Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors
Wilson, Timothy R., Fridlyand, Jane, Yan, Yibing, Penuel, Elicia, Burton, Luciana, Chan, Emily, Peng, Jing, Lin, Eva, Wang, Yulei, Sosman, Jeff, Ribas, Antoni, Li, Jiang, Moffat, John, Sutherlin, Daniel P., Koeppen, Hartmut, Merchant, Mark, Neve, Richard, Settleman, Jeff
Published in Nature (London) (26.07.2012)
Published in Nature (London) (26.07.2012)
Get full text
Journal Article
Fibroblast Activation Protein Cleaves and Inactivates Fibroblast Growth Factor 21
Dunshee, Diana Ronai, Bainbridge, Travis W., Kljavin, Noelyn M., Zavala-Solorio, Jose, Schroeder, Amy C., Chan, Ruby, Corpuz, Racquel, Wong, Manda, Zhou, Wei, Deshmukh, Gauri, Ly, Justin, Sutherlin, Daniel P., Ernst, James A., Sonoda, Junichiro
Published in The Journal of biological chemistry (11.03.2016)
Published in The Journal of biological chemistry (11.03.2016)
Get full text
Journal Article
Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer
Sutherlin, Daniel P, Sampath, Deepak, Berry, Megan, Castanedo, Georgette, Chang, Zhigang, Chuckowree, Irina, Dotson, Jenna, Folkes, Adrian, Friedman, Lori, Goldsmith, Richard, Heffron, Tim, Lee, Leslie, Lesnick, John, Lewis, Cristina, Mathieu, Simon, Nonomiya, Jim, Olivero, Alan, Pang, Jodie, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Tian, Qingping, Tsui, Vickie, Wan, Nan Chi, Wang, Shumei, Wiesmann, Christian, Wong, Susan, Zhu, Bing-Yan
Published in Journal of medicinal chemistry (11.02.2010)
Published in Journal of medicinal chemistry (11.02.2010)
Get full text
Journal Article
Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain
Bankar, Girish, Goodchild, Samuel J., Howard, Sarah, Nelkenbrecher, Karen, Waldbrook, Matthew, Dourado, Michelle, Shuart, Noah G., Lin, Sophia, Young, Clint, Xie, Zhiwei, Khakh, Kuldip, Chang, Elaine, Sojo, Luis E., Lindgren, Andrea, Chowdhury, Sultan, Decker, Shannon, Grimwood, Michael, Andrez, Jean-Christophe, Dehnhardt, Christoph M., Pang, Jodie, Chang, Jae H., Safina, Brian S., Sutherlin, Daniel P., Johnson, James P., Hackos, David H., Robinette, C. Lee, Cohen, Charles J.
Published in Cell reports (Cambridge) (18.09.2018)
Published in Cell reports (Cambridge) (18.09.2018)
Get full text
Journal Article
Activation of caspases-8 and -10 by FLIPL
BOATRIGHT, Kelly M., DEIS, Cristina, DENAULT, Jean-Bernard, SUTHERLIN, Daniel P., SALVESEN, Guy S.
Published in Biochemical journal (01.09.2004)
Published in Biochemical journal (01.09.2004)
Get full text
Journal Article
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor
Heffron, Timothy P., Berry, Megan, Castanedo, Georgette, Chang, Christine, Chuckowree, Irina, Dotson, Jennafer, Folkes, Adrian, Gunzner, Janet, Lesnick, John D., Lewis, Cristina, Mathieu, Simon, Nonomiya, Jim, Olivero, Alan, Pang, Jodie, Peterson, David, Salphati, Laurent, Sampath, Deepak, Sideris, Steve, Sutherlin, Daniel P., Tsui, Vickie, Wan, Nan Chi, Wang, Shumei, Wong, Susan, Zhu, Bing-yan
Published in Bioorganic & medicinal chemistry letters (15.04.2010)
Published in Bioorganic & medicinal chemistry letters (15.04.2010)
Get full text
Journal Article
Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist
