Search Results - "Saiki, Anne Y."

The Role of MDM2 Amplification and Overexpression in Tumorigenesis by Oliner, Jonathan D, Saiki, Anne Y, Caenepeel, Sean

“…Mouse double minute 2 (MDM2) is a critical negative regulator of the tumor suppressor p53, playing a key role in controlling its transcriptional activity,…”
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The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents by Canon, Jude, Osgood, Tao, Olson, Steven H, Saiki, Anne Y, Robertson, Rebecca, Yu, Dongyin, Eksterowicz, John, Ye, Qiuping, Jin, Lixia, Chen, Ada, Zhou, Jing, Cordover, David, Kaufman, Stephen, Kendall, Richard, Oliner, Jonathan D, Coxon, Angela, Radinsky, Robert

“…p53 is a critical tumor suppressor and is the most frequently inactivated gene in human cancer. Inhibition of the interaction of p53 with its negative…”
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Structure-Based Design of Novel Inhibitors of the MDM2–p53 Interaction by Rew, Yosup, Sun, Daqing, Gonzalez-Lopez De Turiso, Felix, Bartberger, Michael D, Beck, Hilary P, Canon, Jude, Chen, Ada, Chow, David, Deignan, Jeffrey, Fox, Brian M, Gustin, Darin, Huang, Xin, Jiang, Min, Jiao, Xianyun, Jin, Lixia, Kayser, Frank, Kopecky, David J, Li, Yihong, Lo, Mei-Chu, Long, Alexander M, Michelsen, Klaus, Oliner, Jonathan D, Osgood, Tao, Ragains, Mark, Saiki, Anne Y, Schneider, Steve, Toteva, Maria, Yakowec, Peter, Yan, Xuelei, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Medina, Julio C, Olson, Steven H

“…Structure-based rational design led to the discovery of novel inhibitors of the MDM2–p53 protein–protein interaction. The affinity of these compounds for MDM2…”
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The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity by Canon, Jude, Rex, Karen, Saiki, Anne Y., Mohr, Christopher, Cooke, Keegan, Bagal, Dhanashri, Gaida, Kevin, Holt, Tyler, Knutson, Charles G., Koppada, Neelima, Lanman, Brian A., Werner, Jonathan, Rapaport, Aaron S., San Miguel, Tisha, Ortiz, Roberto, Osgood, Tao, Sun, Ji-Rong, Zhu, Xiaochun, McCarter, John D., Volak, Laurie P., Houk, Brett E., Fakih, Marwan G., O’Neil, Bert H., Price, Timothy J., Falchook, Gerald S., Desai, Jayesh, Kuo, James, Govindan, Ramaswamy, Hong, David S., Ouyang, Wenjun, Henary, Haby, Arvedson, Tara, Cee, Victor J., Lipford, J. Russell

“…KRAS is the most frequently mutated oncogene in cancer and encodes a key signalling protein in tumours 1 , 2 . The KRAS(G12C) mutant has a cysteine residue…”
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Diverse alterations associated with resistance to KRAS(G12C) inhibition by Zhao, Yulei, Murciano-Goroff, Yonina R., Xue, Jenny Y., Ang, Agnes, Lucas, Jessica, Mai, Trang T., Da Cruz Paula, Arnaud F., Saiki, Anne Y., Mohn, Deanna, Achanta, Pragathi, Sisk, Ann E., Arora, Kanika S., Roy, Rohan S., Kim, Dongsung, Li, Chuanchuan, Lim, Lee P., Li, Mark, Bahr, Amber, Loomis, Brian R., de Stanchina, Elisa, Reis-Filho, Jorge S., Weigelt, Britta, Berger, Michael, Riely, Gregory, Arbour, Kathryn C., Lipford, J. Russell, Li, Bob T., Lito, Piro

“…Inactive state-selective KRAS(G12C) inhibitors 1 – 8 demonstrate a 30–40% response rate and result in approximately 6-month median progression-free survival in…”
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Identifying the determinants of response to MDM2 inhibition by Saiki, Anne Y, Caenepeel, Sean, Cosgrove, Elissa, Su, Cheng, Boedigheimer, Michael, Oliner, Jonathan D

