Search Results - "Johnson, Ted"

Lipophilic Efficiency as an Important Metric in Drug Design by Johnson, Ted W, Gallego, Rebecca A, Edwards, Martin P

“…Lipophilic efficiency (LipE) is an important metric that has been increasingly applied in drug discovery medicinal chemistry lead optimization programs. In…”
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Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound ALK Mutations in ALK-Positive Lung Cancer by Yoda, Satoshi, Lin, Jessica J, Lawrence, Michael S, Burke, Benjamin J, Friboulet, Luc, Langenbucher, Adam, Dardaei, Leila, Prutisto-Chang, Kylie, Dagogo-Jack, Ibiayi, Timofeevski, Sergei, Hubbeling, Harper, Gainor, Justin F, Ferris, Lorin A, Riley, Amanda K, Kattermann, Krystina E, Timonina, Daria, Heist, Rebecca S, Iafrate, A John, Benes, Cyril H, Lennerz, Jochen K, Mino-Kenudson, Mari, Engelman, Jeffrey A, Johnson, Ted W, Hata, Aaron N, Shaw, Alice T

“…The cornerstone of treatment for advanced ALK-positive lung cancer is sequential therapy with increasingly potent and selective ALK inhibitors. The…”
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PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models by Zou, Helen Y., Friboulet, Luc, Kodack, David P., Engstrom, Lars D., Li, Qiuhua, West, Melissa, Tang, Ruth W., Wang, Hui, Tsaparikos, Konstantinos, Wang, Jinwei, Timofeevski, Sergei, Katayama, Ryohei, Dinh, Dac M., Lam, Hieu, Lam, Justine L., Yamazaki, Shinji, Hu, Wenyue, Patel, Bhushankumar, Bezwada, Divya, Frias, Rosa L., Lifshits, Eugene, Mahmood, Sidra, Gainor, Justin F., Affolter, Timothy, Lappin, Patrick B., Gukasyan, Hovhannes, Lee, Nathan, Deng, Shibing, Jain, Rakesh K., Johnson, Ted W., Shaw, Alice T., Fantin, Valeria R., Smeal, Tod

“…We report the preclinical evaluation of PF-06463922, a potent and brain-penetrant ALK/ROS1 inhibitor. Compared with other clinically available ALK inhibitors,…”
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Using the Golden Triangle to optimize clearance and oral absorption by Johnson, Ted W., Dress, Klaus R., Edwards, Martin

“…The Golden Triangle is a visualization tool developed from in vitro permeability, in vitro clearance and computational data designed to aid medicinal chemists…”
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Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F by Shaw, Alice T, Friboulet, Luc, Leshchiner, Ignaty, Gainor, Justin F, Bergqvist, Simon, Brooun, Alexei, Burke, Benjamin J, Deng, Ya-Li, Liu, Wei, Dardaei, Leila, Frias, Rosa L, Schultz, Kate R, Logan, Jennifer, James, Leonard P, Smeal, Tod, Timofeevski, Sergei, Katayama, Ryohei, Iafrate, A. John, Le, Long, McTigue, Michele, Getz, Gad, Johnson, Ted W, Engelman, Jeffrey A

“…A resistance mutation (C1156Y) developed in a woman with anaplastic lymphoma kinase ( ALK )-rearranged lung cancer who had a response to crizotinib. She then…”
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PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations by Zou, Helen Y., Li, Qiuhua, Engstrom, Lars D., West, Melissa, Appleman, Vicky, Wong, Katy A., McTigue, Michele, Deng, Ya-Li, Liu, Wei, Brooun, Alexei, Timofeevski, Sergei, McDonnell, Scott R. P., Jiang, Ping, Falk, Matthew D., Lappin, Patrick B., Affolter, Timothy, Nichols, Tim, Hu, Wenyue, Lam, Justine, Johnson, Ted W., Smeal, Tod, Charest, Al, Fantin, Valeria R.

“…Significance Overcoming resistance to targeted kinase inhibitors is a major clinical challenge in oncology. Development of crizotinib resistance through the…”
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Spectrum of Mechanisms of Resistance to Crizotinib and Lorlatinib in ROS1 Fusion-Positive Lung Cancer by Lin, Jessica J, Choudhury, Noura J, Yoda, Satoshi, Zhu, Viola W, Johnson, Ted W, Sakhtemani, Ramin, Dagogo-Jack, Ibiayi, Digumarthy, Subba R, Lee, Charlotte, Do, Andrew, Peterson, Jennifer, Prutisto-Chang, Kylie, Malik, Wafa, Hubbeling, Harper G, Langenbucher, Adam, Schoenfeld, Adam J, Falcon, Christina J, Temel, Jennifer S, Sequist, Lecia V, Yeap, Beow Y, Lennerz, Jochen K, Shaw, Alice T, Lawrence, Michael S, Ou, Sai-Hong Ignatius, Hata, Aaron N, Drilon, Alexander, Gainor, Justin F

“…Current standard initial therapy for advanced, ROS proto-oncogene 1, receptor tyrosine kinase fusion ( )-positive (ROS1 ) non-small cell lung cancer (NSCLC) is…”
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Unusual Abundances from Planetary System Material Polluting the White Dwarf G238-44 by Johnson, Ted M, Klein, Beth L., Koester, D., Melis, Carl, Zuckerman, B., Jura, M.

