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Structure-Based Discovery of Potent, Orally Bioavailable Benzoxazepinone-Based WD Repeat Domain 5 Inhibitors.
Teuscher KB, Mills JJ, Tian J, Han C, Meyers KM, Sai J, South TM, Crow MM, Van Meveren M, Sensintaffar JL, Zhao B, Amporndanai K, Moore WJ, Stott GM, Tansey WP, Lee T, Fesik SW. Teuscher KB, et al. Among authors: fesik sw. J Med Chem. 2023 Dec 28;66(24):16783-16806. doi: 10.1021/acs.jmedchem.3c01529. Epub 2023 Dec 12. J Med Chem. 2023. PMID: 38085679
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.
Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A.
Patrone JD, Kennedy JP, Frank AO, Feldkamp MD, Vangamudi B, Pelz NF, Rossanese OW, Waterson AG, Chazin WJ, Fesik SW. Patrone JD, et al. Among authors: fesik sw. ACS Med Chem Lett. 2013 Jul 11;4(7):601-605. doi: 10.1021/ml400032y. ACS Med Chem Lett. 2013. PMID: 23914285 Free PMC article.
Fragment-based screening of the bromodomain of ATAD2.
Harner MJ, Chauder BA, Phan J, Fesik SW. Harner MJ, et al. Among authors: fesik sw. J Med Chem. 2014 Nov 26;57(22):9687-92. doi: 10.1021/jm501035j. Epub 2014 Nov 11. J Med Chem. 2014. PMID: 25314628 Free PMC article.
Diphenylpyrazoles as replication protein a inhibitors.
Waterson AG, Kennedy JP, Patrone JD, Pelz NF, Feldkamp MD, Frank AO, Vangamudi B, Souza-Fagundes EM, Rossanese OW, Chazin WJ, Fesik SW. Waterson AG, et al. Among authors: fesik sw. ACS Med Chem Lett. 2014 Nov 11;6(2):140-5. doi: 10.1021/ml5003629. eCollection 2015 Feb 12. ACS Med Chem Lett. 2014. PMID: 25699140 Free PMC article.
Interaction with WDR5 promotes target gene recognition and tumorigenesis by MYC.
Thomas LR, Wang Q, Grieb BC, Phan J, Foshage AM, Sun Q, Olejniczak ET, Clark T, Dey S, Lorey S, Alicie B, Howard GC, Cawthon B, Ess KC, Eischen CM, Zhao Z, Fesik SW, Tansey WP. Thomas LR, et al. Among authors: fesik sw. Mol Cell. 2015 May 7;58(3):440-52. doi: 10.1016/j.molcel.2015.02.028. Epub 2015 Mar 26. Mol Cell. 2015. PMID: 25818646 Free PMC article.
230 results