“…Previous reports have provided evidence that p53 mutation is a strong negative predictor of response to MDM2 inhibitors. However, this correlation is not…”
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Selective and Potent Morpholinone Inhibitors of the MDM2–p53 Protein–Protein Interaction by Gonzalez, Ana Z, Eksterowicz, John, Bartberger, Michael D, Beck, Hilary P, Canon, Jude, Chen, Ada, Chow, David, Duquette, Jason, Fox, Brian M, Fu, Jiasheng, Huang, Xin, Houze, Jonathan B, Jin, Lixia, Li, Yihong, Li, Zhihong, Ling, Yun, Lo, Mei-Chu, Long, Alexander M, McGee, Lawrence R, McIntosh, Joel, McMinn, Dustin L, Oliner, Jonathan D, Osgood, Tao, Rew, Yosup, Saiki, Anne Y, Shaffer, Paul, Wortman, Sarah, Yakowec, Peter, Yan, Xuelei, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Olson, Steven H, Medina, Julio C, Sun, Daqing

“…We previously reported the discovery of AMG 232, a highly potent and selective piperidinone inhibitor of the MDM2–p53 interaction. Our continued search for…”
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Abstract 3761: The MDM2 inhibitor AMG 232 causes tumor regression and potentiates the anti-tumor activity of MEK inhibition and DNA-damaging cytotoxic agents in preclinical models of acute myeloid leukemia by Canon, Jude R., Osgood, Tao, Saiki, Anne Y., Oliner, Jonathan D.

“…Abstract AMG 232 is a potent inhibitor of the MDM2-p53 interaction and is a promising clinical candidate for treating tumors, in particular those harboring…”
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Rational Design and Binding Mode Duality of MDM2–p53 Inhibitors by Gonzalez-Lopez de Turiso, Felix, Sun, Daqing, Rew, Yosup, Bartberger, Michael D, Beck, Hilary P, Canon, Jude, Chen, Ada, Chow, David, Correll, Tiffany L, Huang, Xin, Julian, Lisa D, Kayser, Frank, Lo, Mei-Chu, Long, Alexander M, McMinn, Dustin, Oliner, Jonathan D, Osgood, Tao, Powers, Jay P, Saiki, Anne Y, Schneider, Steve, Shaffer, Paul, Xiao, Shou-Hua, Yakowec, Peter, Yan, Xuelei, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Medina, Julio C, Olson, Steven H

“…Structural analysis of both the MDM2–p53 protein–protein interaction and several small molecules bound to MDM2 led to the design and synthesis of…”
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Discovery of AM-7209, a Potent and Selective 4‑Amidobenzoic Acid Inhibitor of the MDM2–p53 Interaction by Rew, Yosup, Sun, Daqing, Yan, Xuelei, Beck, Hilary P, Canon, Jude, Chen, Ada, Duquette, Jason, Eksterowicz, John, Fox, Brian M, Fu, Jiasheng, Gonzalez, Ana Z, Houze, Jonathan, Huang, Xin, Jiang, Min, Jin, Lixia, Li, Yihong, Li, Zhihong, Ling, Yun, Lo, Mei-Chu, Long, Alexander M, McGee, Lawrence R, McIntosh, Joel, Oliner, Jonathan D, Osgood, Tao, Saiki, Anne Y, Shaffer, Paul, Wang, Yu Chung, Wortman, Sarah, Yakowec, Peter, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Medina, Julio C, Olson, Steven H

“…Structure-based rational design and extensive structure–activity relationship studies led to the discovery of AMG 232 (1), a potent piperidinone inhibitor of…”
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Novel Inhibitors of the MDM2-p53 Interaction Featuring Hydrogen Bond Acceptors as Carboxylic Acid Isosteres by Gonzalez, Ana Z, Li, Zhihong, Beck, Hilary P, Canon, Jude, Chen, Ada, Chow, David, Duquette, Jason, Eksterowicz, John, Fox, Brian M, Fu, Jiasheng, Huang, Xin, Houze, Jonathan, Jin, Lixia, Li, Yihong, Ling, Yun, Lo, Mei-Chu, Long, Alexander M, McGee, Lawrence R, McIntosh, Joel, Oliner, Jonathan D, Osgood, Tao, Rew, Yosup, Saiki, Anne Y, Shaffer, Paul, Wortman, Sarah, Yakowec, Peter, Yan, Xuelei, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Olson, Steven H, Sun, Daqing, Medina, Julio C

