Not logged in 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. Share Save
Structures of the ApoL1 and ApoL2 N-terminal domains reveal a non-classical four-helix bundle motif Ultsch, Mark; Holliday, Michael J.; Gerhardy, Stefan; Moran, Paul; Scales, Suzie J.; Gupta, Nidhi; Oltrabella, Francesca; Chiu, Cecilia; Fairbrother, Wayne; Eigenbrot, Charles; Kirchhofer, Daniel Share Save
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor Huestis, Malcolm P.; Dela Cruz, Darlene; DiPasquale, Antonio G.; Durk, Matthew R.; Eigenbrot, Charles; Gibbons, Paul; Gobbi, Alberto; Hunsaker, Thomas L.; La, Hank; Leung, Dennis H.; Liu, Wendy; Malek, Shiva; Merchant, Mark; Moffat, John G.; Muli, Christine S.; Orr, Christine J.; Parr, Brendan T.; Shanahan, Frances; Sneeringer, Christopher J.; Wang, Weiru; Yen, Ivana; Yin, Jianping; Siu, Michael; Rudolph, Joachim Share Save
Bivalent antibody pliers inhibit β-tryptase by an allosteric mechanism dependent on the IgG hinge Maun, Henry R.; Vij, Rajesh; Walters, Benjamin T.; Morando, Ashley; Jackman, Janet K.; Wu, Ping; Estevez, Alberto; Chen, Xiaocheng; Franke, Yvonne; Lipari, Michael T.; Dennis, Mark S.; Kirchhofer, Daniel; Ciferri, Claudio; Loyet, Kelly M.; Yi, Tangsheng; Eigenbrot, Charles; Lazarus, Robert A.; Koerber, James T. Share Save
Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity Crawford, James J.; Lee, Wendy; Johnson, Adam R.; Delatorre, Kelly J.; Chen, Jacob; Eigenbrot, Charles; Heidmann, Julia; Kakiuchi-Kiyota, Satoko; Katewa, Arna; Kiefer, James R.; Liu, Lichuan; Lubach, Joseph W.; Misner, Dinah; Purkey, Hans; Reif, Karin; Vogt, Jennifer; Wong, Harvey; Yu, Christine; Young, Wendy B. Share Save
Design of Organo-Peptides As Bipartite PCSK9 Antagonists Burdick, Daniel J.; Skelton, Nicholas J.; Ultsch, Mark; Beresini, Maureen H.; Eigenbrot, Charles; Li, Wei; Zhang, Yingnan; Huy Nguyen; Kong-Beltran, Monica; Quinn, John G.; Kirchhofer, Daniel Share Save
Water molecules in protein-ligand interfaces. Evaluation of software tools and SAR comparison Nittinger, Eva; Gibbons, Paul; Eigenbrot, Charles; Davies, Doug R.; Maurer, Brigitte; Yu, Christine L.; Kiefer, James R.; Kuglstatter, Andreas; Murray, Jeremy; Ortwine, Daniel F.; Tang, Yong; Tsui, Vickie Share Save
Share Save
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development Crawford, James J. y; Johnson, Adam R.; Misner, Dinah L.; Belmont, Lisa D.; Castanedo, Georgette; Choy, Regina; Coraggio, Melis; Doug, Liming; Eigenbrot, Charles; Erickson, Rebecca; Ghilardi, Nico; Hau, Jonathan; Katewa, Arna; Kohli, Pawan Bir; Lee, Wendy; Lubach, Joseph W.; McKenzie, Brent S.; Ortwine, Daniel F.; Schutt, Leah; Tay, Suzanne; Wei, BinQing; Reif, Karin; Liu, Lichuan; Wong, Harvey; Young, Wendy B. Share Save
Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity Wei, BinQing; Gunzner-Toste, Janet; Yao, Hui; Wang, Tao; Wang, Jing; Xu, Zijin; Chen, Jinhua; Wai, John; Nonomiya, Jim; Tsai, Siao Ping; Chuh, Josefa; Kozak, Katherine R.; Liu, Yichin; Yu, Shang-Fan; Lau, Jeff; Li, Guangmin; Phillips, Gail D.; Leipold, Doug; Kamath, Amrita; Su, Dian; Xu, Keyang; Eigenbrot, Charles; Steinbacher, Stefan; Ohri, Rachana; Raab, Helga; Staben, Leanna R.; Zhao, Guiling; Flygare, John A.; Pillow, Thomas H.; Verma, Vishal; Masterson, Luke A.; Howard, Philip W.; Safina, Brian Share Save
Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists Zhang, Yingnan; Ultsch, Mark; Skelton, Nicholas J.; Burdick, Daniel J.; Beresini, Maureen H.; Li, Wei; Kong-Beltran, Monica; Peterson, Andrew; Quinn, John; Chiu, Cecilia; Wu, Yan; Shia, Steven; Moran, Paul; Di Lello, Paola; Eigenbrot, Charles; Kirchhofer, Daniel Share Save
Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties Wang, Xiaojing; Barbosa, James; Blomgren, Peter; Bremer, Meire C.; Chen, Jacob; Crawford, James J.; Deng, Wei; Dong, Liming; Eigenbrot, Charles; Gallion, Steve; Hau, Jonathon; Hu, Huiyong; Johnson, Adam R.; Katewa, Arna; Kropf, Jeffrey E.; Lee, Seung H.; Liu, Lichuan; Lubach, Joseph W.; Macaluso, Jen; Maciejewski, Pat; Mitchell, Scott A.; Ortwine, Daniel F.; DiPaolo, Julie; Reif, Karin; Scheerens, Heleen; Schmitt, Aaron; Wong, Harvey; Xiong, Jin-Ming; Xu, Jianjun; Zhao, Zhongdong; Zhou, Fusheng; Currie, Kevin S.; Young, Wendy B. Share Save
Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K) Castanedo, Georgette M.; Blaquiere, Nicole; Beresini, Maureen; Bravo, Brandon; Brightbill, Hans; Chen, Jacob; Cui, Hai-Feng; Eigenbrot, Charles; Everett, Christine; Feng, Jianwen; Godemann, Robert; Gogol, Emily; Hymowitz, Sarah; Johnson, Adam; Kayagald, Nobuhiko; Kohli, Pawan Bir; Knueppel, Kathleen; Kraemer, Joachim; Krueger, Susan; Loke, Pui; McEwan, Paul; Montalbetti, Christian; Roberts, David A.; Smith, Myron; Steinbacher, Stefan; Sujatha-Bhaskar, Swathi; Takahashi, Ryan; Wane, Xiaolu; Wu, Lawren C.; Zhang, Yamin; Staben, Steven T. Share Save
Structure of Crenezumab Complex with Aβ Shows Loss of β-Hairpin Ultsch, Mark; Li, Bing; Maurer, Till; Mathieu, Mary; Adolfsson, Oskar; Muhs, Andreas; Pfeifer, Andrea; Pihlgren, Maria; Bainbridge, Travis W.; Reichelt, Mike; Ernst, James A.; Eigenbrot, Charles; Fuh, Germaine; Atwal, Jasvinder K.; Watts, Ryan J.; Wang, Weiru Share Save
Resolving TYK2 locus genotype-to-phenotype differences in autoimmunity Dendrou, Calliope A.; Cortes, Adrian; Shipman, Lydia; Evans, Hayley G.; Attfield, Kathrine E.; Jostins, Luke; Barber, Thomas; Kaur, Gurman; Kuttikkatte, Subita Balaram; Leach, Oliver A.; Desel, Christiane; Faergeman, Soren L.; Cheeseman, Jane; Neville, Matt J.; Sawcer, Stephen; Compston, Alastair; Johnson, Adam R.; Everett, Christine; Bell, John I.; Karpe, Fredrik; Ultsch, Mark; Eigenbrot, Charles; McVean, Gil; Fugger, Lars Share Save
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. Share Save
Battling Btk Mutants With Noncovalent Inhibitors That Overcome Cys481 and Thr474 Mutations Johnson, Adam R.; Kohli, Pawan Bir; Katewa, Arna; Gogol, Emily; Belmont, Lisa D.; Choy, Regina; Penuel, Elicia; Burton, Luciana; Eigenbrot, Charles; Yu, Christine; Ortwine, Daniel F.; Bowman, Krista; Franke, Yvonne; Tam, Christine; Estevez, Alberto; Mortara, Kyle; Wu, Jiansheng; Li, Hong; Lin, May; Bergeron, Philippe; Crawford, James J.; Young, Wendy B. Share Save
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 Share Save
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 Share Save
Activation mechanism of oncogenic C-helix shifting mutations in BRAF, EGFR, and HER2 Foster, Scott; Whalen, Dan; Ozen, Aysegul; Wongchenko, Matt; Yin, JianPing; Yen, Ivana; Schaefer, Gabriele; Mayfield, John; Chmielecki, Juliann; Stephens, Phil; Albacker, Lee; Yan, Yibing; Song, Kyung; Hatzivassiliou, Georgia; Eigenbrot, Charles; Yu, Christine; Shaw, Andrey; Manning, Gerard; Skelton, Nicholas; Hymowitz, Sarah; Malek, Shiva Share Save
.png){kind=icon}
.png){kind=icon}
.png){kind=icon}
.png){kind=icon}
.png){kind=icon}
Share.png){kind=icon}
Save
Not logged in.png){kind=icon}