Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition
Boudreau, Aaron, Purkey, Hans E, Hitz, Anna, Robarge, Kirk, Peterson, David, Labadie, Sharada, Kwong, Mandy, Hong, Rebecca, Gao, Min, Del Nagro, Christopher, Pusapati, Raju, Ma, Shuguang, Salphati, Laurent, Pang, Jodie, Zhou, Aihe, Lai, Tommy, Li, Yingjie, Chen, Zhongguo, Wei, Binqing, Yen, Ivana, Sideris, Steve, McCleland, Mark, Firestein, Ron, Corson, Laura, Vanderbilt, Alex, Williams, Simon, Daemen, Anneleen, Belvin, Marcia, Eigenbrot, Charles, Jackson, Peter K, Malek, Shiva, Hatzivassiliou, Georgia, Sampath, Deepak, Evangelista, Marie, O'Brien, Thomas
Published in Nature chemical biology (01.10.2016)
Published in Nature chemical biology (01.10.2016)
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Small Molecule Inhibition of GDC-0449 Refractory Smoothened Mutants and Downstream Mechanisms of Drug Resistance
DIJKGRAAF, Gerrit J. P, ALICKE, Bruno, SCALES, Suzie J, GOULD, Stephen E, YAUCH, Robert L, DE SAUVAGE, Frederic J, WEINMANN, Lasse, JANUARIO, Thomas, WEST, Kristina, MODRUSAN, Zora, BURDICK, Dan, GOLDSMITH, Richard, ROBARGE, Kirk, SUTHERLIN, Dan
Published in Cancer research (Chicago, Ill.) (15.01.2011)
Published in Cancer research (Chicago, Ill.) (15.01.2011)
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GDC-0449—A potent inhibitor of the hedgehog pathway
Robarge, Kirk D., Brunton, Shirley A., Castanedo, Georgette M., Cui, Yong, Dina, Michael S., Goldsmith, Richard, Gould, Stephen E., Guichert, Oivin, Gunzner, Janet L., Halladay, Jason, Jia, Wei, Khojasteh, Cyrus, Koehler, Michael F.T., Kotkow, Karen, La, Hank, LaLonde, Rebecca L., Lau, Kevin, Lee, Leslie, Marshall, Derek, Marsters, James C., Murray, Lesley J., Qian, Changgeng, Rubin, Lee L., Salphati, Laurent, Stanley, Mark S., Stibbard, John H.A., Sutherlin, Daniel P., Ubhayaker, Savita, Wang, Shumei, Wong, Susan, Xie, Minli
Published in Bioorganic & medicinal chemistry letters (01.10.2009)
Published in Bioorganic & medicinal chemistry letters (01.10.2009)
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Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists
Fauber, Benjamin P., Gobbi, Alberto, Robarge, Kirk, Zhou, Aihe, Barnard, Adrian, Cao, Jianhua, Deng, Yuzhong, Eidenschenk, Céline, Everett, Christine, Ganguli, Arunima, Hawkins, Julie, Johnson, Adam R., La, Hank, Norman, Maxine, Salmon, Gary, Summerhill, Susan, Ouyang, Wenjun, Tang, Wei, Wong, Harvey
Published in Bioorganic & medicinal chemistry letters (01.08.2015)
Published in Bioorganic & medicinal chemistry letters (01.08.2015)
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A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors
Lee, Wendy, Ortwine, Daniel F., Bergeron, Philippe, Lau, Kevin, Lin, Lichuan, Malek, Shiva, Nonomiya, Jim, Pei, Zhonghua, Robarge, Kirk D., Schmidt, Stephen, Sideris, Steve, Lyssikatos, Joseph P.
