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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 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: thompson 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: thompson 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
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. 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
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: thompson 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
Discovery of tricyclic 5,6-dihydro-1H-pyridin-2-ones as novel, potent, and orally bioavailable inhibitors of HCV NS5B polymerase.
Ruebsam F, Murphy DE, Tran CV, Li LS, Zhao J, Dragovich PS, McGuire HM, Xiang AX, Sun Z, Ayida BK, Blazel JK, Kim SH, Zhou Y, Han Q, Kissinger CR, Webber SE, Showalter RE, Shah AM, Tsan M, Patel RA, Thompson PA, Lebrun LA, Hou HJ, Kamran R, Sergeeva MV, Bartkowski DM, Nolan TG, Norris DA, Khandurina J, Brooks J, Okamoto E, Kirkovsky L. Ruebsam F, et al. Among authors: thompson pa. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6404-12. doi: 10.1016/j.bmcl.2009.09.045. Epub 2009 Sep 17. Bioorg Med Chem Lett. 2009. PMID: 19818610
Structure of hepatitis C virus IRES subdomain IIa.
Zhao Q, Han Q, Kissinger CR, Hermann T, Thompson PA. Zhao Q, et al. Among authors: thompson pa. Acta Crystallogr D Biol Crystallogr. 2008 Apr;64(Pt 4):436-43. doi: 10.1107/S0907444908002011. Epub 2008 Mar 19. Acta Crystallogr D Biol Crystallogr. 2008. PMID: 18391410
534 results