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Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A.
Thompson PA, Eam B, Young NP, Fish S, Chen J, Barrera M, Howard H, Sung E, Parra A, Staunton J, Chiang GG, Gerson-Gurwitz A, Wegerski CJ, Nevarez A, Clarine J, Sperry S, Xiang A, Nilewski C, Packard GK, Michels T, Tran C, Sprengeler PA, Ernst JT, Reich SH, Webster KR. Thompson PA, et al. Among authors: sprengeler pa. Mol Cancer Ther. 2021 Jan;20(1):26-36. doi: 10.1158/1535-7163.MCT-19-0973. Epub 2020 Oct 9. Mol Cancer Ther. 2021. PMID: 33037136
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 SH, Sprengeler PA, Chiang GG, Appleman JR, Chen J, Clarine J, Eam B, Ernst JT, Han Q, Goel VK, Han EZR, Huang V, Hung INJ, Jemison A, Jessen KA, Molter J, Murphy D, Neal M, Parker GS, Shaghafi M, Sperry S, Staunton J, Stumpf CR, Thompson PA, Tran C, Webber SE, Wegerski CJ, Zheng H, Webster KR. Reich SH, et al. Among authors: sprengeler pa. J Med Chem. 2018 Apr 26;61(8):3516-3540. doi: 10.1021/acs.jmedchem.7b01795. Epub 2018 Mar 29. J Med Chem. 2018. PMID: 29526098
Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase.
Ernst JT, Thompson PA, Nilewski C, Sprengeler PA, Sperry S, Packard G, Michels T, Xiang A, Tran C, Wegerski CJ, Eam B, Young NP, Fish S, Chen J, Howard H, Staunton J, Molter J, Clarine J, Nevarez A, Chiang GG, Appleman JR, Webster KR, Reich SH. Ernst JT, et al. Among authors: sprengeler pa. J Med Chem. 2020 Jun 11;63(11):5879-5955. doi: 10.1021/acs.jmedchem.0c00182. Epub 2020 May 29. J Med Chem. 2020. PMID: 32470302
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 C, Michels TD, Packard GK, Xiang AX, Sprengeler PA, Eam B, Fish S, Thompson PA, Wegerski CJ, Nevarez A, Clarine J, Sperry S, Ernst JT, Reich SH. Nilewski C, et al. Among authors: sprengeler pa. Bioorg Med Chem Lett. 2021 Sep 1;47:128111. doi: 10.1016/j.bmcl.2021.128111. Epub 2021 Aug 2. Bioorg Med Chem Lett. 2021. PMID: 34353608
SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo.
Buchanan SG, Hendle J, Lee PS, Smith CR, Bounaud PY, Jessen KA, Tang CM, Huser NH, Felce JD, Froning KJ, Peterman MC, Aubol BE, Gessert SF, Sauder JM, Schwinn KD, Russell M, Rooney IA, Adams J, Leon BC, Do TH, Blaney JM, Sprengeler PA, Thompson DA, Smyth L, Pelletier LA, Atwell S, Holme K, Wasserman SR, Emtage S, Burley SK, Reich SH. Buchanan SG, et al. Among authors: sprengeler pa. Mol Cancer Ther. 2009 Dec;8(12):3181-90. doi: 10.1158/1535-7163.MCT-09-0477. Mol Cancer Ther. 2009. PMID: 19934279
Molecular Characteristics of Repotrectinib That Enable Potent Inhibition of TRK Fusion Proteins and Resistant Mutations.
Murray BW, Rogers E, Zhai D, Deng W, Chen X, Sprengeler PA, Zhang X, Graber A, Reich SH, Stopatschinskaja S, Solomon B, Besse B, Drilon A. Murray BW, et al. Among authors: sprengeler pa. Mol Cancer Ther. 2021 Dec;20(12):2446-2456. doi: 10.1158/1535-7163.MCT-21-0632. Epub 2021 Oct 8. Mol Cancer Ther. 2021. PMID: 34625502 Free PMC article.
Discovery of novel hydroxy pyrazole based factor IXa inhibitor.
Vijaykumar D, Sprengeler PA, Shaghafi M, Spencer JR, Katz BA, Yu C, Rai R, Young WB, Schultz B, Janc J. Vijaykumar D, et al. Among authors: sprengeler pa. Bioorg Med Chem Lett. 2006 May 15;16(10):2796-9. doi: 10.1016/j.bmcl.2006.01.123. Epub 2006 Feb 17. Bioorg Med Chem Lett. 2006. PMID: 16487703
Efforts toward oral bioavailability in factor VIIa inhibitors.
Vijaykumar D, Rai R, Shaghafi M, Ton T, Torkelson S, Leahy EM, Riggs JR, Hu H, Sprengeler PA, Shrader WD, O'Bryan C, Cabuslay R, Sanford E, Gjerstadt E, Liu L, Sukbuntherng J, Young WB. Vijaykumar D, et al. Among authors: sprengeler pa. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3829-32. doi: 10.1016/j.bmcl.2006.04.018. Epub 2006 May 2. Bioorg Med Chem Lett. 2006. PMID: 16650987
53 results