Enhancer Activation by Pharmacologic Displacement of LSD1 from GFI1 Induces Differentiation in Acute Myeloid Leukemia
Maiques-Diaz, Alba, Spencer, Gary J., Lynch, James T., Ciceri, Filippo, Williams, Emma L., Amaral, Fabio M.R., Wiseman, Daniel H., Harris, William J., Li, Yaoyong, Sahoo, Sudhakar, Hitchin, James R., Mould, Daniel P., Fairweather, Emma E., Waszkowycz, Bohdan, Jordan, Allan M., Smith, Duncan L., Somervaille, Tim C.P.
Published in Cell reports (Cambridge) (27.03.2018)
Published in Cell reports (Cambridge) (27.03.2018)
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Journal Article
First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib
James, Dominic I, Smith, Kate M, Jordan, Allan M, Fairweather, Emma E, Griffiths, Louise A, Hamilton, Nicola S, Hitchin, James R, Hutton, Colin P, Jones, Stuart, Kelly, Paul, McGonagle, Alison E, Small, Helen, Stowell, Alexandra I. J, Tucker, Julie, Waddell, Ian D, Waszkowycz, Bohdan, Ogilvie, Donald J
Published in ACS chemical biology (18.11.2016)
Published in ACS chemical biology (18.11.2016)
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Journal Article
Mechanistic and evolutionary insights into isoform-specific ‘supercharging’ in DCLK family kinases
Venkat, Aarya, Watterson, Grace, Byrne, Dominic P, O'Boyle, Brady, Shrestha, Safal, Gravel, Nathan, Fairweather, Emma E, Daly, Leonard A, Bunn, Claire, Yeung, Wayland, Aggarwal, Ishan, Katiyar, Samiksha, Eyers, Claire E, Eyers, Patrick A, Kannan, Natarajan
Published in eLife (26.10.2023)
Published in eLife (26.10.2023)
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Journal Article
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, Bohdan, Smith, Kate M, McGonagle, Alison E, Jordan, Allan M, Acton, Ben, Fairweather, Emma E, Griffiths, Louise A, Hamilton, Niall M, Hamilton, Nicola S, Hitchin, James R, Hutton, Colin P, James, Dominic I, Jones, Clifford D, Jones, Stuart, Mould, Daniel P, Small, Helen F, Stowell, Alexandra I. J, Tucker, Julie A, Waddell, Ian D, Ogilvie, Donald J
Published in Journal of medicinal chemistry (13.12.2018)
Published in Journal of medicinal chemistry (13.12.2018)
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Journal Article
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity
Newton, Rebecca, Bowler, Katherine A., Burns, Emily M., Chapman, Philip J., Fairweather, Emma E., Fritzl, Samantha J.R., Goldberg, Kristin M., Hamilton, Niall M., Holt, Sarah V., Hopkins, Gemma V., Jones, Stuart D., Jordan, Allan M., Lyons, Amanda J., Nikki March, H., McDonald, Neil Q., Maguire, Laura A., Mould, Daniel P., Purkiss, Andrew G., Small, Helen F., Stowell, Alexandra I.J., Thomson, Graeme J., Waddell, Ian D., Waszkowycz, Bohdan, Watson, Amanda J., Ogilvie, Donald J.
Published in European journal of medicinal chemistry (13.04.2016)
Published in European journal of medicinal chemistry (13.04.2016)
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Journal Article
Novel Steroid Inhibitors of Glucose 6-Phosphate Dehydrogenase
Hamilton, Niall M, Dawson, Martin, Fairweather, Emma E, Hamilton, Nicola S, Hitchin, James R, James, Dominic I, Jones, Stuart D, Jordan, Allan M, Lyons, Amanda J, Small, Helen F, Thomson, Graeme J, Waddell, Ian D, Ogilvie, Donald J
Published in Journal of medicinal chemistry (10.05.2012)
Published in Journal of medicinal chemistry (10.05.2012)
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Journal Article
An assay to measure poly(ADP ribose) glycohydrolase (PARG) activity in cells [version 2; peer review: 2 approved]
James, Dominic I, Durant, Stephen, Eckersley, Kay, Fairweather, Emma, Griffiths, Louise A, Hamilton, Nicola, Kelly, Paul, O'Connor, Mark, Shea, Kerry, Waddell, Ian D, Ogilvie, Donald J
Published in F1000 research (2016)
Published in F1000 research (2016)
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Journal Article
Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments
Hitchin, James R., Blagg, Julian, Burke, Rosemary, Burns, Samantha, Cockerill, Mark J., Fairweather, Emma E., Hutton, Colin, Jordan, Allan M., McAndrew, Craig, Mirza, Amin, Mould, Daniel, Thomson, Graeme J., Waddell, Ian, Ogilvie, Donald J.
