERK Levels that Are Regulated through Negative Feedback on SOS1
Howes, Jennifer E, Akan, Denis T, Burns, Michael C, Rossanese, Olivia W, Waterson, Alex G, Fesik, Stephen W
Published in Molecular cancer therapeutics (01.05.2018)
Published in Molecular cancer therapeutics (01.05.2018)
Get full text
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)
Get full text
Journal Article
Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH)
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
Published in Journal of medicinal chemistry (22.11.2017)
Published in Journal of medicinal chemistry (22.11.2017)
Get full text
Journal Article
Arrest of mouse preterm labor until term delivery by combination therapy with atosiban and mundulone, a natural product with tocolytic efficacy
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.
Published in Pharmacological research (01.09.2023)
Published in Pharmacological research (01.09.2023)
Get full text
Journal Article
Allosteric antagonism of insect odorant receptor ion channels
Jones, Patrick L, Pask, Gregory M, Romaine, Ian M, Taylor, Robert W, Reid, Paul R, Waterson, Alex G, Sulikowski, Gary A, Zwiebel, Laurence J
Published in PloS one (17.01.2012)
Published in PloS one (17.01.2012)
Get full text
Journal Article
Dynamic Imaging of LDH Inhibition in Tumors Reveals Rapid In Vivo Metabolic Rewiring and Vulnerability to Combination Therapy
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.
Published in Cell reports (Cambridge) (11.02.2020)
Published in Cell reports (Cambridge) (11.02.2020)
Get full text
Journal Article
A fragment‐based approach to discovery of Receptor for Advanced Glycation End products inhibitors
Kozlyuk, Natalia, Gilston, Benjamin A., Salay, Lauren E., Gogliotti, Rocco D., Christov, Plamen P., Kim, Kwangho, Ovee, Mohiuddin, Waterson, Alex G., Chazin, Walter J.
Published in Proteins, structure, function, and bioinformatics (01.11.2021)
Published in Proteins, structure, function, and bioinformatics (01.11.2021)
Get full text
Journal Article
Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5–MYC Protein–Protein Interaction
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
Published in Journal of medicinal chemistry (26.12.2019)
Published in Journal of medicinal chemistry (26.12.2019)
Get full text
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)
Get full text
Journal Article
Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties
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
Published in Journal of medicinal chemistry (08.10.2020)
Published in Journal of medicinal chemistry (08.10.2020)
Get full text
Journal Article
Small Molecule Activation of NAPE-PLD Enhances Efferocytosis by Macrophages
Zarrow, Jonah E., Alli-Oluwafuyi, Abdul-Musawwir, Youwakim, Cristina M., Kim, Kwangho, Jenkins, Andrew N., Suero, Isabelle C., Jones, Margaret R., Mashhadi, Zahra, Mackie, Ken, Waterson, Alex G., Doran, Amanda C., Sulikowski, Gary A., Davies, Sean S.
Published in ACS chemical biology (18.08.2023)
Published in ACS chemical biology (18.08.2023)
Get full text
Journal Article
Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: Development of a highly selective and more potent in vitro probe
Delpire, Eric, Baranczak, Aleksandra, Waterson, Alex G., Kim, Kwangho, Kett, Nathan, Morrison, Ryan D., Scott Daniels, J., David Weaver, C., Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (15.07.2012)
Published in Bioorganic & medicinal chemistry letters (15.07.2012)
Get full text
Journal Article