“…Ultraviolet and optical spectra of the hydrogen-dominated atmosphere white dwarf star G238-44 obtained with FUSE, Keck/HIRES, HST/COS, and HST/STIS reveal 10…”
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Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations by Johnson, Ted W, Richardson, Paul F, Bailey, Simon, Brooun, Alexei, Burke, Benjamin J, Collins, Michael R, Cui, J Jean, Deal, Judith G, Deng, Ya-Li, Dinh, Dac, Engstrom, Lars D, He, Mingying, Hoffman, Jacqui, Hoffman, Robert L, Huang, Qinhua, Kania, Robert S, Kath, John C, Lam, Hieu, Lam, Justine L, Le, Phuong T, Lingardo, Laura, Liu, Wei, McTigue, Michele, Palmer, Cynthia L, Sach, Neal W, Smeal, Tod, Smith, Graham L, Stewart, Albert E, Timofeevski, Sergei, Zhu, Huichun, Zhu, Jinjiang, Zou, Helen Y, Edwards, Martin P

“…Although crizotinib demonstrates robust efficacy in anaplastic lymphoma kinase (ALK)-positive non-small-cell lung carcinoma patients, progression during…”
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LTK fusions: A new target emerges in non-small cell lung cancer by Cooper, Alissa J., Sequist, Lecia V., Johnson, Ted W., Lin, Jessica J.

“…Identification of targetable fusions as oncogenic drivers in non-small cell lung cancer has transformed its diagnostic and therapeutic paradigm. In a recent…”
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Conformational Studies and Atropisomerism Kinetics of the ALK Clinical Candidate Lorlatinib (PF-06463922) and Desmethyl Congeners by Elleraas, Jeff, Ewanicki, Jason, Johnson, Ted W., Sach, Neal W., Collins, Michael R., Richardson, Paul F.

“…Lorlatinib (PF‐06463922) is an ALK/ROS1 inhibitor and is in clinical trials for the treatment of ALK positive or ROS1 positive NSCLC (i.e. specific subsets of…”
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Multiple conformational states of the HPK1 kinase domain in complex with sunitinib reveal the structural changes accompanying HPK1 trans-regulation by Johnson, Eric, McTigue, Michele, Gallego, Rebecca A., Johnson, Ted W., Timofeevski, Sergei, Maestre, Michael, Fisher, Timothy S., Kania, Robert, Sawasdikosol, Sansana, Burakoff, Steven, Cronin, Ciarán N.

“…Hematopoietic progenitor kinase 1 (HPK1 or MAP4K1) is a Ser/Thr kinase that operates via the c-Jun N-terminal kinase (JNK) and extracellular signal-regulated…”
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Lipophilic efficiency: the most important efficiency metric in medicinal chemistry by Freeman-Cook, Kevin D, Hoffman, Robert L, Johnson, Ted W

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The Axl kinase domain in complex with a macrocyclic inhibitor offers first structural insights into an active TAM receptor kinase by Gajiwala, Ketan S., Grodsky, Neil, Bolaños, Ben, Feng, Junli, Ferre, RoseAnn, Timofeevski, Sergei, Xu, Meirong, Murray, Brion W., Johnson, Ted W., Stewart, Al

“…The receptor tyrosine kinase family consisting of Tyro3, Axl, and Mer (TAM) is one of the most recently identified receptor tyrosine kinase families. TAM…”
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Design and Synthesis of Functionally Active 5‑Amino-6-Aryl Pyrrolopyrimidine Inhibitors of Hematopoietic Progenitor Kinase 1 by Gallego, Rebecca A., Bernier, Louise, Chen, Hui, Cho-Schultz, Sujin, Chung, Loanne, Collins, Michael, Del Bel, Matthew, Elleraas, Jeff, Costa Jones, Cinthia, Cronin, Ciaran N., Edwards, Martin, Fang, Xu, Fisher, Timothy, He, Mingying, Hoffman, Jacqui, Huo, Ruiduan, Jalaie, Mehran, Johnson, Eric, Johnson, Ted W., Kania, Robert S., Kraus, Manfred, Lafontaine, Jennifer, Le, Phuong, Liu, Tongnan, Maestre, Michael, Matthews, Jean, McTigue, Michele, Miller, Nichol, Mu, Qiming, Qin, Xulong, Ren, Shijian, Richardson, Paul, Rohner, Allison, Sach, Neal, Shao, Li, Smith, Graham, Su, Ruirui, Sun, Bin, Timofeevski, Sergei, Tran, Phuong, Wang, Shuiwang, Wang, Wei, Zhou, Ru, Zhu, Jinjiang, Nair, Sajiv K.