Published in Bioorganic & medicinal chemistry letters (15.09.2013)
Published in Bioorganic & medicinal chemistry letters (15.09.2013)
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Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479
Robarge, Kirk D., Lee, Wendy, Eigenbrot, Charles, Ultsch, Mark, Wiesmann, Christian, Heald, Robert, Price, Steve, Hewitt, Joanne, Jackson, Philip, Savy, Pascal, Burton, Brenda, Choo, Edna F., Pang, Jodie, Boggs, Jason, Yang, April, Yang, Xioaye, Baumgardner, Matthew
Published in Bioorganic & medicinal chemistry letters (01.10.2014)
Published in Bioorganic & medicinal chemistry letters (01.10.2014)
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Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions
Choo, Edna F, Belvin, Marcia, Boggs, Jason, Deng, Yuzhong, Hoeflich, Klaus P, Ly, Justin, Merchant, Mark, Orr, Christine, Plise, Emile, Robarge, Kirk, Martini, Jean F, Kassees, Robert, Aoyama, Ron G, Ramaiya, Atulkumar, Johnston, Stuart H
Published in Drug metabolism and disposition (01.05.2012)
Published in Drug metabolism and disposition (01.05.2012)
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Potent, Selective, and Orally Bioavailable Inhibitors of Mammalian Target of Rapamycin (mTOR) Kinase Based on a Quaternary Substituted Dihydrofuropyrimidine
Cohen, Frederick, Bergeron, Philippe, Blackwood, Elizabeth, Bowman, Krista K, Chen, Huifen, DiPasquale, Antonio G, Epler, Jennifer A, Koehler, Michael F. T, Lau, Kevin, Lewis, Cristina, Liu, Lichuan, Ly, Cuong Q, Malek, Shiva, Nonomiya, Jim, Ortwine, Daniel F, Pei, Zhonghua, Robarge, Kirk D, Sideris, Steve, Trinh, Lan, Truong, Tom, Wu, Jiansheng, Zhao, Xianrui, Lyssikatos, Joseph P
Published in Journal of medicinal chemistry (12.05.2011)
Published in Journal of medicinal chemistry (12.05.2011)
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Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway
Castanedo, Georgette M., Wang, Shumei, Robarge, Kirk D., Blackwood, Elizabeth, Burdick, Daniel, Chang, Christine, Dijkgraaf, Gerrit J.P., Gould, Stephen, Gunzner, Janet, Guichert, Oivin, Halladay, Jason, Khojasteh, Cyrus, Lee, Leslie, Marsters, James C., Murray, Lesley, Peterson, David, Plise, Emile, Salphati, Laurent, de Sauvage, Frederic J., Wong, Susan, Sutherlin, Daniel P.
Published in Bioorganic & medicinal chemistry letters (15.11.2010)
Published in Bioorganic & medicinal chemistry letters (15.11.2010)
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A Selective, Slow Binding Inhibitor of Factor VIIa Binds to a Nonstandard Active Site Conformation and Attenuates Thrombus Formation in Vivo
Olivero, Alan G., Eigenbrot, Charles, Goldsmith, Richard, Robarge, Kirk, Artis, Dean R., Flygare, John, Rawson, Thomas, Sutherlin, Daniel P., Kadkhodayan, Saloumeh, Beresini, Maureen, Elliott, Linda O., DeGuzman, Geralyn G., Banner, David W., Ultsch, Mark, Marzec, Ulla, Hanson, Stephen R., Refino, Canio, Bunting, Stuart, Kirchhofer, Daniel
Published in The Journal of biological chemistry (11.03.2005)
Published in The Journal of biological chemistry (11.03.2005)
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From Peptide to Non-Peptide. 3. Atropisomeric GPIIbIIIa Antagonists Containing the 3,4-Dihydro-1H-1,4-benzodiazepine-2,5-dione Nucleus
Blackburn, Brent K, Lee, Arthur, Baier, Mark, Kohl, Benjamin, Olivero, Alan G, Matamoros, Regina, Robarge, Kirk D, McDowell, Robert S
Published in Journal of medicinal chemistry (28.02.1997)
Published in Journal of medicinal chemistry (28.02.1997)
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From Peptide to Non-Peptide. 2. The de Novo Design of Potent, Non-peptidal Inhibitors of Platelet Aggregation Based on a Benzodiazepinedione Scaffold
McDowell, Robert S, Blackburn, Brent K, Gadek, Thomas R, McGee, Lawrence R, Rawson, Thomas, Reynolds, Mark E, Robarge, Kirk D, Somers, Todd C, Thorsett, Eugene D
Published in Journal of the American Chemical Society (01.06.1994)
Published in Journal of the American Chemical Society (01.06.1994)
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Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase
Wei, BinQing, Robarge, Kirk, Labadie, Sharada S., Chen, Jinhua, Corson, Laura B., DiPasquale, Antonio, Dragovich, Peter S., Eigenbrot, Charles, Evangelista, Marie, Fauber, Benjamin P., Hitz, Anna, Hong, Rebecca, Lai, Kwong Wah, Liu, Wenfeng, Ma, Shuguang, Malek, Shiva, O'Brien, Thomas, Pang, Jodie, Peterson, David, Salphati, Laurent, Sampath, Deepak, Sideris, Steven, Ultsch, Mark, Xu, Zijin, Yen, Ivana, Yu, Dong, Yue, Qin, Zhou, Aihe, Purkey, Hans E.
