Optimized arylomycins are a new class of Gram-negative antibiotics von Smith, Peter A., Koehler, Michael F. T., Girgis, Hany S., Yan, Donghong, Chen, Yongsheng, Chen, Yuan, Crawford, James J., Durk, Matthew R., Higuchi, Robert I., Kang, Jing, Murray, Jeremy, Paraselli, Prasuna, Park, Summer, Phung, Wilson, Quinn, John G., Roberts, Tucker C., Rougé, Lionel, Schwarz, Jacob B., Skippington, Elizabeth, Wai, John, Xu, Min, Yu, Zhiyong, Zhang, Hua, Tan, Man-Wah, Heise, Christopher E.

Volltext

GDC-0449—A potent inhibitor of the hedgehog pathway von 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

Volltext

Potent Killing of Pseudomonas aeruginosa by an Antibody-Antibiotic Conjugate von Kajihara, Kimberly K., Pantua, Homer, Hernandez-Barry, Hilda, Hazen, Meredith, Deshmukh, Kiran, Chiang, Nancy, Ohri, Rachana, Castellanos, Erick R., Martin, Lynn, Matsumoto, Marissa L., Payandeh, Jian, Storek, Kelly M., Schneider, Kellen, Smith, Peter A., Koehler, Michael F. T., Tsai, Siao Ping, Vandlen, Richard, Loyet, Kelly M., Nakamura, Gerald, Pillow, Thomas, Seshasayee, Dhaya, Kapadia, Sharookh B., Hazenbos, Wouter L. W.

Volltext

Disrupting Gram-Negative Bacterial Outer Membrane Biosynthesis through Inhibition of the Lipopolysaccharide Transporter MsbA von 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

Volltext

Discovery of Inhibitors of the Lipopolysaccharide Transporter MsbA: From a Screening Hit to Potent Wild-Type Gram-Negative Activity von Verma, Vishal A, Wang, Lan, Labadie, Sharada S, Liang, Jun, Sellers, Benjamin D, Wang, Jian, Dong, Liting, Wang, Qiuyue, Zhang, Shuang, Xu, Zhongya, Zhang, Yexia, Niu, Yanan, Wang, Xinxin, Wai, John, Koehler, Michael F. T, Hu, Huiyong, Alexander, Mary Kate, Nishiyama, Mireille, Miu, Anh, Xu, Yiming, Pang, Jodie, Katakam, Anand K, Reichelt, Michael, Austin, Cary D, Ho, Hoangdung, Payandeh, Jian, Koth, Christopher M

Volltext

Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells von Koehler, Michael F. T, Bergeron, Philippe, Blackwood, Elizabeth M, Bowman, Krista, Clark, Kevin R, Firestein, Ron, Kiefer, James R, Maskos, Klaus, McCleland, Mark L, Orren, Linda, Salphati, Laurent, Schmidt, Steve, Schneider, Elisabeth V, Wu, Jiansheng, Beresini, Maureen H

Volltext

Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8 von Bergeron, Philippe, Koehler, Michael F. T, Blackwood, Elizabeth M, Bowman, Krista, Clark, Kevin, Firestein, Ron, Kiefer, James R, Maskos, Klaus, McCleland, Mark L, Orren, Linda, Ramaswamy, Sreemathy, Salphati, Laurent, Schmidt, Steve, Schneider, Elisabeth V, Wu, Jiansheng, Beresini, Maureen

