Serine is a natural ligand and allosteric activator of pyruvate kinase M2
Chaneton, Barbara, Hillmann, Petra, Zheng, Liang, Martin, Agnès C. L., Maddocks, Oliver D. K., Chokkathukalam, Achuthanunni, Coyle, Joseph E., Jankevics, Andris, Holding, Finn P., Vousden, Karen H., Frezza, Christian, O’Reilly, Marc, Gottlieb, Eyal
Published in Nature (London) (15.11.2012)
Published in Nature (London) (15.11.2012)
Get full text
Journal Article
Crystallographic screening using ultra-low-molecular-weight ligands to guide drug design
O’Reilly, Marc, Cleasby, Anne, Davies, Thomas G., Hall, Richard J., Ludlow, R. Frederick, Murray, Christopher W., Tisi, Dominic, Jhoti, Harren
Published in Drug discovery today (01.05.2019)
Published in Drug discovery today (01.05.2019)
Get full text
Journal Article
X‑ray Screening of an Electrophilic Fragment Library and Application toward the Development of a Novel ERK 1/2 Covalent Inhibitor
St. Denis, Jeffrey D., Chessari, Gianni, Cleasby, Anne, Cons, Benjamin D., Cowan, Suzanna, Dalton, Samuel E., East, Charlotte, Murray, Christopher W., O’Reilly, Marc, Peakman, Torren, Rapti, Magdalini, Stow, Jessie L.
Published in Journal of medicinal chemistry (22.09.2022)
Published in Journal of medicinal chemistry (22.09.2022)
Get full text
Journal Article
Dual-Mechanism ERK1/2 Inhibitors Exploit a Distinct Binding Mode to Block Phosphorylation and Nuclear Accumulation of ERK1/2
Kidger, Andrew M, Munck, Joanne M, Saini, Harpreet K, Balmanno, Kathryn, Minihane, Emma, Courtin, Aurelie, Graham, Brent, O'Reilly, Marc, Odle, Richard, Cook, Simon J
Published in Molecular cancer therapeutics (01.02.2020)
Published in Molecular cancer therapeutics (01.02.2020)
Get full text
Journal Article
Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity
Howard, Steven, Berdini, Valerio, Boulstridge, John A, Carr, Maria G, Cross, David M, Curry, Jayne, Devine, Lindsay A, Early, Theresa R, Fazal, Lynsey, Gill, Adrian L, Heathcote, Michelle, Maman, Sarita, Matthews, Julia E, McMenamin, Rachel L, Navarro, Eva F, O’Brien, Michael A, O’Reilly, Marc, Rees, David C, Reule, Matthias, Tisi, Dominic, Williams, Glyn, Vinković, Mladen, Wyatt, Paul G
Published in Journal of medicinal chemistry (22.01.2009)
Published in Journal of medicinal chemistry (22.01.2009)
Get full text
Journal Article
Fragment-Based Discovery of a Series of Allosteric-Binding Site Modulators of β‑Glucocerebrosidase
Palmer, Nick, Agnew, Christopher, Benn, Caroline, Buffham, William J., Castro, Joan N., Chessari, Gianni, Clark, Mellissa, Cons, Benjamin D., Coyle, Joseph E., Dawson, Lee A., Hamlett, Christopher C. F., Hodson, Charlotte, Holding, Finn, Johnson, Christopher N., Liebeschuetz, John W., Mahajan, Pravin, McCarthy, James M., Murray, Christopher W., O’Reilly, Marc, Peakman, Torren, Price, Amanda, Rapti, Magdalini, Reeks, Judith, Schöpf, Patrick, St-Denis, Jeffrey D., Valenzano, Chiara, Wallis, Nicola G., Walser, Reto, Weir, Heather, Wilsher, Nicola E., Woodhead, Andrew, Bento, Carla F., Tisi, Dominic
Published in Journal of medicinal chemistry (11.07.2024)
Published in Journal of medicinal chemistry (11.07.2024)
Get full text
Journal Article
ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK
Munck, Joanne M, Berdini, Valerio, Bevan, Luke, Brothwood, Jessica L, Castro, Juan, Courtin, Aurélie, East, Charlotte, Ferraldeschi, Roberta, Heightman, Tom D, Hindley, Christopher J, Kucia-Tran, Justyna, Lyons, John F, Martins, Vanessa, Muench, Sandra, Murray, Christopher W, Norton, David, O'Reilly, Marc, Reader, Michael, Rees, David C, Rich, Sharna J, Richardson, Caroline J, Shah, Alpesh D, Stanczuk, Lukas, Thompson, Neil T, Wilsher, Nicola E, Woolford, Alison J-A, Wallis, Nicola G