Published in Bioorganic & medicinal chemistry letters (19.01.2022)
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Published in Bioorganic & medicinal chemistry letters (19.01.2022)
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Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase
Wei, BinQing, Robarge, Kirk, Labadie, Sharada S., Chen, Jinhua, Corson, Laura B., DiPasquale, Antonio, Dragovich, Peter S., Eigenbrot, Charles, Evangelista, Marie, Fauber, Benjamin P., Hitz, Anna, Hong, Rebecca, Lai, Kwong Wah, Liu, Wenfeng, Ma, Shuguang, Malek, Shiva, O'Brien, Thomas, Pang, Jodie, Peterson, David, Salphati, Laurent, Sampath, Deepak, Sideris, Steven, Ultsch, Mark, Xu, Zijin, Yen, Ivana, Yu, Dong, Yue, Qin, Zhou, Aihe, Purkey, Hans E.
Published in Bioorganic & medicinal chemistry letters (01.03.2022)
Published in Bioorganic & medicinal chemistry letters (01.03.2022)
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Pharmacokinetics, pharmacodynamics and tolerability of a potent, non-peptidic, GP IIb/IIIa receptor antagonist following multiple oral administrations of a prodrug form
Refino, C J, Modi, N B, Bullens, S, Pater, C, Lipari, M T, Robarge, K, Blackburn, B, Beresini, M, Weller, T, Steiner, B, Bunting, S
Published in Thrombosis and haemostasis (01.01.1998)
Published in Thrombosis and haemostasis (01.01.1998)
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Discovery and preclinical development of vismodegib
Gould, Stephen E, Low, Jennifer A, Marsters, Jr, James C, Robarge, Kirk, Rubin, Lee L, de Sauvage, Frederic J, Sutherlin, Daniel P, Wong, Harvey, Yauch, Robert L
Published in Expert opinion on drug discovery (01.08.2014)
Published in Expert opinion on drug discovery (01.08.2014)
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Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice
Purkey, Hans E, Robarge, Kirk, Chen, Jinhua, Chen, Zhongguo, Corson, Laura B, Ding, Charles Z, DiPasquale, Antonio G, Dragovich, Peter S, Eigenbrot, Charles, Evangelista, Marie, Fauber, Benjamin P, Gao, Zhenting, Ge, Hongxiu, Hitz, Anna, Ho, Qunh, Labadie, Sharada S, Lai, Kwong Wah, Liu, Wenfeng, Liu, Yajing, Li, Chiho, Ma, Shuguang, Malek, Shiva, O’Brien, Thomas, Pang, Jodie, Peterson, David, Salphati, Laurent, Sideris, Steve, Ultsch, Mark, Wei, BinQing, Yen, Ivana, Yue, Qin, Zhang, Huihui, Zhou, Aihe
Published in ACS medicinal chemistry letters (13.10.2016)
Published in ACS medicinal chemistry letters (13.10.2016)
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Discovery of (S)‑1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl‑1H‑pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)‑one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development
Blake, James F, Burkard, Michael, Chan, Jocelyn, Chen, Huifen, Chou, Kang-Jye, Diaz, Dolores, Dudley, Danette A, Gaudino, John J, Gould, Stephen E, Grina, Jonas, Hunsaker, Thomas, Liu, Lichuan, Martinson, Matthew, Moreno, David, Mueller, Lars, Orr, Christine, Pacheco, Patricia, Qin, Ann, Rasor, Kevin, Ren, Li, Robarge, Kirk, Shahidi-Latham, Sheerin, Stults, Jeffrey, Sullivan, Francis, Wang, Weiru, Yin, Jianping, Zhou, Aihe, Belvin, Marcia, Merchant, Mark, Moffat, John, Schwarz, Jacob B
Published in Journal of medicinal chemistry (23.06.2016)
Published in Journal of medicinal chemistry (23.06.2016)
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