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Drugging the undruggable RAS: Mission possible?
Cox AD, Fesik SW, Kimmelman AC, Luo J, Der CJ. Cox AD, et al. Among authors: fesik sw. Nat Rev Drug Discov. 2014 Nov;13(11):828-51. doi: 10.1038/nrd4389. Epub 2014 Oct 17. Nat Rev Drug Discov. 2014. PMID: 25323927 Free PMC article. Review.
Drugging an undruggable pocket on KRAS.
Kessler D, Gmachl M, Mantoulidis A, Martin LJ, Zoephel A, Mayer M, Gollner A, Covini D, Fischer S, Gerstberger T, Gmaschitz T, Goodwin C, Greb P, Häring D, Hela W, Hoffmann J, Karolyi-Oezguer J, Knesl P, Kornigg S, Koegl M, Kousek R, Lamarre L, Moser F, Munico-Martinez S, Peinsipp C, Phan J, Rinnenthal J, Sai J, Salamon C, Scherbantin Y, Schipany K, Schnitzer R, Schrenk A, Sharps B, Siszler G, Sun Q, Waterson A, Wolkerstorfer B, Zeeb M, Pearson M, Fesik SW, McConnell DB. Kessler D, et al. Among authors: fesik sw. Proc Natl Acad Sci U S A. 2019 Aug 6;116(32):15823-15829. doi: 10.1073/pnas.1904529116. Epub 2019 Jul 22. Proc Natl Acad Sci U S A. 2019. PMID: 31332011 Free PMC article.
Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation.
Sun Q, Burke JP, Phan J, Burns MC, Olejniczak ET, Waterson AG, Lee T, Rossanese OW, Fesik SW. Sun Q, et al. Among authors: fesik sw. Angew Chem Int Ed Engl. 2012 Jun 18;51(25):6140-3. doi: 10.1002/anie.201201358. Epub 2012 May 8. Angew Chem Int Ed Engl. 2012. PMID: 22566140 Free PMC article. No abstract available.
Twenty years on: the impact of fragments on drug discovery.
Erlanson DA, Fesik SW, Hubbard RE, Jahnke W, Jhoti H. Erlanson DA, et al. Among authors: fesik sw. Nat Rev Drug Discov. 2016 Sep;15(9):605-619. doi: 10.1038/nrd.2016.109. Epub 2016 Jul 15. Nat Rev Drug Discov. 2016. PMID: 27417849 Review.
Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling.
Abbott JR, Hodges TR, Daniels RN, Patel PA, Kennedy JP, Howes JE, Akan DT, Burns MC, Sai J, Sobolik T, Beesetty Y, Lee T, Rossanese OW, Phan J, Waterson AG, Fesik SW. Abbott JR, et al. Among authors: fesik sw. J Med Chem. 2018 Jul 26;61(14):6002-6017. doi: 10.1021/acs.jmedchem.8b00360. Epub 2018 Jul 11. J Med Chem. 2018. PMID: 29856609
Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction.
Macdonald JD, Chacón Simon S, Han C, Wang F, Shaw JG, Howes JE, Sai J, Yuh JP, Camper D, Alicie BM, Alvarado J, Nikhar S, Payne W, Aho ER, Bauer JA, Zhao B, Phan J, Thomas LR, Rossanese OW, Tansey WP, Waterson AG, Stauffer SR, Fesik SW. Macdonald JD, et al. Among authors: fesik sw. J Med Chem. 2019 Dec 26;62(24):11232-11259. doi: 10.1021/acs.jmedchem.9b01411. Epub 2019 Dec 5. J Med Chem. 2019. PMID: 31724864 Free PMC article.
227 results