Published in MedChemComm (01.11.2013)
Published in MedChemComm (01.11.2013)
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Journal Article
An assay to measure poly(ADP ribose) glycohydrolase (PARG) activity in cells
James, Dominic I, Durant, Stephen, Eckersley, Kay, Fairweather, Emma, Griffiths, Louise A, Hamilton, Nicola, Kelly, Paul, O'Connor, Mark, Shea, Kerry, Waddell, Ian D, Ogilvie, Donald J
Published in F1000 research (2016)
Published in F1000 research (2016)
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Journal Article
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia
Pappalardi, Melissa B, Keenan, Kathryn, Cockerill, Mark, Kellner, Wendy A, Stowell, Alexandra, Sherk, Christian, Wong, Kristen, Pathuri, Sarath, Briand, Jacques, Steidel, Michael, Chapman, Philip, Groy, Arthur, Wiseman, Ashley K, McHugh, Charles F, Campobasso, Nino, Graves, Alan P, Fairweather, Emma, Werner, Thilo, Raoof, Ali, Butlin, Roger J, Rueda, Lourdes, Horton, John R, Fosbenner, David T, Zhang, Cunyu, Handler, Jessica L, Muliaditan, Morris, Mebrahtu, Makda, Jaworski, Jon-Paul, McNulty, Dean E, Burt, Charlotte, Eberl, H Christian, Taylor, Amy N, Ho, Thau, Merrihew, Susan, Foley, Shawn W, Rutkowska, Anna, Li, Mei, Romeril, Stuart P, Goldberg, Kristin, Zhang, Xing, Kershaw, Christopher S, Bantscheff, Marcus, Jurewicz, Anthony J, Minthorn, Elisabeth, Grandi, Paola, Patel, Mehul, Benowitz, Andrew B, Mohammad, Helai P, Gilmartin, Aidan G, Prinjha, Rab K, Ogilvie, Donald, Carpenter, Christopher, Heerding, Dirk, Baylin, Stephen B, Jones, Peter A, Cheng, Xiaodong, King, Bryan W, Luengo, Juan I, Jordan, Allan M, Waddell, Ian, Kruger, Ryan G, McCabe, Michael T
Published in Nature cancer (01.10.2021)
Published in Nature cancer (01.10.2021)
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Journal Article
Mechanistic and evolutionary insights into isoform-specific ‘supercharging’ in DCLK family kinases
Venkat, Aarya, Watterson, Grace, Byrne, Dominic P, O'Boyle, Brady, Shrestha, Safal, Gravel, Nathan, Fairweather, Emma E, Daly, Leonard A, Bunn, Claire, Yeung, Wayland, Aggarwal, Ishan, Katiyar, Samiksha, Eyers, Claire E, Eyers, Patrick A, Kannan, Natarajan
Published in eLife (26.10.2023)
Published in eLife (26.10.2023)
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Journal Article
Mechanism of APTX nicked DNA sensing and pleiotropic inactivation in neurodegenerative disease
Tumbale, Percy, Schellenberg, Matthew J, Mueller, Geoffrey A, Fairweather, Emma, Watson, Mandy, Little, Jessica N, Krahn, Juno, Waddell, Ian, London, Robert E, Williams, R Scott
Published in The EMBO journal (13.07.2018)
Published in The EMBO journal (13.07.2018)
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Journal Article
Abstract LB-068: Development of a screening cascade to identify selective small molecule inhibitors of DNMT1
Stowell, Alexandra, Thomson, Graeme, Cockerill, Mark, Burt, Charlotte, Fairweather, Emma, Waddell, Ian, Raoof, Ali, Jordan, Allan, 0gilvie, Donald, Pappalardi, Melissa, Luengo, Juan, Patel, Mehul, Kruger, Ryan, Carpenter, Chris
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Journal Article