“…We previously reported the discovery of potent and selective morpholinone and piperidinone inhibitors of the MDM2-p53 interaction. These inhibitors have in…”
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MDM2 antagonists synergize broadly and robustly with compounds targeting fundamental oncogenic signaling pathways by Saiki, Anne Y, Caenepeel, Sean, Yu, Dongyin, Lofgren, Julie A, Osgood, Tao, Robertson, Rebecca, Canon, Jude, Su, Cheng, Jones, Adrie, Zhao, Xiaoning, Deshpande, Chetan, Payton, Marc, Ledell, Jebediah, Hughes, Paul E, Oliner, Jonathan D

“…While MDM2 inhibitors hold great promise as cancer therapeutics, drug resistance will likely limit their efficacy as single agents. To identify drug…”
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Discovery of a Covalent Inhibitor of KRAS G12C (AMG 510) for the Treatment of Solid Tumors by Lanman, Brian A, Allen, Jennifer R, Allen, John G, Amegadzie, Albert K, Ashton, Kate S, Booker, Shon K, Chen, Jian Jeffrey, Chen, Ning, Frohn, Michael J, Goodman, Guy, Kopecky, David J, Liu, Longbin, Lopez, Patricia, Low, Jonathan D, Ma, Vu, Minatti, Ana E, Nguyen, Thomas T, Nishimura, Nobuko, Pickrell, Alexander J, Reed, Anthony B, Shin, Youngsook, Siegmund, Aaron C, Tamayo, Nuria A, Tegley, Christopher M, Walton, Mary C, Wang, Hui-Ling, Wurz, Ryan P, Xue, May, Yang, Kevin C, Achanta, Pragathi, Bartberger, Michael D, Canon, Jude, Hollis, L Steven, McCarter, John D, Mohr, Christopher, Rex, Karen, Saiki, Anne Y, San Miguel, Tisha, Volak, Laurie P, Wang, Kevin H, Whittington, Douglas A, Zech, Stephan G, Lipford, J Russell, Cee, Victor J

“…KRAS has emerged as a promising target in the treatment of solid tumors. Covalent inhibitors targeting the mutant cysteine-12 residue have been shown to…”
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Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors by Lanman, Brian A, Allen, Jennifer R, Allen, John G, Amegadzie, Albert K, Ashton, Kate S, Booker, Shon K, Chen, Jian Jeffrey, Chen, Ning, Frohn, Michael J, Goodman, Guy, Kopecky, David J, Liu, Longbin, Lopez, Patricia, Low, Jonathan D, Ma, Vu, Minatti, Ana E, Nguyen, Thomas T, Nishimura, Nobuko, Pickrell, Alexander J, Reed, Anthony B, Shin, Youngsook, Siegmund, Aaron C, Tamayo, Nuria A, Tegley, Christopher M, Walton, Mary C, Wang, Hui-Ling, Wurz, Ryan P, Xue, May, Yang, Kevin C, Achanta, Pragathi, Bartberger, Michael D, Canon, Jude, Hollis, L. Steven, McCarter, John D, Mohr, Christopher, Rex, Karen, Saiki, Anne Y, San Miguel, Tisha, Volak, Laurie P, Wang, Kevin H, Whittington, Douglas A, Zech, Stephan G, Lipford, J. Russell, Cee, Victor J

“…KRASG12C has emerged as a promising target in the treatment of solid tumors. Covalent inhibitors targeting the mutant cysteine-12 residue have been shown to…”
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Improvement of the synthesis and pharmacokinetic properties of chromenotriazolopyrimidine MDM2-p53 protein-protein inhibitors by Beck, Hilary P., DeGraffenreid, Michael, Fox, Brian, Allen, John G., Rew, Yosup, Schneider, Stephen, Saiki, Anne Y., Yu, Dongyin, Oliner, Jonathan D., Salyers, Kevin, Ye, Qiuping, Olson, Steven

