Translation control of the immune checkpoint in cancer and its therapeutic targeting
Xu, Yichen, Poggio, Mauro, Jin, Hyun Yong, Shi, Zhen, Forester, Craig M, Wang, Ying, Stumpf, Craig R, Xue, Lingru, Devericks, Emily, So, Lomon, Nguyen, Hao G, Griselin, Alice, Gordan, John D, Umetsu, Sarah E, Reich, Siegfried H, Worland, Stephen T, Asthana, Saurabh, Barna, Maria, Webster, Kevin R, Cunningham, John T, Ruggero, Davide
Published in Nature medicine (01.02.2019)
Published in Nature medicine (01.02.2019)
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Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase
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Published in Journal of medicinal chemistry (11.06.2020)
Published in Journal of medicinal chemistry (11.06.2020)
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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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Molecular Characteristics of Repotrectinib That Enable Potent Inhibition of TRK Fusion Proteins and Resistant Mutations
Murray, Brion W, Rogers, Evan, Zhai, Dayong, Deng, Wei, Chen, Xi, Sprengeler, Paul A, Zhang, Xin, Graber, Armin, Reich, Siegfried H, Stopatschinskaja, Shanna, Solomon, Benjamin, Besse, Benjamin, Drilon, Alexander
Published in Molecular cancer therapeutics (01.12.2021)
Published in Molecular cancer therapeutics (01.12.2021)
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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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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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SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo
Buchanan, Sean G, Hendle, Jorg, Lee, Patrick S, Smith, Christopher R, Bounaud, Pierre-Yves, Jessen, Katti A, Tang, Crystal M, Huser, Nanni H, Felce, Jeremy D, Froning, Karen J, Peterman, Marshall C, Aubol, Brandon E, Gessert, Steve F, Sauder, J Michael, Schwinn, Kenneth D, Russell, Marijane, Rooney, Isabelle A, Adams, Jason, Leon, Barbara C, Do, Tuan H, Blaney, Jeff M, Sprengeler, Paul A, Thompson, Devon A, Smyth, Lydia, Pelletier, Laura A, Atwell, Shane, Holme, Kevin, Wasserman, Stephen R, Emtage, Spencer, Burley, Stephen K, Reich, Siegfried H
Published in Molecular cancer therapeutics (01.12.2009)
Published in Molecular cancer therapeutics (01.12.2009)
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Structure-Based Design and Synthesis of Substituted 2-Butanols as Nonpeptidic Inhibitors of HIV Protease: Secondary Amide Series
Reich, Siegfried H, Melnick, Michael, Pino, Mark J, Fuhry, Mary Ann M, Trippe, Anthony J, Appelt, Krzysztof, Davies, Jay F, Wu, Bor-Wen, Musick, Linda
Published in Journal of medicinal chemistry (05.07.1996)
Published in Journal of medicinal chemistry (05.07.1996)
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Bis Tertiary Amide Inhibitors of the HIV-1 Protease Generated via Protein Structure-Based Iterative Design
Melnick, Michael, Reich, Siegfried H, Lewis, Kathy K, Mitchell, Lennert J, Nguyen, Dzuy, Trippe, Anthony J, Dawson, Heather, Davies, Jay F, Appelt, Krzysztof, Wu, Bor-Wen, Musick, Linda, Gehlhaar, Dan K, Webber, Stephanie, Shetty, Bhasker, Kosa, Maha, Kahil, Deborah, Andrada, Dominic
Published in Journal of medicinal chemistry (05.07.1996)
Published in Journal of medicinal chemistry (05.07.1996)
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MNK 억제제의 결정질 형태
XIANG ALAN X, WILSON JO ANN Z, SPERRY SAMUEL, WEBBER STEPHEN E, SPRENGELER PAUL A, REICH SIEGFRIED H, BORER BENNETT C, ERNST JUSTIN T
Year of Publication 19.08.2021
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Year of Publication 19.08.2021
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Design and synthesis of novel 6,7-imidazotetrahydroquinoline inhibitors of thymidylate synthase using iterative protein crystal structure analysis
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Published in Journal of medicinal chemistry (01.03.1992)
Published in Journal of medicinal chemistry (01.03.1992)
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EIF4E-억제 4-옥소-3,4-디히드로피리도[3,4-D]피리미딘 화합물
NILEWSKI CHRISTIAN, PACKARD GARRICK KENNETH, MICHELS THEO, SPRENGELER PAUL A, MUKAIYAMA TAKASUKE, URKALAN KAVERI, ERNST JUSTIN T, XIANG ALAN X, SHAGHAFI MIKE, SPERRY SAMUEL, GRUBBS ALAN, REICH SIEGFRIED H, TRAN CHINH VIET
Year of Publication 13.05.2022
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Year of Publication 13.05.2022
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Enantioselective total synthesis of 9S-dihydroerythronolide A seco acid
Chamberlin, A. Richard, Dezube, Milana, Reich, Siegfried H, Sall, Daniel J
Published in Journal of the American Chemical Society (01.08.1989)
Published in Journal of the American Chemical Society (01.08.1989)
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MNK1 및 MNK2를 억제하는 피롤로-, 피라졸로-, 이미다조-피리미딘 및 피리딘 화합물
WEBBER STEPHEN E, SPRENGELER PAUL A, REICH SIEGFRIED H, ERNST JUSTIN T
Year of Publication 26.06.2018
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Year of Publication 26.06.2018
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MNK1 및 MNK2의 이소인돌린, 아자이소인돌린, 디히드로인데논 및 디히드로아자인데논 억제제
TRAN CHINH, SHAGHAFI MIKE, WEBBER STEPHEN E, SPRENGELER PAUL A, REICH SIEGFRIED H, ERNST JUSTIN T, MURPHY DOUGLAS
Year of Publication 26.06.2018
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Year of Publication 26.06.2018
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Structure-Based Design of a Parallel Synthetic Array Directed Toward the Discovery of Irreversible Inhibitors of Human Rhinovirus 3C Protease
Johnson, Theodore O, Hua, Ye, Luu, Hiep T, Brown, Edward L, Chan, Fora, Chu, Shao Song, Dragovich, Peter S, Eastman, Brian W, Ferre, Rose Ann, Fuhrman, Shella A, Hendrickson, Thomas F, Maldonado, Fausto C, Matthews, David A, Meador, James W, Patick, Amy K, Reich, Siegfried H, Skalitzky, Donald J, Worland, Stephen T, Yang, Michelle, Zalman, Leora S
Published in Journal of medicinal chemistry (09.05.2002)
Published in Journal of medicinal chemistry (09.05.2002)
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Tripeptide Aldehyde Inhibitors of Human Rhinovirus 3C Protease: Design, Synthesis, Biological Evaluation, and Cocrystal Structure Solution of P1 Glutamine Isosteric Replacements
Webber, Stephen E, Okano, Koji, Little, Thomas L, Reich, Siegfried H, Xin, Yue, Fuhrman, Shella A, Matthews, David A, Love, Robert A, Hendrickson, Thomas F, Patick, Amy K, Meador, James W, Ferre, Rose Ann, Brown, Edward L, Ford, Clifford E, Binford, Susan L, Worland, Stephen T
Published in Journal of medicinal chemistry (16.07.1998)
Published in Journal of medicinal chemistry (16.07.1998)
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Mnk MNK INHIBITORS AND METHODS RELATED THERETO
XIANG ALAN XIN, ERNST JUSTIN THOMAS, WEBBER STEPHEN E, SPRENGELER PAUL A, REICH SIEGFRIED H
Year of Publication 02.03.2017
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Year of Publication 02.03.2017
Patent