Published in Molecular cancer therapeutics (01.10.2021)
Published in Molecular cancer therapeutics (01.10.2021)
Get full text
Journal Article
Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2
Heightman, Tom D, Berdini, Valerio, Braithwaite, Hannah, Buck, Ildiko M, Cassidy, Megan, Castro, Juan, Courtin, Aurélie, Day, James E. H, East, Charlotte, Fazal, Lynsey, Graham, Brent, Griffiths-Jones, Charlotte M, Lyons, John F, Martins, Vanessa, Muench, Sandra, Munck, Joanne M, Norton, David, O’Reilly, Marc, Palmer, Nick, Pathuri, Puja, Reader, Michael, Rees, David C, Rich, Sharna J, Richardson, Caroline, Saini, Harpreet, Thompson, Neil T, Wallis, Nicola G, Walton, Hugh, Wilsher, Nicola E, Woolford, Alison J.-A, Cooke, Michael, Cousin, David, Onions, Stuart, Shannon, Jonathan, Watts, John, Murray, Christopher W
Published in Journal of medicinal chemistry (14.06.2018)
Published in Journal of medicinal chemistry (14.06.2018)
Get full text
Journal Article
Crystal structure of human CDK4 in complex with a D-type cyclin
Day, Philip J, Cleasby, Anne, Tickle, Ian J, O'Reilly, Marc, Coyle, Joe E, Holding, Finn P, McMenamin, Rachel L, Yon, Jeff, Chopra, Rajiv, Lengauer, Christoph, Jhoti, Harren
Published in Proceedings of the National Academy of Sciences - PNAS (17.03.2009)
Published in Proceedings of the National Academy of Sciences - PNAS (17.03.2009)
Get full text
Journal Article
Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2
Heightman, Tom D., Berdini, Valerio, Bevan, Luke, Buck, Ildiko M., Carr, Maria G., Courtin, Aurelie, Coyle, Joseph E., Day, James E. H., East, Charlotte, Fazal, Lynsey, Griffiths-Jones, Charlotte M., Howard, Steven, Kucia-Tran, Justyna, Martins, Vanessa, Muench, Sandra, Munck, Joanne M., Norton, David, O'Reilly, Marc, Palmer, Nicholas, Pathuri, Puja, Peakman, Torren M., Reader, Michael, Rees, David C., Rich, Sharna J., Shah, Alpesh, Wallis, Nicola G., Walton, Hugh, Wilsher, Nicola E., Woolford, Alison J-A, Cooke, Michael, Cousin, David, Onions, Stuart, Shannon, Jonathan, Watts, John, Murray, Christopher W.
Published in Journal of medicinal chemistry (26.08.2021)
Published in Journal of medicinal chemistry (26.08.2021)
Get full text
Journal Article
Identification of N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design
Wyatt, Paul G, Woodhead, Andrew J, Berdini, Valerio, Boulstridge, John A, Carr, Maria G, Cross, David M, Davis, Deborah J, Devine, Lindsay A, Early, Theresa R, Feltell, Ruth E, Lewis, E. Jonathan, McMenamin, Rachel L, Navarro, Eva F, O’Brien, Michael A, O’Reilly, Marc, Reule, Matthias, Saxty, Gordon, Seavers, Lisa C. A, Smith, Donna-Michelle, Squires, Matt S, Trewartha, Gary, Walker, Margaret T, Woolford, Alison J.-A
Published in Journal of medicinal chemistry (28.08.2008)
Published in Journal of medicinal chemistry (28.08.2008)
Get full text
Journal Article
4-(Pyrazol-4-yl)-pyrimidines as Selective Inhibitors of Cyclin-Dependent Kinase 4/6
Cho, Young Shin, Borland, Maria, Brain, Christopher, Chen, Christine H.-T, Cheng, Hong, Chopra, Rajiv, Chung, Kristy, Groarke, James, He, Guo, Hou, Ying, Kim, Sunkyu, Kovats, Steven, Lu, Yipin, O’Reilly, Marc, Shen, Junqing, Smith, Troy, Trakshel, Gary, Vögtle, Markus, Xu, Mei, Xu, Ming, Sung, Moo Je
Published in Journal of medicinal chemistry (25.11.2010)
Published in Journal of medicinal chemistry (25.11.2010)
Get full text
Journal Article
Telomerases
O’Reilly, Marc, Teichmann, Sarah A, Rhodes, Daniela
Published in Current opinion in structural biology (01.02.1999)
Published in Current opinion in structural biology (01.02.1999)
Get full text
Journal Article