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)
Get full text
Journal Article
Structural basis for dual-mode inhibition of the ABC transporter MsbA
Ho, Hoangdung, Miu, Anh, Alexander, Mary Kate, Garcia, Natalie K., Oh, Angela, Zilberleyb, Inna, Reichelt, Mike, Austin, Cary D., Tam, Christine, Shriver, Stephanie, Hu, Huiyong, Labadie, Sharada S., Liang, Jun, Wang, Lan, Wang, Jian, Lu, Yan, Purkey, Hans E., Quinn, John, Franke, Yvonne, Clark, Kevin, Beresini, Maureen H., Tan, Man-Wah, Sellers, Benjamin D., Maurer, Till, Koehler, Michael F. T., Wecksler, Aaron T., Kiefer, James R., Verma, Vishal, Xu, Yiming, Nishiyama, Mireille, Payandeh, Jian, Koth, Christopher M.
Published in Nature (London) (01.05.2018)
Published in Nature (London) (01.05.2018)
Get full text
Journal Article
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα
Hanan, Emily J., Braun, Marie-Gabrielle, Heald, Robert A., MacLeod, Calum, Chan, Connie, Clausen, Saundra, Edgar, Kyle A., Eigenbrot, Charles, Elliott, Richard, Endres, Nicholas, Friedman, Lori S., Gogol, Emily, Gu, Xiao-Hui, Thibodeau, Rebecca Hong, Jackson, Philip S., Kiefer, James R., Knight, Jamie D., Nannini, Michelle, Narukulla, Raman, Pace, Amanda, Pang, Jodie, Purkey, Hans E., Salphati, Laurent, Sampath, Deepak, Schmidt, Stephen, Sideris, Steve, Song, Kyung, Sujatha-Bhaskar, Swathi, Ultsch, Mark, Wallweber, Heidi, Xin, Jianfeng, Yeap, SiewKuen, Young, Amy, Zhong, Yu, Staben, Steven T.
Published in Journal of medicinal chemistry (22.12.2022)
Published in Journal of medicinal chemistry (22.12.2022)
Get full text
Journal Article
Overall survival in patients with advanced non-small cell lung cancer with KRAS G12C mutation with or without STK11 and/or KEAP1 mutations in a real-world setting
Julian, Cristina, Pal, Navdeep, Gershon, Anda, Evangelista, Marie, Purkey, Hans, Lambert, Peter, Shi, Zhen, Zhang, Qing
Published in BMC cancer (17.04.2023)
Published in BMC cancer (17.04.2023)
Get full text
Journal Article
Assessment of KRAS G12C Target Engagement by a Covalent Inhibitor in Tumor Biopsies Using an Ultra-Sensitive Immunoaffinity 2D-LC–MS/MS Approach
Meng, Lingyao, Chan, Emily W., Ng, Carl, Aimi, Junko, Tran, John C., Oh, Angela J., Merchant, Mark, Purkey, Hans E., Heffron, Timothy P., Kaur, Surinder, Xu, Keyang, Shi, Zhen, He, Jintang
Published in Analytical chemistry (Washington) (20.09.2022)
Published in Analytical chemistry (Washington) (20.09.2022)
Get full text
Journal Article
Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability
Ladi, Ena, Everett, Christine, Stivala, Craig E, Daniels, Blake E, Durk, Matthew R, Harris, Seth F, Huestis, Malcolm P, Purkey, Hans E, Staben, Steven T, Augustin, Martin, Blaesse, Michael, Steinbacher, Stefan, Eidenschenk, Celine, Pappu, Rajita, Siu, Michael
Published in Journal of medicinal chemistry (08.08.2019)
Published in Journal of medicinal chemistry (08.08.2019)
Get full text
Journal Article
Disrupting Gram-Negative Bacterial Outer Membrane Biosynthesis through Inhibition of the Lipopolysaccharide Transporter MsbA
