Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase
Ernst, Justin T., Thompson, Peggy A., Nilewski, Christian, Sprengeler, Paul A., Sperry, Samuel, Packard, Garrick, Michels, Theodore, Xiang, Alan, Tran, Chinh, Wegerski, Christopher J., Eam, Boreth, Young, Nathan P., Fish, Sarah, Chen, Joan, Howard, Haleigh, Staunton, Jocelyn, Molter, Jolene, Clarine, Jeff, Nevarez, Andres, Chiang, Gary G., Appleman, Jim R., Webster, Kevin R., Reich, Siegfried H.
Published in Journal of medicinal chemistry (11.06.2020)
Published in Journal of medicinal chemistry (11.06.2020)
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Journal Article
Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A
Thompson, Peggy A, Eam, Boreth, Young, Nathan P, Fish, Sarah, Chen, Joan, Barrera, Maria, Howard, Haleigh, Sung, Eric, Parra, Ana, Staunton, Jocelyn, Chiang, Gary G, Gerson-Gurwitz, Adina, Wegerski, Christopher J, Nevarez, Andres, Clarine, Jeff, Sperry, Samuel, Xiang, Alan, Nilewski, Christian, Packard, Garrick K, Michels, Theodore, Tran, Chinh, Sprengeler, Paul A, Ernst, Justin T, Reich, Siegfried H, Webster, Kevin R
Published in Molecular cancer therapeutics (01.01.2021)
Published in Molecular cancer therapeutics (01.01.2021)
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Journal Article
Strategic Diastereoselective C1 Functionalization in the Aza-Rocaglamide Scaffold toward Natural Product-Inspired eIF4A Inhibitors
Nilewski, Christian, Michels, Theodore D, Xiang, Alan X, Packard, Garrick K, Sprengeler, Paul A, Eam, Boreth, Fish, Sarah, Thompson, Peggy A, Wegerski, Christopher J, Ernst, Justin T, Reich, Siegfried H
Published in Organic letters (21.08.2020)
Published in Organic letters (21.08.2020)
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Journal Article
1-Aminomethyl SAR in a novel series of flavagline-inspired eIF4A inhibitors: Effects of amine substitution on cell potency and in vitro PK properties
Nilewski, Christian, Michels, Theodore D., Packard, Garrick K., Xiang, Alan X., Sprengeler, Paul A., Eam, Boreth, Fish, Sarah, Thompson, Peggy A., Wegerski, Christopher J., Nevarez, Andres, Clarine, Jeff, Sperry, Samuel, Ernst, Justin T., Reich, Siegfried H.
Published in Bioorganic & medicinal chemistry letters (01.09.2021)
Published in Bioorganic & medicinal chemistry letters (01.09.2021)
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Journal Article
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115
Mortensen, Deborah S., Perrin-Ninkovic, Sophie M., Shevlin, Graziella, Elsner, Jan, Zhao, Jingjing, Whitefield, Brandon, Tehrani, Lida, Sapienza, John, Riggs, Jennifer R., Parnes, Jason S., Papa, Patrick, Packard, Garrick, Lee, Branden G.S., Harris, Roy, Correa, Matthew, Bahmanyar, Sogole, Richardson, Samantha J., Peng, Sophie X., Leisten, Jim, Khambatta, Godrej, Hickman, Matt, Gamez, James C., Bisonette, René R., Apuy, Julius, Cathers, Brian E., Canan, Stacie S., Moghaddam, Mehran F., Raymon, Heather K., Worland, Peter, Narla, Rama Krishna, Fultz, Kimberly E., Sankar, Sabita
Published in Journal of medicinal chemistry (23.07.2015)
Published in Journal of medicinal chemistry (23.07.2015)
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Journal Article
A Novel Triazolopyridine-Based Spleen Tyrosine Kinase Inhibitor That Arrests Joint Inflammation
Ferguson, Gregory D, Delgado, Mercedes, Plantevin-Krenitsky, Veronique, Jensen-Pergakes, Kristen, Bates, R J, Torres, Sanaa, Celeridad, Maria, Brown, Heather, Burnett, Kelven, Nadolny, Lisa, Tehrani, Lida, Packard, Garrick, Pagarigan, Barbra, Haelewyn, Jason, Nguyen, Trish, Xu, Li, Tang, Yang, Hickman, Matthew, Baculi, Frans, Pierce, Steven, Miyazawa, Keiji, Jackson, Pilgrim, Chamberlain, Philip, LeBrun, Laurie, Xie, Weilin, Bennett, Brydon, Blease, Kate
Published in PloS one (12.01.2016)
Published in PloS one (12.01.2016)
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Journal Article
Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors
Packard, Garrick K., Papa, Patrick, Riggs, Jennifer R., Erdman, Paul, Tehrani, Lida, Robinson, Dale, Harris, Roy, Shevlin, Graziella, Perrin-Ninkovic, Sophie, Hilgraf, Robert, McCarrick, Margaret A., Tran, Tam, Fleming, Yuedi, Bai, April, Richardson, Samantha, Katz, Jason, Tang, Yang, Leisten, Jim, Moghaddam, Mehran, Cathers, Brian, Zhu, Dan, Sakata, Steven
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
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Synthesis of Rimocidinolide Methyl Ester, the Aglycone of (+)-Rimocidin
Packard, Garrick K., Hu, Yueqing, Vescovi, Andrea, Rychnovsky, Scott D.