Ahuja, Shivani, Mukund, Susmith, Deng, Lunbin, Khakh, Kuldip, Chang, Elaine, Ho, Hoangdung, Shriver, Stephanie, Young, Clint, Lin, Sophia, Johnson, J. P., Wu, Ping, Li, Jun, Coons, Mary, Tam, Christine, Brillantes, Bobby, Sampang, Honorio, Mortara, Kyle, Bowman, Krista K., Clark, Kevin R., Estevez, Alberto, Xie, Zhiwei, Verschoof, Henry, Grimwood, Michael, Dehnhardt, Christoph, Andrez, Jean–Christophe, Focken, Thilo, Sutherlin, Daniel P., Safina, Brian S., Starovasnik, Melissa A., Ortwine, Daniel F., Franke, Yvonne, Cohen, Charles J., Hackos, David H., Koth, Christopher M., Payandeh, Jian
Published in Science (American Association for the Advancement of Science) (18.12.2015)
Published in Science (American Association for the Advancement of Science) (18.12.2015)
Get full text
Journal Article
Activation and Substrate Specificity of Caspase-14
Mikolajczyk, Jowita, Scott, Fiona L, Krajewski, Stan, Sutherlin, Daniel P, Salvesen, Guy S
Published in Biochemistry (Easton) (17.08.2004)
Published in Biochemistry (Easton) (17.08.2004)
Get full text
Journal Article
GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway
Wallin, Jeffrey J, Edgar, Kyle A, Guan, Jane, Berry, Megan, Prior, Wei Wei, Lee, Leslie, Lesnick, John D, Lewis, Cristina, Nonomiya, Jim, Pang, Jodie, Salphati, Laurent, Olivero, Alan G, Sutherlin, Daniel P, O'Brien, Carol, Spoerke, Jill M, Patel, Sonal, Lensun, Letitia, Kassees, Robert, Ross, Leanne, Lackner, Mark R, Sampath, Deepak, Belvin, Marcia, Friedman, Lori S
Published in Molecular cancer therapeutics (01.12.2011)
Published in Molecular cancer therapeutics (01.12.2011)
Get full text
Journal Article
Discovery of a Potent, Selective, and Orally Available Class I Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor (GDC-0980) for the Treatment of Cancer
Sutherlin, Daniel P, Bao, Linda, Berry, Megan, Castanedo, Georgette, Chuckowree, Irina, Dotson, Jenna, Folks, Adrian, Friedman, Lori, Goldsmith, Richard, Gunzner, Janet, Heffron, Timothy, Lesnick, John, Lewis, Cristina, Mathieu, Simon, Murray, Jeremy, Nonomiya, Jim, Pang, Jodie, Pegg, Niel, Prior, Wei Wei, Rouge, Lionel, Salphati, Laurent, Sampath, Deepak, Tian, Qingping, Tsui, Vickie, Wan, Nan Chi, Wang, Shumei, Wei, BinQing, Wiesmann, Christian, Wu, Ping, Zhu, Bing-Yan, Olivero, Alan
Published in Journal of medicinal chemistry (10.11.2011)
Published in Journal of medicinal chemistry (10.11.2011)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain
McKerrall, Steven J, Nguyen, Teresa, Lai, Kwong Wah, Bergeron, Philippe, Deng, Lunbin, DiPasquale, Antonio, Chang, Jae H, Chen, Jun, Chernov-Rogan, Tania, Hackos, David H, Maher, Jonathan, Ortwine, Daniel F, Pang, Jodie, Payandeh, Jian, Proctor, William R, Shields, Shannon D, Vogt, Jennifer, Ji, Pengfei, Liu, Wenfeng, Ballini, Elisa, Schumann, Lilia, Tarozzo, Glauco, Bankar, Girish, Chowdhury, Sultan, Hasan, Abid, Johnson, J. P, Khakh, Kuldip, Lin, Sophia, Cohen, Charles J, Dehnhardt, Christoph M, Safina, Brian S, Sutherlin, Daniel P
Published in Journal of medicinal chemistry (25.04.2019)
Published in Journal of medicinal chemistry (25.04.2019)
Get full text
Journal Article
Identification of Selective Acyl Sulfonamide–Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (NaV) 1.7 with Potent Analgesic Activity
Sun, Shaoyi, Jia, Qi, Zenova, Alla Y, Wilson, Michael S, Chowdhury, Sultan, Focken, Thilo, Li, Jun, Decker, Shannon, Grimwood, Michael E, Andrez, Jean-Christophe, Hemeon, Ivan, Sheng, Tao, Chen, Chien-An, White, Andy, Hackos, David H, Deng, Lunbin, Bankar, Girish, Khakh, Kuldip, Chang, Elaine, Kwan, Rainbow, Lin, Sophia, Nelkenbrecher, Karen, Sellers, Benjamin D, DiPasquale, Antonio G, Chang, Jae, Pang, Jodie, Sojo, Luis, Lindgren, Andrea, Waldbrook, Matthew, Xie, Zhiwei, Young, Clint, Johnson, James P, Robinette, C. Lee, Cohen, Charles J, Safina, Brian S, Sutherlin, Daniel P, Ortwine, Daniel F, Dehnhardt, Christoph M