Alexander, Mary Kate, Miu, Anh, Oh, Angela, Reichelt, Mike, Ho, Hoangdung, Chalouni, Cecile, Labadie, Sharada, Wang, Lan, Liang, Jun, Nickerson, Nicholas N, Hu, Huiyong, Yu, Lan, Du, Miaofen, Yan, Donghong, Park, Summer, Kim, Janice, Xu, Min, Sellers, Benjamin D, Purkey, Hans E, Skelton, Nicholas J, Koehler, Michael F T, Payandeh, Jian, Verma, Vishal, Xu, Yiming, Koth, Christopher M, Nishiyama, Mireille
Published in Antimicrobial agents and chemotherapy (01.11.2018)
Published in Antimicrobial agents and chemotherapy (01.11.2018)
Get full text
Journal Article
Quantifying KRAS G12C Covalent Drug Inhibitor Activity in Mouse Tumors Using Mass Spectrometry
Tran, John C., Hunsaker, Thomas, Bell, Christina, Ma, Taylur P., Chan, Emily, Larrocha, Pablo Saenz-Lopez, Homyk, Kelsey, Liu, Liling, La, Hank, Mao, Jialin, de la Cruz, Cecile C., Yu, Kebing, Beresini, Maureen, Forrest, William F., Xiao, Yang, Jang, Anne, Samus, Natalia, Stesco, Nicholas Dupuis, Mentinova, Marija, Parent, Stephane, Pottiez, Gwenael, Schirm, Michael, Purkey, Hans E., Liu, Yichin, Merchant, Mark
Published in Analytical chemistry (Washington) (21.03.2023)
Published in Analytical chemistry (Washington) (21.03.2023)
Get full text
Journal Article
Discovery of a Potent and Selective BCL‑XL Inhibitor with in Vivo Activity
Tao, Zhi-Fu, Hasvold, Lisa, Wang, Le, Wang, Xilu, Petros, Andrew M, Park, Chang H, Boghaert, Erwin R, Catron, Nathaniel D, Chen, Jun, Colman, Peter M, Czabotar, Peter E, Deshayes, Kurt, Fairbrother, Wayne J, Flygare, John A, Hymowitz, Sarah G, Jin, Sha, Judge, Russell A, Koehler, Michael F. T, Kovar, Peter J, Lessene, Guillaume, Mitten, Michael J, Ndubaku, Chudi O, Nimmer, Paul, Purkey, Hans E, Oleksijew, Anatol, Phillips, Darren C, Sleebs, Brad E, Smith, Brian J, Smith, Morey L, Tahir, Stephen K, Watson, Keith G, Xiao, Yu, Xue, John, Zhang, Haichao, Zobel, Kerry, Rosenberg, Saul H, Tse, Chris, Leverson, Joel D, Elmore, Steven W, Souers, Andrew J
Published in ACS medicinal chemistry letters (09.10.2014)
Published in ACS medicinal chemistry letters (09.10.2014)
Get full text
Journal Article
Conformation-locking antibodies for the discovery and characterization of KRAS inhibitors
Davies, Christopher W., Oh, Angela J., Mroue, Rana, Steffek, Micah, Bruning, John M., Xiao, Yang, Feng, Siyu, Jayakar, Sangeeta, Chan, Emily, Arumugam, Vidhyalakshmi, Uribe, Sean Carlo, Drummond, Jake, Frommlet, Alexandra, Lu, Cheng, Franke, Yvonne, Merchant, Mark, Koeppen, Hartmut, Quinn, John G., Malhotra, Sushant, Do, Steve, Gazzard, Lewis, Purkey, Hans E., Rudolph, Joachim, Mulvihill, Melinda M., Koerber, James T., Wang, Weiru, Evangelista, Marie
Published in Nature biotechnology (01.05.2022)
Published in Nature biotechnology (01.05.2022)
Get full text
Journal Article
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase
Hanan, Emily J., Baumgardner, Matt, Bryan, Marian C., Chen, Yuan, Eigenbrot, Charles, Fan, Peter, Gu, Xiao-Hui, La, Hank, Malek, Shiva, Purkey, Hans E., Schaefer, Gabriele, Schmidt, Stephen, Sideris, Steve, Yen, Ivana, Yu, Christine, Heffron, Timothy P.
