Structure of Rhomboid Protease in Complex with β-Lactam Inhibitors Defines the S2′ Cavity

por Vinothkumar, Kutti R., Pierrat, Olivier A., Large, Jonathan M., Freeman, Matthew
Publicado 2013

The exon junction complex senses energetic stress and regulates contractility and cell architecture in cardiac myocytes

por Pierrat, Olivier A., Paudyal, Anju, Woodruff, James, Koroleva, Olga, Boateng, Samuel Y.
Publicado 2017

Monocyclic β-Lactams Are Selective, Mechanism-Based Inhibitors of Rhomboid Intramembrane Proteases

por Pierrat, Olivier A., Strisovsky, Kvido, Christova, Yonka, Large, Jonathan, Ansell, Keith, Bouloc, Nathalie, Smiljanic, Ela, Freeman, Matthew
Publicado 2010

Determination of Ligand-Binding Affinity (K(d)) Using Transverse Relaxation Rate (R(2)) in the Ligand-Observed (1)H NMR Experiment and Applications to Fragment-Based Drug Discovery

por Liu, Manjuan, Mirza, Amin, McAndrew, P. Craig, Thapaliya, Arjun, Pierrat, Olivier A., Stubbs, Mark, Hahner, Tamas, Chessum, Nicola E. A., Innocenti, Paolo, Caldwell, John, Cheeseman, Matthew D., Bellenie, Benjamin R., van Montfort, Rob L. M., Newton, Gary K., Burke, Rosemary, Collins, Ian, Hoelder, Swen
Publicado 2023

Investigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1

por Wilding, Birgit, Pasqua, A. Elisa, E. A. Chessum, Nicola, Pierrat, Olivier A., Hahner, Tamas, Tomlin, Kathy, Shehu, Erald, Burke, Rosemary, Richards, G. Meirion, Whitton, Bradleigh, Arwert, Esther N., Thapaliya, Arjun, Salimraj, Ramya, van Montfort, Rob, Skawinska, Agi, Hayes, Angela, Raynaud, Florence, Chopra, Rajesh, Jones, Keith, Newton, Gary, Cheeseman, Matthew D.
Publicado 2021

Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket

por Lloyd, Matthew G., Huckvale, Rosemary, Cheung, Kwai-Ming J., Rodrigues, Matthew J., Collie, Gavin W., Pierrat, Olivier A., Gatti Iou, Mahad, Carter, Michael, Davis, Owen A., McAndrew, P. Craig, Gunnell, Emma, Le Bihan, Yann-Vaï, Talbot, Rachel, Henley, Alan T., Johnson, Louise D., Hayes, Angela, Bright, Michael D., Raynaud, Florence I., Meniconi, Mirco, Burke, Rosemary, van Montfort, Rob L. M., Rossanese, Olivia W., Bellenie, Benjamin R., Hoelder, Swen
Publicado 2021

Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors

por Davis, Owen A., Cheung, Kwai-Ming J., Brennan, Alfie, Lloyd, Matthew G., Rodrigues, Matthew J., Pierrat, Olivier A., Collie, Gavin W., Le Bihan, Yann-Vaï, Huckvale, Rosemary, Harnden, Alice C., Varela, Ana, Bright, Michael D., Eve, Paul, Hayes, Angela, Henley, Alan T., Carter, Michael D., McAndrew, P. Craig, Talbot, Rachel, Burke, Rosemary, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Meniconi, Mirco, Bellenie, Benjamin R., Hoelder, Swen
Publicado 2022

Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones

por Harnden, Alice C., Davis, Owen A., Box, Gary M., Hayes, Angela, Johnson, Louise D., Henley, Alan T., de Haven Brandon, Alexis K., Valenti, Melanie, Cheung, Kwai-Ming J., Brennan, Alfie, Huckvale, Rosemary, Pierrat, Olivier A., Talbot, Rachel, Bright, Michael D., Akpinar, Hafize Aysin, Miller, Daniel S. J., Tarantino, Dalia, Gowan, Sharon, de Klerk, Selby, McAndrew, Peter Craig, Le Bihan, Yann-Vaï, Meniconi, Mirco, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Bellenie, Benjamin R., Hoelder, Swen
Publicado 2023

Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders

por Bellenie, Benjamin R., Cheung, Kwai-Ming J., Varela, Ana, Pierrat, Olivier A., Collie, Gavin W., Box, Gary M., Bright, Michael D., Gowan, Sharon, Hayes, Angela, Rodrigues, Matthew J., Shetty, Kartika N., Carter, Michael, Davis, Owen A., Henley, Alan T., Innocenti, Paolo, Johnson, Louise D., Liu, Manjuan, de Klerk, Selby, Le Bihan, Yann-Vaï, Lloyd, Matthew G., McAndrew, P. Craig, Shehu, Erald, Talbot, Rachel, Woodward, Hannah L., Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Hoelder, Swen
Publicado 2020

Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

por Huckvale, Rosemary, Harnden, Alice C., Cheung, Kwai-Ming J., Pierrat, Olivier A., Talbot, Rachel, Box, Gary M., Henley, Alan T., de Haven Brandon, Alexis K., Hallsworth, Albert E., Bright, Michael D., Akpinar, Hafize Aysin, Miller, Daniel S. J., Tarantino, Dalia, Gowan, Sharon, Hayes, Angela, Gunnell, Emma A., Brennan, Alfie, Davis, Owen A., Johnson, Louise D., de Klerk, Selby, McAndrew, Craig, Le Bihan, Yann-Vaï, Meniconi, Mirco, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Bellenie, Benjamin R., Hoelder, Swen
Publicado 2022

Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays

por Pierrat, Olivier A., Liu, Manjuan, Collie, Gavin W., Shetty, Kartika, Rodrigues, Matthew J., Le Bihan, Yann-Vaï, Gunnell, Emma A., McAndrew, P. Craig, Stubbs, Mark, Rowlands, Martin G., Yahya, Norhakim, Shehu, Erald, Talbot, Rachel, Pickard, Lisa, Bellenie, Benjamin R., Cheung, Kwai-Ming J., Drouin, Ludovic, Innocenti, Paolo, Woodward, Hannah, Davis, Owen A., Lloyd, Matthew G., Varela, Ana, Huckvale, Rosemary, Broccatelli, Fabio, Carter, Michael, Galiwango, David, Hayes, Angela, Raynaud, Florence I., Bryant, Christopher, Whittaker, Steven, Rossanese, Olivia W., Hoelder, Swen, Burke, Rosemary, van Montfort, Rob L. M.
Publicado 2022