Published in Angewandte Chemie (International ed.) (17.05.2004)
Published in Angewandte Chemie (International ed.) (17.05.2004)
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Synthesis and structure–activity relationship of 3,4′-bispyridinylethylenes: Discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer
Li, Qun, Woods, Keith W., Thomas, Sheela, Zhu, Gui-Dong, Packard, Garrick, Fisher, John, Li, Tongmei, Gong, Jianchun, Dinges, Jurgen, Song, Xiaohong, Abrams, Jason, Luo, Yan, Johnson, Eric F., Shi, Yan, Liu, Xuesong, Klinghofer, Vered, Des Jong, Ron, Oltersdorf, Tilman, Stoll, Vincent S., Jakob, Clarissa G., Rosenberg, Saul H., Giranda, Vincent L.
Published in Bioorganic & medicinal chemistry letters (01.04.2006)
Published in Bioorganic & medicinal chemistry letters (01.04.2006)
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Journal Article
ASGPR 세포 표면 수용체 결합 화합물 및 접합체
BUSCH BRETT BRADLEY, TURTLE ERIC D, ERNST JUSTIN THOMAS, PACKARD GARRICK K, LEWIS JASON G
Year of Publication 20.03.2024
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Year of Publication 20.03.2024
Patent
세포 표면 수용체 결합 화합물 및 접합체
BUSCH BRETT BRADLEY, TURTLE ERIC D, ERNST JUSTIN THOMAS, PACKARD GARRICK K, LEWIS JASON G
Year of Publication 27.10.2022
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Year of Publication 27.10.2022
Patent
CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization
Mortensen, Deborah S, Fultz, Kimberly E, Xu, Shuichan, Xu, Weiming, Packard, Garrick, Khambatta, Godrej, Gamez, James C, Leisten, Jim, Zhao, Jingjing, Apuy, Julius, Ghoreishi, Kamran, Hickman, Matt, Narla, Rama Krishna, Bissonette, Rene, Richardson, Samantha, Peng, Sophie X, Perrin-Ninkovic, Sophie, Tran, Tam, Shi, Tao, Yang, Wen Qing, Tong, Zeen, Cathers, Brian E, Moghaddam, Mehran F, Canan, Stacie S, Worland, Peter, Sankar, Sabita, Raymon, Heather K
Published in Molecular cancer therapeutics (01.06.2015)
Published in Molecular cancer therapeutics (01.06.2015)
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Journal Article
Abstract B33: Targeting PI3K/mTOR signaling with potent, selective and orally-available small-molecule inhibitors of eIF4E
Parker, Gregory S., Hung, Ivy N.J., Staunton, Jocelyn, Barrera, Maria, Sung, Eric, Parra, Ana, Stumpf, Craig R., Chen, Joan, Thompson, Peggy A., Nevarez, Andreas, Wegerski, Christopher J., Clarine, Jeff, Sperry, Samuel, Xiang, Alan, Nilewski, Christian, Packard, Garrick K., Urklalan, Kaveri, Mukaiyama, Takasuke, Michels, Theo, Ernst, Justin T., Sprengeler, Paul A., Reich, Siegfried H., Chiang, Gary G., Webster, Kevin R.
