2022
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 (Journal article)
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-xDOI: 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 (Journal article)
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.8b01407DOI: 10.1021/acs.jmedchem.8b01407
Mechanism of APTX nicked DNA sensing and pleiotropic inactivation in neurodegenerative disease (Journal article)
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.201798875DOI: 10.15252/embj.201798875
Enhancer Activation by Pharmacologic Displacement of LSD1 from GFI1 Induces Differentiation in Acute Myeloid Leukemia (Journal article)
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.2018.03.012DOI: 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 (Journal article)
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.6b01320DOI: 10.1021/acs.jmedchem.6b01320
First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib (Journal article)
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.6b00609DOI: 10.1021/acschembio.6b00609
Anilinoquinazoline inhibitors of the RET kinase domain-Elaboration of the 7-position (Journal article)
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.2016.03.100DOI: 10.1016/j.bmcl.2016.03.100
An assay to measure poly(ADP ribose) glycohydrolase (PARG) activity in cells (Journal article)
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.8463.1DOI: 10.12688/f1000research.8463.1
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity (Journal article)
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.2016.01.039DOI: 10.1016/j.ejmech.2016.01.039
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.8463.2DOI: 10.12688/f1000research.8463.2
2013
Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments (Journal article)
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/c3md00226hDOI: 10.1039/c3md00226h
2012
Novel Steroid Inhibitors of Glucose 6-Phosphate Dehydrogenase (Journal article)
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/jm300317kDOI: 10.1021/jm300317k
