Publications
2022
Kinome-based evaluation of drug-resistance mechanisms in human cancer
Fairweather, E. (2022, September 27). Kinome-based evaluation of drug-resistance mechanisms in human cancer.
2021
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia
Pappalardi, M. B., Keenan, K., Cockerill, M., Kellner, W. A., Stowell, A., Sherk, C., . . . McCabe, M. T. (2021). Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. NATURE CANCER, 2(10), 1002-+. doi:10.1038/s43018-021-00249-x
2018
Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides
Waszkowycz, B., Smith, K. M., McGonagle, A. E., Jordan, A. M., Acton, B., Fairweather, E. E., . . . Ogilvie, D. J. (2018). Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides. JOURNAL OF MEDICINAL CHEMISTRY, 61(23), 10767-10792. doi:10.1021/acs.jmedchem.8b01407
Mechanism of APTX nicked DNA sensing and pleiotropic inactivation in neurodegenerative disease
Tumbale, P., Schellenberg, M. J., Mueller, G. A., Fairweather, E., Watson, M., Little, J. N., . . . Williams, R. S. (2018). Mechanism of APTX nicked DNA sensing and pleiotropic inactivation in neurodegenerative disease. EMBO JOURNAL, 37(14). doi:10.15252/embj.201798875
Enhancer Activation by Pharmacologic Displacement of LSD1 from GFI1 Induces Differentiation in Acute Myeloid Leukemia
Maiques-Diaz, A., Spencer, G. J., Lynch, J. T., Ciceri, F., Williams, E. L., Amaral, F. M. R., . . . Somervaille, T. C. P. (2018). Enhancer Activation by Pharmacologic Displacement of LSD1 from GFI1 Induces Differentiation in Acute Myeloid Leukemia. CELL REPORTS, 22(13), 3641-3659. doi:10.1016/j.celrep.2018.03.012
2016
Discovery and Optimization of Allosteric Inhibitors of Mutant Isocitrate Dehydrogenase 1 (R132H IDH1) Displaying Activity in Human Acute Myeloid Leukemia Cells
Jones, S., Ahmet, J., Ayton, K., Ball, M., Cockerill, M., Fairweather, E., . . . Ogilvie, D. (2016). Discovery and Optimization of Allosteric Inhibitors of Mutant Isocitrate Dehydrogenase 1 (R132H IDH1) Displaying Activity in Human Acute Myeloid Leukemia Cells. JOURNAL OF MEDICINAL CHEMISTRY, 59(24), 11120-11137. doi:10.1021/acs.jmedchem.6b01320
First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib
James, D. I., Smith, K. M., Jordan, A. M., Fairweather, E. E., Griffiths, L. A., Hamilton, N. S., . . . Ogilvie, D. J. (2016). First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib. ACS CHEMICAL BIOLOGY, 11(11), 3179-3190. doi:10.1021/acschembio.6b00609
Anilinoquinazoline inhibitors of the RET kinase domain-Elaboration of the 7-position
Jordan, A. M., Begum, H., Fairweather, E., Fritzl, S., Goldberg, K., Hopkins, G. V., . . . Ogilvie, D. J. (2016). Anilinoquinazoline inhibitors of the RET kinase domain-Elaboration of the 7-position. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 26(11), 2724-2729. doi:10.1016/j.bmcl.2016.03.100
An assay to measure poly(ADP ribose) glycohydrolase (PARG) activity in cells
James, D. I., Durant, S., Eckersley, K., Fairweather, E., Griffiths, L. A., Hamilton, N., . . . Ogilvie, D. J. (n.d.). An assay to measure poly(ADP ribose) glycohydrolase (PARG) activity in cells. F1000Research, 5, 736. doi:10.12688/f1000research.8463.1
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity
Newton, R., Bowler, K. A., Burns, E. M., Chapman, P. J., Fairweather, E. E., Fritzl, S. J. R., . . . Ogilvie, D. J. (2016). The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 112, 20-32. doi:10.1016/j.ejmech.2016.01.039
An assay to measure poly(ADP ribose) glycohydrolase (PARG) activity in cells.
James, D. I., Durant, S., Eckersley, K., Fairweather, E., Griffiths, L. A., Hamilton, N., . . . Ogilvie, D. J. (2016). An assay to measure poly(ADP ribose) glycohydrolase (PARG) activity in cells.. F1000Research, 5, 736. doi:10.12688/f1000research.8463.2
2013
Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments
Hitchin, J. R., Blagg, J., Burke, R., Burns, S., Cockerill, M. J., Fairweather, E. E., . . . Ogilvie, D. J. (2013). Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments. MEDCHEMCOMM, 4(11), 1513-1522. doi:10.1039/c3md00226h
2012
Novel Steroid Inhibitors of Glucose 6-Phosphate Dehydrogenase
Hamilton, N. M., Dawson, M., Fairweather, E. E., Hamilton, N. S., Hitchin, J. R., James, D. I., . . . Ogilvie, D. J. (2012). Novel Steroid Inhibitors of Glucose 6-Phosphate Dehydrogenase. JOURNAL OF MEDICINAL CHEMISTRY, 55(9), 4431-4445. doi:10.1021/jm300317k