“…Immune activating agents represent a valuable class of therapeutics for the treatment of cancer. An area of active research is expanding the types of these…”
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Discovery of Highly Selective Inhibitors of Microtubule-Associated Serine/Threonine Kinase-like (MASTL) by Gallego, Rebecca A., Scales, Stephanie, Toledo, Chad, Auth, Marin, Bernier, Louise, Berry, Madeline, Brun, Sonja, Chung, Loanne, Davis, Carl, Diehl, Wade, Dress, Klaus, Eisele, Koleen, Elleraas, Jeff, Ewanicki, Jason, Fobian, Yvette, Greasley, Samantha, Greenwald, Eric C., Johnson, Ted W., Khamphavong, Penney, Lafontaine, Jennifer, Li, Jian, Linton, Angelica, Maestre, Michael, Miller, Nichol, Murtaza, Anwar, Patman, Ryan L., Quinlan, Casey L., Ramms, Dana J., Richardson, Paul, Sach, Neal, Salomon-Ferrer, Romelia, Silva, Francisco, Timofeevski, Sergei, Tran, Phuong, Tran-Dubé, Michelle, Wang, Fen, Wang, Wei, Wythes, Martin, Yang, Shouliang, Zou, Aihua, VanArsdale, Todd, McAlpine, Indrawan

“…By virtue of its role in cellular proliferation, microtubule-associated serine/threonine kinase-like (MASTL) represents a novel target and a first-in-class…”
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Digital civic engagement, open data, and the informal sector: a think piece by Hasselwander, Marc, Kiko, Mwendwa, Johnson, Ted

“…•Digital civic engagement and open data spur innovation in informal sectors.•This often leads to the creation of people-centered solutions.•Policymakers should…”
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Discovery of 1‑{(3R,4R)‑3-[({5-Chloro-2-[(1-methyl‑1H‑pyrazol-4-yl)amino]‑7H‑pyrrolo[2,3‑d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants by Cheng, Hengmiao, Nair, Sajiv K, Murray, Brion W, Almaden, Chau, Bailey, Simon, Baxi, Sangita, Behenna, Doug, Cho-Schultz, Sujin, Dalvie, Deepak, Dinh, Dac M, Edwards, Martin P, Feng, Jun Li, Ferre, Rose Ann, Gajiwala, Ketan S, Hemkens, Michelle D, Jackson-Fisher, Amy, Jalaie, Mehran, Johnson, Ted O, Kania, Robert S, Kephart, Susan, Lafontaine, Jennifer, Lunney, Beth, Liu, Kevin K.-C, Liu, Zhengyu, Matthews, Jean, Nagata, Asako, Niessen, Sherry, Ornelas, Martha A, Orr, Suvi T. M, Pairish, Mason, Planken, Simon, Ren, Shijian, Richter, Daniel, Ryan, Kevin, Sach, Neal, Shen, Hong, Smeal, Tod, Solowiej, Jim, Sutton, Scott, Tran, Khanh, Tseng, Elaine, Vernier, William, Walls, Marlena, Wang, Shuiwang, Weinrich, Scott L, Xin, Shuibo, Xu, Haiwei, Yin, Min-Jean, Zientek, Michael, Zhou, Ru, Kath, John C

“…First generation EGFR TKIs (gefitinib, erlotinib) provide significant clinical benefit for NSCLC cancer patients with oncogenic EGFR mutations. Ultimately,…”
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Reviving B‑Factors: Retrospective Normalized B‑Factor Analysis of c‑ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib by Johnson, Ted W, Gallego, Rebecca A, Brooun, Alexei, Gehlhaar, Dan, McTigue, Michele

“…Structure-based drug design (SBDD) is commonly leveraged in rational drug design. Usually, ligand and binding site atomic coordinates from crystallographic…”
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The urban motorcycle taxi sector in Sub-Saharan Africa: needs, practices and equity issues by Owino, Fredrick, Peters, Krijn, Jenkins, Jack, Opiyo, Paul, Chetto, Reginald, Ntramah, Simon, Marion Mutabazi, Mugisha, Vincent, James, Johnson, Ted P., Santos, Rosemarie T., Hayombe, Patrick

“…Motorcycle taxis in Sub-Saharan Africa are an essential component of the urban transport mix, providing vital services - such as access to markets, education…”
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