Volltext

Identification of C‑2 Hydroxyethyl Imidazopyrrolopyridines as Potent JAK1 Inhibitors with Favorable Physicochemical Properties and High Selectivity over JAK2 von Zak, Mark, Hurley, Christopher A, Ward, Stuart I, Bergeron, Philippe, Barrett, Kathy, Balazs, Mercedesz, Blair, Wade S, Bull, Richard, Chakravarty, Paroma, Chang, Christine, Crackett, Peter, Deshmukh, Gauri, DeVoss, Jason, Dragovich, Peter S, Eigenbrot, Charles, Ellwood, Charles, Gaines, Simon, Ghilardi, Nico, Gibbons, Paul, Gradl, Stefan, Gribling, Peter, Hamman, Chris, Harstad, Eric, Hewitt, Peter, Johnson, Adam, Johnson, Tony, Kenny, Jane R, Koehler, Michael F. T, Bir Kohli, Pawan, Labadie, Sharada, Lee, Wyne P, Liao, Jiangpeng, Liimatta, Marya, Mendonca, Rohan, Narukulla, Raman, Pulk, Rebecca, Reeve, Austin, Savage, Scott, Shia, Steven, Steffek, Micah, Ubhayakar, Savita, van Abbema, Anne, Aliagas, Ignacio, Avitabile-Woo, Barbara, Xiao, Yisong, Yang, Jing, Kulagowski, Janusz J

Volltext

Discovery and Optimization of C-2 Methyl Imidazopyrrolopyridines as Potent and Orally Bioavailable JAK1 Inhibitors with Selectivity over JAK2 von Zak, Mark, Mendonca, Rohan, Balazs, Mercedesz, Barrett, Kathy, Bergeron, Philippe, Blair, Wade S, Chang, Christine, Deshmukh, Gauri, DeVoss, Jason, Dragovich, Peter S, Eigenbrot, Charles, Ghilardi, Nico, Gibbons, Paul, Gradl, Stefan, Hamman, Chris, Hanan, Emily J, Harstad, Eric, Hewitt, Peter R, Hurley, Christopher A, Jin, Tian, Johnson, Adam, Johnson, Tony, Kenny, Jane R, Koehler, Michael F. T, Bir Kohli, Pawan, Kulagowski, Janusz J, Labadie, Sharada, Liao, Jiangpeng, Liimatta, Marya, Lin, Zhonghua, Lupardus, Patrick J, Maxey, Robert J, Murray, Jeremy M, Pulk, Rebecca, Rodriguez, Madeleine, Savage, Scott, Shia, Steven, Steffek, Micah, Ubhayakar, Savita, Ultsch, Mark, van Abbema, Anne, Ward, Stuart I, Xiao, Ling, Xiao, Yisong

Volltext

Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres von Cohen, Frederick, Koehler, Michael F.T., Bergeron, Philippe, Elliott, Linda O., Flygare, John A., Franklin, Matthew C., Gazzard, Lewis, Keteltas, Stephen F., Lau, Kevin, Ly, Cuong Q., Tsui, Vickie, Fairbrother, Wayne J.

Volltext

Quinazoline Sulfonamides as Dual Binders of the Proteins B-Cell Lymphoma 2 and B-Cell Lymphoma Extra Long with Potent Proapoptotic Cell-Based Activity von Sleebs, Brad E, Czabotar, Peter E, Fairbrother, Wayne J, Fairlie, W. Douglas, Flygare, John A, Huang, David C. S, Kersten, Wilhelmus J. A, Koehler, Michael F. T, Lessene, Guillaume, Lowes, Kym, Parisot, John P, Smith, Brian J, Smith, Morey L, Souers, Andrew J, Street, Ian P, Yang, Hong, Baell, Jonathan B

Volltext

Potent, Selective, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin Kinase Domain Exhibiting Single Agent Antiproliferative Activity von Koehler, Michael F. T, Bergeron, Philippe, Blackwood, Elizabeth, Bowman, Krista K, Chen, Yung-Hsiang, Deshmukh, Gauri, Ding, Xiao, Epler, Jennifer, Lau, Kevin, Lee, Leslie, Liu, Lichuan, Ly, Cuong, Malek, Shiva, Nonomiya, Jim, Oeh, Jason, Ortwine, Daniel F, Sampath, Deepak, Sideris, Steve, Trinh, Lan, Truong, Tom, Wu, Jiansheng, Pei, Zhonghua, Lyssikatos, Joseph P

