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Page 1
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. Among authors: chessum ne. Medchemcomm. 2016 Aug 1;7(8):1580-1586. doi: 10.1039/c6md00159a. Epub 2016 Jun 13. Medchemcomm. 2016. PMID: 27746890 Free PMC article.
Recent advances in cancer therapeutics.
Chessum N, Jones K, Pasqua E, Tucker M. Chessum N, et al. Prog Med Chem. 2015;54:1-63. doi: 10.1016/bs.pmch.2014.11.002. Epub 2015 Jan 23. Prog Med Chem. 2015. PMID: 25727702 Review.
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: chessum ne. 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.
Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).
Chessum NEA, Sharp SY, Caldwell JJ, Pasqua AE, Wilding B, Colombano G, Collins I, Ozer B, Richards M, Rowlands M, Stubbs M, Burke R, McAndrew PC, Clarke PA, Workman P, Cheeseman MD, Jones K. Chessum NEA, et al. J Med Chem. 2018 Feb 8;61(3):918-933. doi: 10.1021/acs.jmedchem.7b01406. Epub 2018 Jan 5. J Med Chem. 2018. PMID: 29240418 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: chessum nea. 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: chessum nea. 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.
HSF1 Pathway Inhibitor Clinical Candidate (CCT361814/NXP800) Developed from a Phenotypic Screen as a Potential Treatment for Refractory Ovarian Cancer and Other Malignancies.
Pasqua AE, Sharp SY, Chessum NEA, Hayes A, Pellegrino L, Tucker MJ, Miah A, Wilding B, Evans LE, Rye CS, Mok NY, Liu M, Henley AT, Gowan S, De Billy E, Te Poele R, Powers M, Eccles SA, Clarke PA, Raynaud FI, Workman P, Jones K, Cheeseman MD. Pasqua AE, et al. Among authors: chessum nea. J Med Chem. 2023 Apr 27;66(8):5907-5936. doi: 10.1021/acs.jmedchem.3c00156. Epub 2023 Apr 5. J Med Chem. 2023. PMID: 37017629 Free PMC article.
Determination of Ligand-Binding Affinity (Kd) Using Transverse Relaxation Rate (R2) in the Ligand-Observed 1H NMR Experiment and Applications to Fragment-Based Drug Discovery.
Liu M, Mirza A, McAndrew PC, Thapaliya A, Pierrat OA, Stubbs M, Hahner T, Chessum NEA, Innocenti P, Caldwell J, Cheeseman MD, Bellenie BR, van Montfort RLM, Newton GK, Burke R, Collins I, Hoelder S. Liu M, et al. Among authors: chessum nea. J Med Chem. 2023 Aug 10;66(15):10617-10627. doi: 10.1021/acs.jmedchem.3c00758. Epub 2023 Jul 19. J Med Chem. 2023. PMID: 37467168 Free PMC article.
Synthesis and in vivo evaluation of 3-substituted gababutins.
Blakemore DC, Bryans JS, Carnell P, Chessum NE, Field MJ, Kinsella N, Kinsora JK, Osborne SA, Williams SC. Blakemore DC, et al. Among authors: chessum ne. Bioorg Med Chem Lett. 2010 Jan 1;20(1):362-5. doi: 10.1016/j.bmcl.2009.10.089. Epub 2009 Oct 25. Bioorg Med Chem Lett. 2010. PMID: 19897364
11 results