Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer von Heffron, Timothy P

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Challenges of developing small-molecule kinase inhibitors for brain tumors and the need for emphasis on free drug levels von Heffron, Timothy P

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Prevalence of Acid-Reducing Agents (ARA) in Cancer Populations and ARA Drug–Drug Interaction Potential for Molecular Targeted Agents in Clinical Development von Smelick, Gillian S, Heffron, Timothy P, Chu, Laura, Dean, Brian, West, David A, DuVall, Scott L, Lum, Bert L, Budha, Nageshwar, Holden, Scott N, Benet, Leslie Z, Frymoyer, Adam, Dresser, Mark J, Ware, Joseph A

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RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy von Song, Kyung W, Edgar, Kyle A, Hanan, Emily J, Hafner, Marc, Oeh, Jason, Merchant, Mark, Sampath, Deepak, Nannini, Michelle A, Hong, Rebecca, Phu, Lilian, Forrest, William F, Stawiski, Eric, Schmidt, Stephen, Endres, Nicholas, Guan, Jane, Wallin, Jeffrey J, Cheong, Jonathan, Plise, Emile G, Lewis Phillips, Gail D, Salphati, Laurent, Heffron, Timothy P, Olivero, Alan G, Malek, Shiva, Staben, Steven T, Kirkpatrick, Donald S, Dey, Anwesha, Friedman, Lori S

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Assessment of KRAS G12C Target Engagement by a Covalent Inhibitor in Tumor Biopsies Using an Ultra-Sensitive Immunoaffinity 2D-LC–MS/MS Approach von 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

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Discovery of 2‑{3-[2-(1-Isopropyl-3-methyl‑1H‑1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl]‑1H‑pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β‑Sparing... von Ndubaku, Chudi O, Heffron, Timothy P, Staben, Steven T, Baumgardner, Matthew, Blaquiere, Nicole, Bradley, Erin, Bull, Richard, Do, Steven, Dotson, Jennafer, Dudley, Danette, Edgar, Kyle A, Friedman, Lori S, Goldsmith, Richard, Heald, Robert A, Kolesnikov, Aleksandr, Lee, Leslie, Lewis, Cristina, Nannini, Michelle, Nonomiya, Jim, Pang, Jodie, Price, Steve, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Wallin, Jeffery J, Wang, Lan, Wei, BinQing, Sampath, Deepak, Olivero, Alan G

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Hematopoietic Progenitor Kinase-1 Structure in a Domain-Swapped Dimer von Wu, Ping, Sneeringer, Christopher J., Pitts, Keith E., Day, Eric S., Chan, Bryan K., Wei, Binqing, Lehoux, Isabelle, Mortara, Kyle, Li, Hong, Wu, Jiansheng, Franke, Yvonne, Moffat, John G., Grogan, Jane L., Heffron, Timothy P., Wang, Weiru

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The Rational Design of Selective Benzoxazepin Inhibitors of the α‑Isoform of Phosphoinositide 3‑Kinase Culminating in the Identification of (S)‑2-((2-(1-Isopropyl‑1H‑1,2,4-triazol-... von Heffron, Timothy P, Heald, Robert A, Ndubaku, Chudi, Wei, BinQing, Augistin, Martin, Do, Steven, Edgar, Kyle, Eigenbrot, Charles, Friedman, Lori, Gancia, Emanuela, Jackson, Philip S, Jones, Graham, Kolesnikov, Aleksander, Lee, Leslie B, Lesnick, John D, Lewis, Cristina, McLean, Neville, Mörtl, Mario, Nonomiya, Jim, Pang, Jodie, Price, Steve, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Staben, Steven T, Steinbacher, Stefan, Tsui, Vickie, Wallin, Jeffrey, Sampath, Deepak, Olivero, Alan G

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Noncovalent wild-type-sparing inhibitors of EGFR T790M von Lee, Ho-June, Schaefer, Gabriele, Heffron, Timothy P, Shao, Lily, Ye, Xiaofen, Sideris, Steve, Malek, Shiva, Chan, Emily, Merchant, Mark, La, Hank, Ubhayakar, Savita, Yauch, Robert L, Pirazzoli, Valentina, Politi, Katerina, Settleman, Jeff

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Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma von Bronner, Sarah M., Merrick, Karl A., Murray, Jeremy, Salphati, Laurent, Moffat, John G., Pang, Jodie, Sneeringer, Christopher J., Dompe, Nicholas, Cyr, Patrick, Purkey, Hans, Boenig, Gladys de Leon, Li, Jun, Kolesnikov, Aleksandr, Larouche-Gauthier, Robin, Lai, Kwong Wah, Shen, Xiaoli, Aubert-Nicol, Samuel, Chen, Yi-Chen, Cheong, Jonathan, Crawford, James J., Hafner, Marc, Haghshenas, Pouyan, Jakalian, Araz, Leclerc, Jean-Philippe, Lim, Ngiap-Kie, O'Brien, Tom, Plise, Emile G., Shalan, Hadil, Sturino, Claudio, Wai, John, Xiao, Yang, Yin, Jianping, Zhao, Liang, Gould, Stephen, Olivero, Alan, Heffron, Timothy P.