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
Get full text
Journal Article
Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase
Dragovich, Peter S., Fauber, Benjamin P., Corson, Laura B., Ding, Charles Z., Eigenbrot, Charles, Ge, HongXiu, Giannetti, Anthony M., Hunsaker, Thomas, Labadie, Sharada, Liu, Yichin, Malek, Shiva, Pan, Borlan, Peterson, David, Pitts, Keith, Purkey, Hans E., Sideris, Steve, Ultsch, Mark, VanderPorten, Erica, Wei, BinQing, Xu, Qing, Yen, Ivana, Yue, Qin, Zhang, Huihui, Zhang, Xuying
Published in Bioorganic & medicinal chemistry letters (01.06.2013)
Published in Bioorganic & medicinal chemistry letters (01.06.2013)
Get full text
Journal Article
Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation
Hanan, Emily J, Eigenbrot, Charles, Bryan, Marian C, Burdick, Daniel J, Chan, Bryan K, Chen, Yuan, Dotson, Jennafer, Heald, Robert A, Jackson, Philip S, La, Hank, Lainchbury, Michael D, Malek, Shiva, Purkey, Hans E, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen M, Sideris, Steve, Tam, Christine, Wang, Shumei, Yeap, Siew Kuen, Yen, Ivana, Yin, Jianping, Yu, Christine, Zilberleyb, Inna, Heffron, Timothy P
Published in Journal of medicinal chemistry (11.12.2014)
Published in Journal of medicinal chemistry (11.12.2014)
Get full text
Journal Article
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)
Get full text
Journal Article
Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor
Chan, Bryan K, Hanan, Emily J, Bowman, Krista K, Bryan, Marian C, Burdick, Daniel, Chan, Emily, Chen, Yuan, Clausen, Saundra, Dela Vega, Trisha, Dotson, Jennafer, Eigenbrot, Charles, Elliott, Richard L, Heald, Robert A, Jackson, Philip S, Knight, Jamie D, La, Hank, Lainchbury, Michael D, Malek, Shiva, Purkey, Hans E, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen M, Sideris, Steve, Shao, Lily, Wang, Shumei, Yeap, Siew Kuen, Yen, Ivana, Yu, Christine, Heffron, Timothy P
Published in Journal of medicinal chemistry (13.10.2016)
Published in Journal of medicinal chemistry (13.10.2016)
Get full text
Journal Article
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)
Get full text
Journal Article
Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase
Dragovich, Peter S., Fauber, Benjamin P., Boggs, Jason, Chen, Jinhua, Corson, Laura B., Ding, Charles Z., Eigenbrot, Charles, Ge, HongXiu, Giannetti, Anthony M., Hunsaker, Thomas, Labadie, Sharada, Li, Chiho, Liu, Yichin, Liu, Yingchun, Ma, Shuguang, Malek, Shiva, Peterson, David, Pitts, Keith E., Purkey, Hans E., Robarge, Kirk, Salphati, Laurent, Sideris, Steve, Ultsch, Mark, VanderPorten, Erica, Wang, Jing, Wei, BinQing, Xu, Qing, Yen, Ivana, Yue, Qin, Zhang, Huihui, Zhang, Xuying, Zhou, Aihe
Published in Bioorganic & medicinal chemistry letters (15.08.2014)
Published in Bioorganic & medicinal chemistry letters (15.08.2014)
Get full text
Journal Article
Benzoxazoles as Transthyretin Amyloid Fibril Inhibitors: Synthesis, Evaluation, and Mechanism of Action
Razavi, Hossein, Palaninathan, Satheesh K., Powers, Evan T., Wiseman, R. Luke, Purkey, Hans E., Mohamedmohaideen, Nilofar N., Deechongkit, Songpon, Chiang, Kyle P., Dendle, Maria T. A., Sacchettini, James C., Kelly, Jeffery W.
Published in Angewandte Chemie International Edition (23.06.2003)
Published in Angewandte Chemie International Edition (23.06.2003)
Get full text
Journal Article
Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase
Fauber, Benjamin P., Dragovich, Peter S., Chen, Jinhua, Corson, Laura B., Ding, Charles Z., Eigenbrot, Charles, Labadie, Sharada, Malek, Shiva, Peterson, David, Purkey, Hans E., Robarge, Kirk, Sideris, Steve, Ultsch, Mark, Wei, BinQing, Yen, Ivana, Yue, Qin, Zhou, Aihe
Published in Bioorganic & medicinal chemistry letters (15.12.2014)
Published in Bioorganic & medicinal chemistry letters (15.12.2014)
Get full text
Journal Article
Discovery of 7‑Tetrahydropyran-2-yl Chromans: β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors That Reduce Amyloid β‑Protein (Aβ) in the Central Nervous System
Thomas, Allen A, Hunt, Kevin W, Volgraf, Matthew, Watts, Ryan J, Liu, Xingrong, Vigers, Guy, Smith, Darin, Sammond, Douglas, Tang, Tony P, Rhodes, Susan P, Metcalf, Andrew T, Brown, Karin D, Otten, Jennifer N, Burkard, Michael, Cox, April A, Do, Mary K. Geck, Dutcher, Darrin, Rana, Sumeet, DeLisle, Robert K, Regal, Kelly, Wright, Albion D, Groneberg, Robert, Scearce-Levie, Kimberly, Siu, Michael, Purkey, Hans E, Lyssikatos, Joseph P, Gunawardana, Indrani W
Published in Journal of medicinal chemistry (13.02.2014)
Published in Journal of medicinal chemistry (13.02.2014)
Get full text
Journal Article