Published in Molecular cancer research (01.10.2020)
Published in Molecular cancer research (01.10.2020)
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Journal Article
Abstract 2698: eFT226, a potent and selective inhibitor of eIF4A, is efficacious in preclinical models of lymphoma
Thompson, Peggy A., Eam, Boreth, Young, Nathan P., Fish, Sarah, Chen, Joan, Barrera, Maria, Howard, Haleigh, Sung, Eric, Parra, Ana, Staunton, Jocelyn, Chiang, Gary G., Wegerski, Christopher J., Nevarez, Andres, Clarine, Jeff, Sperry, Samuel, Xiang, Alan, Tran, Chinh, Nilewski, Christian, Packard, Garrick K., Michels, Theodore, Sprengeler, Paul A., Ernst, Justin T., Reich, Siegfried H., Webster, Kevin R.
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Abstract 1302: Targeting hormone receptor-dependent cancers with potent, selective and orally-available small molecule inhibitors of eIF4E
Chiang, Gary G., Parker, Gregory S., Hung, Ivy N., Goel, Vikas K., Staunton, Jocelyn, Barrera, Maria, Sung, Eric, Parra, Ana, Stumpf, Craig R., Chen, Joan, Thompson, Peggy A., Nevarez, Andreas, Wegerski, Christopher J., Parker, Cody, Clarine, Jeff, Sperry, Samuel, Xiang, Alan, Nilewski, Christian, Packard, Garrick K., Urkalan, Kaveri, Mukaiyama, Takasuke, Michels, Theo, Ernst, Justin T., Sprengeler, Paul A., Reich, Siegfried H., Webster, Kevin R.
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Abstract DDT02-05: eFT226: A selective and highly potent inhibitor of eukaryotic initiation factor 4A (eIF4A), a novel approach for the treatment of cancer
Reich, Siegfried H., Thompson, Peggy A., Ernst, Justin T., Eam, Boreth, Young, Nathan P., Fish, Sarah, Chen, Joan, Barrera, Maria, Howard, Haleigh, Parra, Ana, Sung, Eric, Staunton, Jocelyn, Hung, Ivy Nj, Parker, Gregory S., Chiang, Gary G., Wegerski, Christopher J., Nevarez, Andres, Clarine, Jeff, Sperry, Samuel, Xiang, Alan, Tran, Chinh, Nilewski, Christian, Packard, Garrick K., Michels, Theodore, Sprengeler, Paul A., Webster, Kevin R.
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Journal Article
Discovery of Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor CC-223
Mortensen, Deborah S, Perrin-Ninkovic, Sophie M, Shevlin, Graziella, Zhao, Jingjing, Packard, Garrick, Bahmanyar, Sogole, Correa, Matthew, Elsner, Jan, Harris, Roy, Lee, Branden G. S, Papa, Patrick, Parnes, Jason S, Riggs, Jennifer R, Sapienza, John, Tehrani, Lida, Whitefield, Brandon, Apuy, Julius, Bisonette, René R, Gamez, James C, Hickman, Matt, Khambatta, Godrej, Leisten, Jim, Peng, Sophie X, Richardson, Samantha J, Cathers, Brian E, Canan, Stacie S, Moghaddam, Mehran F, Raymon, Heather K, Worland, Peter, Narla, Rama Krishna, Fultz, Kimberly E, Sankar, Sabita
Published in Journal of medicinal chemistry (09.07.2015)
Published in Journal of medicinal chemistry (09.07.2015)
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Journal Article
Preclinical Evaluation of eFT226, a Novel, Potent and Selective eIF4A Inhibitor with Anti-Tumor Activity in B-Cell Malignancies
Thompson, Peggy A, Eam, Boreth, Young, Nathan P, Fish, Sarah, Chen, Joan, Barrera, Maria, Howard, Haleigh, Parra, Ana, Molter, Jolene, Staunton, Jocelyn, Hung, Ivy NJ, Parker, Greg S, Chiang, Gary G, Wegerski, Chris J, Nevarez, Andres, Clarine, Jeff, Sperry, Sam, Xiang, Alan, Tran, Chinh, Nilewski, Christian, Packard, Garrick K, Michels, Theodore, Sprengeler, Paul A, Ernst, Justin T, Reich, Siegfried H, Webster, Kevin R
Published in Blood (08.12.2017)
Published in Blood (08.12.2017)
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