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Discovery of Highly Potent, Selective, and Brain-Penetrant Aminopyrazole Leucine-Rich Repeat Kinase 2 (LRRK2) Small Molecule Inhibitors von Estrada, Anthony A, Chan, Bryan K, Baker-Glenn, Charles, Beresford, Alan, Burdick, Daniel J, Chambers, Mark, Chen, Huifen, Dominguez, Sara L, Dotson, Jennafer, Drummond, Jason, Flagella, Michael, Fuji, Reina, Gill, Andrew, Halladay, Jason, Harris, Seth F, Heffron, Timothy P, Kleinheinz, Tracy, Lee, Donna W, Pichon, Claire E. Le, Liu, Xingrong, Lyssikatos, Joseph P, Medhurst, Andrew D, Moffat, John G, Nash, Kevin, Scearce-Levie, Kimberly, Sheng, Zejuan, Shore, Daniel G, Wong, Susan, Zhang, Shuo, Zhang, Xiaolin, Zhu, Haitao, Sweeney, Zachary K

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Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR von Heffron, Timothy P, Ndubaku, Chudi O, Salphati, Laurent, Alicke, Bruno, Cheong, Jonathan, Drobnick, Joy, Edgar, Kyle, Gould, Stephen E, Lee, Leslie B, Lesnick, John D, Lewis, Cristina, Nonomiya, Jim, Pang, Jodie, Plise, Emile G, Sideris, Steve, Wallin, Jeffrey, Wang, Lan, Zhang, Xiaolin, Olivero, Alan G

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Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma von Salphati, Laurent, Alicke, Bruno, Heffron, Timothy P, Shahidi-Latham, Sheerin, Nishimura, Merry, Cao, Tim, Carano, Richard A, Cheong, Jonathan, Greve, Joan, Koeppen, Hartmut, Lau, Shari, Lee, Leslie B, Nannini-Pepe, Michelle, Pang, Jodie, Plise, Emile G, Quiason, Cristine, Rangell, Linda, Zhang, Xiaolin, Gould, Stephen E, Phillips, Heidi S, Olivero, Alan G

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Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study von Heald, Robert, Bowman, Krista K, Bryan, Marian C, Burdick, Daniel, Chan, Bryan, Chan, Emily, Chen, Yuan, Clausen, Saundra, Dominguez-Fernandez, Belen, Eigenbrot, Charles, Elliott, Richard, Hanan, Emily J, Jackson, Philip, Knight, Jamie, La, Hank, Lainchbury, Michael, Malek, Shiva, Mann, Sam, Merchant, Mark, Mortara, Kyle, Purkey, Hans, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen, Sideris, Steve, Shao, Lily, Wang, Shumei, Yeap, Kuen, Yen, Ivana, Yu, Christine, Heffron, Timothy P

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4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase von 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.

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Characterization of Antineovascularization Activity and Ocular Pharmacokinetics of Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GNE-947 von Liu, Xingrong, Liang, Xiaorong, LeCouter, Jenninfer, Ubhayakar, Savita, Chen, Jacob, Cheng, Jay, Lee, Tom, Lubach, Joe, Nonomiya, Jim, Shahidi-Latham, Sheerin, Quiason, Cristine, Solon, Eric, Wright, Matthew, Hop, Cornelis E.C.A., Heffron, Timothy P.

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Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation von 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

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Discovery of Highly Potent, Selective, and Brain-Penetrable Leucine-Rich Repeat Kinase 2 (LRRK2) Small Molecule Inhibitors von Estrada, Anthony A, Liu, Xingrong, Baker-Glenn, Charles, Beresford, Alan, Burdick, Daniel J, Chambers, Mark, Chan, Bryan K, Chen, Huifen, Ding, Xiao, DiPasquale, Antonio G, Dominguez, Sara L, Dotson, Jennafer, Drummond, Jason, Flagella, Michael, Flynn, Sean, Fuji, Reina, Gill, Andrew, Gunzner-Toste, Janet, Harris, Seth F, Heffron, Timothy P, Kleinheinz, Tracy, Lee, Donna W, Le Pichon, Claire E, Lyssikatos, Joseph P, Medhurst, Andrew D, Moffat, John G, Mukund, Susmith, Nash, Kevin, Scearce-Levie, Kimberly, Sheng, Zejuan, Shore, Daniel G, Tran, Thuy, Trivedi, Naimisha, Wang, Shumei, Zhang, Shuo, Zhang, Xiaolin, Zhao, Guiling, Zhu, Haitao, Sweeney, Zachary K

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Discovery of GNE-6893, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of HPK1 von Tellis, John C, Wei, BinQing, Siu, Michael, An, Le, Chan, Grace Kayan, Chen, Yong, Du, Xiangnan, Gazzard, Lewis, Hu, Baihua, Kiefer, James, Kakiuchi-Kiyota, Satoko, Lainchbury, Michael, Linehan, Jonathan L, Luo, Xifeng, Malhotra, Sushant, Mendonca, Rohan, Pang, Jodie, Ran, Yinqing, Sethuraman, Vijay, Seward, Eileen, Sneeringer, Chris, Su, Dian, Wang, Weiru, Wu, Ping, Moffat, John G, Heffron, Timothy P, Choo, Edna F, Chan, Bryan K

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Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1) von Chan, Bryan K, Seward, Eileen, Lainchbury, Michael, Brewer, Thomas F, An, Le, Blench, Toby, Cartwright, Matthew W, Chan, Grace Ka Yan, Choo, Edna F, Drummond, Jason, Elliott, Richard L, Gancia, Emanuela, Gazzard, Lewis, Hu, Baihua, Jones, Graham E, Luo, Xifeng, Madin, Andrew, Malhotra, Sushant, Moffat, John G, Pang, Jodie, Salphati, Laurent, Sneeringer, Christopher J, Stivala, Craig E, Wei, Binqing, Wang, Weiru, Wu, Ping, Heffron, Timothy P

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