“…Human murine double minute 2 (MDM2) is a negative regulator of p53, which plays an important role in cell cycle and apoptosis. We report several optimizations…”
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Discovery of N‑(1-Acryloylazetidin-3-yl)-2-(1H‑indol-1-yl)acetamides as Covalent Inhibitors of KRASG12C by Shin, Youngsook, Jeong, Joon Won, Wurz, Ryan P, Achanta, Pragathi, Arvedson, Tara, Bartberger, Michael D, Campuzano, Iain D. G, Fucini, Ray, Hansen, Stig K, Ingersoll, John, Iwig, Jeffrey S, Lipford, J. Russell, Ma, Vu, Kopecky, David J, McCarter, John, San Miguel, Tisha, Mohr, Christopher, Sabet, Sudi, Saiki, Anne Y, Sawayama, Andrew, Sethofer, Steven, Tegley, Christopher M, Volak, Laurie P, Yang, Kevin, Lanman, Brian A, Erlanson, Daniel A, Cee, Victor J

“…KRAS regulates many cellular processes including proliferation, survival, and differentiation. Point mutants of KRAS have long been known to be molecular…”
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Discovery of N -(1-Acryloylazetidin-3-yl)-2-(1 H -indol-1-yl)acetamides as Covalent Inhibitors of KRAS G12C by Shin, Youngsook, Jeong, Joon Won, Wurz, Ryan P, Achanta, Pragathi, Arvedson, Tara, Bartberger, Michael D, Campuzano, Iain D G, Fucini, Ray, Hansen, Stig K, Ingersoll, John, Iwig, Jeffrey S, Lipford, J Russell, Ma, Vu, Kopecky, David J, McCarter, John, San Miguel, Tisha, Mohr, Christopher, Sabet, Sudi, Saiki, Anne Y, Sawayama, Andrew, Sethofer, Steven, Tegley, Christopher M, Volak, Laurie P, Yang, Kevin, Lanman, Brian A, Erlanson, Daniel A, Cee, Victor J

“…KRAS regulates many cellular processes including proliferation, survival, and differentiation. Point mutants of KRAS have long been known to be molecular…”
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Discovery of Potent and Simplified Piperidinone-Based Inhibitors of the MDM2–p53 Interaction by Yu, Ming, Wang, Yingcai, Zhu, Jiang, Bartberger, Michael D, Canon, Jude, Chen, Ada, Chow, David, Eksterowicz, John, Fox, Brian, Fu, Jiasheng, Gribble, Michael, Huang, Xin, Li, Zhihong, Liu, Jiwen (Jim), Lo, Mei-chu, McMinn, Dustin, Oliner, Jonathan D, Osgood, Tao, Rew, Yosup, Saiki, Anne Y, Shaffer, Paul, Yan, Xuelei, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Olson, Steven H, Medina, Julio C, Sun, Daqing

“…Continued optimization of the N-substituent in the piperidinone series provided potent piperidinone–pyridine inhibitors 6, 7, 14, and 15 with improved…”
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DNA Cleavage Activities of Staphylococcus aureus Gyrase and Topoisomerase IV Stimulated by Quinolones and 2-Pyridones by SAIKI, A. Y. C, SHEN, L. L, CHEN, C.-M, BARANOWSKI, J, LERNER, C. G

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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From Bacterial Genomes to Novel Antibacterial Agents: Discovery, Characterization, and Antibacterial Activity of Compounds that Bind to HI0065 (YjeE) from Haemophilus influenzae by Lerner, Claude G., Hajduk, Philip J., Wagner, Rolf, Wagenaar, Frank L., Woodall, Charlotte, Gu, Yu‐Gui, Searle, Xenia B., Florjancic, Alan S., Zhang, Tianyuan, Clark, Richard F., Cooper, Curt S., Mack, Jamey C., Yu, Liping, Cai, Mengli, Betz, Steven F., Chovan, Linda E., McCall, J. Owen, Black‐Schaefer, Candace L., Kakavas, Stephan J., Schurdak, Mark E., Comess, Kenneth M., Walter, Karl A., Edalji, Rohinton, Dorwin, Sarah A., Smith, Richard A., Hebert, Eric J., Harlan, John E., Metzger, Randy E., Merta, Philip J., Baranowski, John L., Coen, Michael L., Thornewell, Susan J., Shivakumar, Annapur G., Saiki, Anne Y., Soni, Niru, Bui, Mai, Balli, Darlene J., Sanders, William J., Nilius, Angela M., Holzman, Thomas F., Fesik, Stephen W., Beutel, Bruce A.

“…As part of a fully integrated and comprehensive strategy to discover novel antibacterial agents, NMR‐ and mass spectrometry‐based affinity selection screens…”
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