Discovery and Optimization of Allosteric Inhibitors of Mutant Isocitrate Dehydrogenase 1 (R132H IDH1) Displaying Activity in Human Acute Myeloid Leukemia Cells
Jones, Stuart, Ahmet, Jonathan, Ayton, Kelly, Ball, Matthew, Cockerill, Mark, Fairweather, Emma, Hamilton, Nicola, Harper, Paul, Hitchin, James, Jordan, Allan, Levy, Colin, Lopez, Ruth, McKenzie, Eddie, Packer, Martin, Plant, Darren, Simpson, Iain, Simpson, Peter, Sinclair, Ian, Somervaille, Tim C. P, Small, Helen, Spencer, Gary J, Thomson, Graeme, Tonge, Michael, Waddell, Ian, Walsh, Jarrod, Waszkowycz, Bohdan, Wigglesworth, Mark, Wiseman, Daniel H, Ogilvie, Donald
Published in Journal of medicinal chemistry (22.12.2016)
Published in Journal of medicinal chemistry (22.12.2016)
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Journal Article
Analysis of human Tribbles 2 (TRIB2) pseudokinase
Harris, John A, Fairweather, Emma, Byrne, Dominic P, Eyers, Patrick A
Published in Methods in enzymology (2022)
Published in Methods in enzymology (2022)
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Abstract 5429: Inhibition of SMARCA2: a novel target for SMARCA4-deficient lung adenocarcinoma
Chapman, Phil, March, Nikki, Thomson, Graeme, Fairweather, Emma, Fritzl, Samantha, Hitchin, James, Hamilton, Nicola, Jordan, Allan, Waddell, Ian, Ogilvie, Donald
Published in Cancer research (Chicago, Ill.) (01.08.2015)
Published in Cancer research (Chicago, Ill.) (01.08.2015)
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Journal Article
Abstract 3656: PARG inhibition: development of novel compounds and a biomarker strategy to determine cell line sensitivity in breast cancer
Waddell, Ian D., James, Dominic, Smith, Kate, Holt, Sarah, Acton, Ben, Fairweather, Emma, Hamilton, Niall, Hamilton, Nicola, Hitchen, James, Huttom, Colin, Jordan, Allan, McGonagle, Alison, Small, Helen, Stowell, Alex, Waszkowycz, Bohdan, Ogilvie, Donald
Published in Cancer research (Chicago, Ill.) (01.08.2015)
Published in Cancer research (Chicago, Ill.) (01.08.2015)
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Journal Article
Abstract C39: First-in-class inhibitors of the putatively undruggable DNA repair target Poly(ADP-ribose) glycohydrolase (PARG)
Waszkowycz, Bohdan, James, Dominic, Acton, Ben, Fairweather, Emma, Fritzl, Sam, Hamilton, Niall, Hamilton, Nicola, Holt, Sarah, Hitchen, James, Hutton, Colin, Jones, Stuart, Jordan, Allan, McGonagle, Alison, Mould, Daniel, Small, Helen, Smith, Kate, Stowell, Alexandra, Waddell, Ian D., Ogilvie, Donald
Published in Molecular cancer therapeutics (01.12.2015)
Published in Molecular cancer therapeutics (01.12.2015)
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Journal Article
Anilinoquinazoline inhibitors of the RET kinase domain—Elaboration of the 7-position
Jordan, Allan M., Begum, Habiba, Fairweather, Emma, Fritzl, Samantha, Goldberg, Kristin, Hopkins, Gemma V., Hamilton, Niall M., Lyons, Amanda J., March, H. Nikki, Newton, Rebecca, Small, Helen F., Vishwanath, Swamy, Waddell, Ian D., Waszkowycz, Bohdan, Watson, Amanda J., Ogilvie, Donald J.
Published in Bioorganic & medicinal chemistry letters (01.06.2016)
Published in Bioorganic & medicinal chemistry letters (01.06.2016)
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