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
Structure-based Design of Pyridone–Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition
Reich, Siegfried H, Sprengeler, Paul A, Chiang, Gary G, Appleman, James R, Chen, Joan, Clarine, Jeff, Eam, Boreth, Ernst, Justin T, Han, Qing, Goel, Vikas K, Han, Edward Z. R, Huang, Vera, Hung, Ivy N. J, Jemison, Adrianna, Jessen, Katti A, Molter, Jolene, Murphy, Douglas, Neal, Melissa, Parker, Gregory S, Shaghafi, Michael, Sperry, Samuel, Staunton, Jocelyn, Stumpf, Craig R, Thompson, Peggy A, Tran, Chinh, Webber, Stephen E, Wegerski, Christopher J, Zheng, Hong, Webster, Kevin R
Published in Journal of medicinal chemistry (26.04.2018)
Published in Journal of medicinal chemistry (26.04.2018)
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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
Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases
Ernst, Justin T, Liu, Michael, Zuccola, Harmon, Neubert, Timothy, Beaumont, Kevin, Turnbull, Amy, Kallel, Adam, Vought, Bryan, Stamos, Dean
Published in Bioorganic & medicinal chemistry letters (01.01.2014)
Published in Bioorganic & medicinal chemistry letters (01.01.2014)
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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
Identification of Novel HSP90α/β Isoform Selective Inhibitors Using Structure-Based Drug Design. Demonstration of Potential Utility in Treating CNS Disorders such as Huntington’s Disease
Ernst, Justin T, Neubert, Timothy, Liu, Michael, Sperry, Samuel, Zuccola, Harmon, Turnbull, Amy, Fleck, Beth, Kargo, William, Woody, Lisa, Chiang, Peggy, Tran, Dao, Chen, Weichao, Snyder, Phillip, Alcacio, Timothy, Nezami, Azin, Reynolds, James, Alvi, Khisal, Goulet, Lance, Stamos, Dean
Published in Journal of medicinal chemistry (24.04.2014)
Published in Journal of medicinal chemistry (24.04.2014)
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Journal Article
Design and Application of an α-Helix-Mimetic Scaffold Based on an Oligoamide-Foldamer Strategy: Antagonism of the Bak BH3/Bcl-xL Complex
Ernst, Justin T., Becerril, Jorge, Park, Hyung Soon, Yin, Hang, Hamilton, Andrew D.
Published in Angewandte Chemie International Edition (03.02.2003)
Published in Angewandte Chemie International Edition (03.02.2003)
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Journal Article
Terphenyl-Based Bak BH3 α-Helical Proteomimetics as Low-Molecular-Weight Antagonists of Bcl-xL
Yin, Hang, Lee, Gui-in, Sedey, Kristine A, Kutzki, Olaf, Park, Hyung Soon, Orner, Brendan P, Ernst, Justin T, Wang, Hong-Gang, Sebti, Said M, Hamilton, Andrew D
Published in Journal of the American Chemical Society (27.07.2005)
Published in Journal of the American Chemical Society (27.07.2005)
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Journal Article
Development of a Potent Bcl-xL Antagonist Based on α-Helix Mimicry
Kutzki, Olaf, Park, Hyung Soon, Ernst, Justin T, Orner, Brendan P, Yin, Hang, Hamilton, Andrew D
Published in Journal of the American Chemical Society (09.10.2002)
Published in Journal of the American Chemical Society (09.10.2002)
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Journal Article
Optimization of α-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site
Montalban, Antonio Garrido, Boman, Erik, Chang, Chau-Dung, Ceide, Susana Conde, Dahl, Russell, Dalesandro, David, Delaet, Nancy G.J., Erb, Eric, Ernst, Justin T., Gibbs, Andrew, Kahl, Jeffrey, Kessler, Linda, Kucharski, Jeff, Lum, Christopher, Lundström, Jan, Miller, Stephen, Nakanishi, Hiroshi, Roberts, Edward, Saiah, Eddine, Sullivan, Robert, Urban, Jan, Wang, Zhijun, Larson, Christopher J.
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
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Journal Article
The design and synthesis of novel α-ketoamide-based p38 MAP kinase inhibitors
Montalban, Antonio Garrido, Boman, Erik, Chang, Chau-Dung, Ceide, Susana Conde, Dahl, Russell, Dalesandro, David, Delaet, Nancy G.J., Erb, Eric, Ernst, Justin T., Gibbs, Andrew, Kahl, Jeffrey, Kessler, Linda, Lundström, Jan, Miller, Stephen, Nakanishi, Hiroshi, Roberts, Edward, Saiah, Eddine, Sullivan, Robert, Wang, Zhijun, Larson, Christopher J.
Published in Bioorganic & medicinal chemistry letters (15.03.2008)
Published in Bioorganic & medicinal chemistry letters (15.03.2008)
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Journal Article
Protein recognition using synthetic surface-targeted agents
Jain, Rishi, Ernst, Justin T, Kutzki, Olaf, Park, Hyung Soon, Hamilton, Andrew D
Published in Molecular diversity (2004)
Published in Molecular diversity (2004)
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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
Discovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors
Neubert, Timothy, Numa, Mehdi, Ernst, Justin, Clemens, Jeremy, Krenitsky, Paul, Liu, Michael, Fleck, Beth, Woody, Lisa, Zuccola, Harmon, Stamos, Dean
Published in Bioorganic & medicinal chemistry letters (15.03.2015)
Published in Bioorganic & medicinal chemistry letters (15.03.2015)
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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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