Published in Journal of medicinal chemistry (24.01.2019)
Published in Journal of medicinal chemistry (24.01.2019)
Get full text
Journal Article
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNa V 1.7 Inhibitors for the Treatment of Pain
Focken, Thilo, Chowdhury, Sultan, Zenova, Alla, Grimwood, Michael E, Chabot, Christine, Sheng, Tao, Hemeon, Ivan, Decker, Shannon M, Wilson, Michael, Bichler, Paul, Jia, Qi, Sun, Shaoyi, Young, Clint, Lin, Sophia, Goodchild, Samuel J, Shuart, Noah G, Chang, Elaine, Xie, Zhiwei, Li, Bowen, Khakh, Kuldip, Bankar, Girish, Waldbrook, Matthew, Kwan, Rainbow, Nelkenbrecher, Karen, Karimi Tari, Parisa, Chahal, Navjot, Sojo, Luis, Robinette, C Lee, White, Andrew D, Chen, Chien-An, Zhang, Yi, Pang, Jodie, Chang, Jae H, Hackos, David H, Johnson, Jr, J P, Cohen, Charles J, Ortwine, Daniel F, Sutherlin, Daniel P, Dehnhardt, Christoph M, Safina, Brian S
Published in Journal of medicinal chemistry (14.06.2018)
Published in Journal of medicinal chemistry (14.06.2018)
Get full text
Journal Article
Discovery of Acyl-sulfonamide Nav1.7 Inhibitors GDC-0276 and GDC-0310
Safina, Brian S, McKerrall, Steven J, Sun, Shaoyi, Chen, Chien-An, Chowdhury, Sultan, Jia, Qi, Li, Jun, Zenova, Alla Y, Andrez, Jean-Christophe, Bankar, Girish, Bergeron, Philippe, Chang, Jae H, Chang, Elaine, Chen, Jun, Dean, Richard, Decker, Shannon M, DiPasquale, Antonio, Focken, Thilo, Hemeon, Ivan, Khakh, Kuldip, Kim, Amy, Kwan, Rainbow, Lindgren, Andrea, Lin, Sophia, Maher, Jonathan, Mezeyova, Janette, Misner, Dinah, Nelkenbrecher, Karen, Pang, Jodie, Reese, Rebecca, Shields, Shannon D, Sojo, Luis, Sheng, Tao, Verschoof, Henry, Waldbrook, Matthew, Wilson, Michael S, Xie, Zhiwei, Young, Clint, Zabka, Tanja S, Hackos, David H, Ortwine, Daniel F, White, Andrew D, Johnson, J.P, Robinette, C. Lee, Dehnhardt, Christoph M, Cohen, Charles J, Sutherlin, Daniel P
Published in Journal of medicinal chemistry (25.03.2021)
Published in Journal of medicinal chemistry (25.03.2021)
Get full text
Journal Article
Nav1.7 inhibitors for the treatment of chronic pain
McKerrall, Steven J., Sutherlin, Daniel P.
Published in Bioorganic & medicinal chemistry letters (15.10.2018)
Published in Bioorganic & medicinal chemistry letters (15.10.2018)
Get full text
Journal Article
A Unified Model for Apical Caspase Activation
Boatright, Kelly M, Renatus, Martin, Scott, Fiona L, Sperandio, Sabina, Shin, Hwain, Pedersen, Irene M, Ricci, Jean-Ehrland, Edris, Wade A, Sutherlin, Daniel P, Green, Douglas R, Salvesen, Guy S
Published in Molecular cell (01.02.2003)
Published in Molecular cell (01.02.2003)
Get full text
Journal Article
Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform
Heffron, Timothy P, Wei, BinQing, Olivero, Alan, Staben, Steven T, Tsui, Vickie, Do, Steven, Dotson, Jennafer, Folkes, Adrian J, Goldsmith, Paul, Goldsmith, Richard, Gunzner, Janet, Lesnick, John, Lewis, Cristina, Mathieu, Simon, Nonomiya, Jim, Shuttleworth, Stephen, Sutherlin, Daniel P, Wan, Nan Chi, Wang, Shumei, Wiesmann, Christian, Zhu, Bing-Yan
Published in Journal of medicinal chemistry (24.11.2011)
Published in Journal of medicinal chemistry (24.11.2011)
Get full text
Journal Article