Volltext

Pyrimidoaminotropanes as Potent, Selective, and Efficacious Small Molecule Kinase Inhibitors of the Mammalian Target of Rapamycin (mTOR) von Estrada, Anthony A, Shore, Daniel G, Blackwood, Elizabeth, Chen, Yung-Hsiang, Deshmukh, Gauri, Ding, Xiao, DiPasquale, Antonio G, Epler, Jennifer A, Friedman, Lori S, Koehler, Michael F. T, Liu, Lichuan, Malek, Shiva, Nonomiya, Jim, Ortwine, Daniel F, Pei, Zhonghua, Sideris, Steve, St-Jean, Frederic, Trinh, Lan, Truong, Tom, Lyssikatos, Joseph P

Volltext

A Putative Bacterial ABC Transporter Circumvents the Essentiality of Signal Peptidase von Morisaki, J Hiroshi, Smith, Peter A, Date, Shailesh V, Kajihara, Kimberly K, Truong, Chau Linda, Modrusan, Zora, Yan, Donghong, Kang, Jing, Xu, Min, Shah, Ishita M, Mintzer, Robert, Kofoed, Eric M, Cheung, Tommy K, Arnott, David, Koehler, Michael F T, Heise, Christopher E, Brown, Eric J, Tan, Man-Wah, Hazenbos, Wouter L W

Volltext

Potent, Selective, and Orally Bioavailable Inhibitors of Mammalian Target of Rapamycin (mTOR) Kinase Based on a Quaternary Substituted Dihydrofuropyrimidine von 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

Volltext

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349 von Pei, Zhonghua, Blackwood, Elizabeth, Liu, Lichuan, Malek, Shiva, Belvin, Marcia, Koehler, Michael F. T, Ortwine, Daniel F, Chen, Huifen, Cohen, Frederick, Kenny, Jane R, Bergeron, Philippe, Lau, Kevin, Ly, Cuong, Zhao, Xianrui, Estrada, Anthony A, Truong, Tom, Epler, Jennifer A, Nonomiya, Jim, Trinh, Lan, Sideris, Steve, Lesnick, John, Bao, Linda, Vijapurkar, Ulka, Mukadam, Sophie, Tay, Suzanne, Deshmukh, Gauri, Chen, Yung-Hsiang, Ding, Xiao, Friedman, Lori S, Lyssikatos, Joseph P

Volltext

Structure-Guided Rescaffolding of Selective Antagonists of BCL‑XL von Koehler, Michael F. T, Bergeron, Philippe, Choo, Edna F, Lau, Kevin, Ndubaku, Chudi, Dudley, Danette, Gibbons, Paul, Sleebs, Brad E, Rye, Carl S, Nikolakopoulos, George, Bui, Chinh, Kulasegaram, Sanji, Kersten, Wilhelmus J. A, Smith, Brian J, Czabotar, Peter E, Colman, Peter M, Huang, David C. S, Baell, Jonathan B, Watson, Keith G, Hasvold, Lisa, Tao, Zhi-Fu, Wang, Le, Souers, Andrew J, Elmore, Steven W, Flygare, John A, Fairbrother, Wayne J, Lessene, Guillaume

Volltext

Membrane Permeability in a Large Macrocyclic Peptide Driven by a Saddle-Shaped Conformation von Faris, Justin H., Adaligil, Emel, Popovych, Nataliya, Ono, Satoshi, Takahashi, Mifune, Nguyen, Huy, Plise, Emile, Taechalertpaisarn, Jaru, Lee, Hsiau-Wei, Koehler, Michael F. T., Cunningham, Christian N., Lokey, R. Scott

Volltext

Structural basis for dual-mode inhibition of the ABC transporter MsbA von 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.

Volltext

Discovery of a Potent and Selective BCL‑XL Inhibitor with in Vivo Activity von 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

Volltext