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Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9.
Rye CS, Chessum NE, Lamont S, Pike KG, Faulder P, Demeritt J, Kemmitt P, Tucker J, Zani L, Cheeseman MD, Isaac R, Goodwin L, Boros J, Raynaud F, Hayes A, Henley AT, de Billy E, Lynch CJ, Sharp SY, Te Poele R, Fee LO, Foote KM, Green S, Workman P, Jones K. Rye CS, et al. Medchemcomm. 2016 Aug 1;7(8):1580-1586. doi: 10.1039/c6md00159a. Epub 2016 Jun 13. Medchemcomm. 2016. PMID: 27746890 Free PMC article.
Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.
Cheeseman MD, Chessum NE, Rye CS, Pasqua AE, Tucker MJ, Wilding B, Evans LE, Lepri S, Richards M, Sharp SY, Ali S, Rowlands M, O'Fee L, Miah A, Hayes A, Henley AT, Powers M, Te Poele R, De Billy E, Pellegrino L, Raynaud F, Burke R, van Montfort RL, Eccles SA, Workman P, Jones K. Cheeseman MD, et al. Among authors: rye cs. J Med Chem. 2017 Jan 12;60(1):180-201. doi: 10.1021/acs.jmedchem.6b01055. Epub 2016 Dec 22. J Med Chem. 2017. PMID: 28004573 Free PMC article.
HSF1 Is Essential for Myeloma Cell Survival and A Promising Therapeutic Target.
Fok JHL, Hedayat S, Zhang L, Aronson LI, Mirabella F, Pawlyn C, Bright MD, Wardell CP, Keats JJ, De Billy E, Rye CS, Chessum NEA, Jones K, Morgan GJ, Eccles SA, Workman P, Davies FE. Fok JHL, et al. Among authors: rye cs. Clin Cancer Res. 2018 May 15;24(10):2395-2407. doi: 10.1158/1078-0432.CCR-17-1594. Epub 2018 Feb 1. Clin Cancer Res. 2018. PMID: 29391353 Free PMC article.
Privileged Structures and Polypharmacology within and between Protein Families.
Meyers J, Chessum NEA, Ali S, Mok NY, Wilding B, Pasqua AE, Rowlands M, Tucker MJ, Evans LE, Rye CS, O'Fee L, Le Bihan YV, Burke R, Carter M, Workman P, Blagg J, Brown N, van Montfort RLM, Jones K, Cheeseman MD. Meyers J, et al. Among authors: rye cs. ACS Med Chem Lett. 2018 Nov 16;9(12):1199-1204. doi: 10.1021/acsmedchemlett.8b00364. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613326 Free PMC article.
Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.
Koehler MF, Bergeron P, Choo EF, Lau K, Ndubaku C, Dudley D, Gibbons P, Sleebs BE, Rye CS, Nikolakopoulos G, Bui C, Kulasegaram S, Kersten WJ, Smith BJ, Czabotar PE, Colman PM, Huang DC, Baell JB, Watson KG, Hasvold L, Tao ZF, Wang L, Souers AJ, Elmore SW, Flygare JA, Fairbrother WJ, Lessene G. Koehler MF, et al. Among authors: rye cs. ACS Med Chem Lett. 2014 Mar 21;5(6):662-7. doi: 10.1021/ml500030p. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944740 Free PMC article.
Phosphate isosteres in medicinal chemistry.
Rye CS, Baell JB. Rye CS, et al. Curr Med Chem. 2005;12(26):3127-41. doi: 10.2174/092986705774933452. Curr Med Chem. 2005. PMID: 16375706 Review.
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