Molecular mechanisms of human IRE1 activation through dimerization and ligand binding

por Joshi, Amar, Newbatt, Yvette, McAndrew, P. Craig, Stubbs, Mark, Burke, Rosemary, Richards, Mark W., Bhatia, Chitra, Caldwell, John J., McHardy, Tatiana, Collins, Ian, Bayliss, Richard
Publicado 2015

MODL-19. DIPG HARBOUR ALTERATIONS TARGETABLE BY MEK INHIBITORS, WITH ACQUIRED RESISTANCE MECHANISMS OVERCOME BY COMBINATORIAL UP- OR DOWN-STREAM INHIBITION

por Izquierdo, Elisa, Carvalho, Diana, Mackay, Alan, Temelso, Sara, Boult, Jessica K R, Molinari, Valeria, Stubbs, Mark, Depani, Sarita, O’Hare, Patricia, Robinson, Simon P, Hubank, Michael, Hargrave, Darren, Jones, Chris
Publicado 2020

Targeted therapy for LIMD1-deficient non-small cell lung cancer subtypes

por Davidson, Kathryn, Grevitt, Paul, Contreras-Gerenas, Maria F., Bridge, Katherine S., Hermida, Miguel, Shah, Kunal M., Mardakheh, Faraz K., Stubbs, Mark, Burke, Rosemary, Casado, Pedro, Cutillas, Pedro R., Martin, Sarah A., Sharp, Tyson V.
Publicado 2021

Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)

por Chessum, Nicola E. A., Sharp, Swee Y., Caldwell, John J., Pasqua, A. Elisa, Wilding, Birgit, Colombano, Giampiero, Collins, Ian, Ozer, Bugra, Richards, Meirion, Rowlands, Martin, Stubbs, Mark, Burke, Rosemary, McAndrew, P. Craig, Clarke, Paul A., Workman, Paul, Cheeseman, Matthew D., Jones, Keith
Publicado 2017

Exploiting evolutionary steering to induce collateral drug sensitivity in cancer

por Acar, Ahmet, Nichol, Daniel, Fernandez-Mateos, Javier, Cresswell, George D., Barozzi, Iros, Hong, Sung Pil, Trahearn, Nicholas, Spiteri, Inmaculada, Stubbs, Mark, Burke, Rosemary, Stewart, Adam, Caravagna, Giulio, Werner, Benjamin, Vlachogiannis, Georgios, Maley, Carlo C., Magnani, Luca, Valeri, Nicola, Banerji, Udai, Sottoriva, Andrea
Publicado 2020

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

2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19

por Mallinger, Aurélie, Schiemann, Kai, Rink, Christian, Sejberg, Jimmy, Honey, Mark A., Czodrowski, Paul, Stubbs, Mark, Poeschke, Oliver, Busch, Michael, Schneider, Richard, Schwarz, Daniel, Musil, Djordje, Burke, Rosemary, Urbahns, Klaus, Workman, Paul, Wienke, Dirk, Clarke, Paul A., Raynaud, Florence I., Eccles, Suzanne A., Esdar, Christina, Rohdich, Felix, Blagg, Julian
Publicado 2016

iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells

por Bouguenina, Habib, Nicolaou, Stephanos, Le Bihan, Yann-Vaï, Bowling, Elizabeth A., Calderon, Cheyenne, Caldwell, John J., Harrington, Brinley, Hayes, Angela, McAndrew, P. Craig, Mitsopoulos, Costas, Sialana, Fernando Jr., Scarpino, Andrea, Stubbs, Mark, Thapaliya, Arjun, Tyagi, Siddhartha, Wang, Hannah Z., Wood, Francesca, Burke, Rosemary, Raynaud, Florence, Choudhary, Jyoti, van Montfort, Rob L.M., Sadok, Amine, Westbrook, Thomas F., Collins, Ian, Chopra, Rajesh
Publicado 2023

Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19

por Mallinger, Aurélie, Schiemann, Kai, Rink, Christian, Stieber, Frank, Calderini, Michel, Crumpler, Simon, Stubbs, Mark, Adeniji-Popoola, Olajumoke, Poeschke, Oliver, Busch, Michael, Czodrowski, Paul, Musil, Djordje, Schwarz, Daniel, Ortiz-Ruiz, Maria-Jesus, Schneider, Richard, Thai, Ching, Valenti, Melanie, de Haven Brandon, Alexis, Burke, Rosemary, Workman, Paul, Dale, Trevor, Wienke, Dirk, Clarke, Paul A., Esdar, Christina, Raynaud, Florence I., Eccles, Suzanne A., Rohdich, Felix, Blagg, Julian
Publicado 2016

A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease

por Dale, Trevor, Clarke, Paul A., Esdar, Christina, Waalboer, Dennis, Adeniji-Popoola, Olajumoke, Ortiz-Ruiz, Maria-Jesus, Mallinger, Aurélie, Samant, Rahul S., Czodrowski, Paul, Musil, Djordje, Schwarz, Daniel, Schneider, Klaus, Stubbs, Mark, Ewan, Ken, Fraser, Elizabeth, TePoele, Robert, Court, Will, Box, Gary, Valenti, Melanie, de Haven Brandon, Alexis, Gowan, Sharon, Rohdich, Felix, Raynaud, Florence, Schneider, Richard, Poeschke, Oliver, Blaukat, Andree, Workman, Paul, Schiemann, Kai, Eccles, Suzanne A., Wienke, Dirk, Blagg, Julian
Publicado 2015

Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen

por Mallinger, Aurélie, Crumpler, Simon, Pichowicz, Mark, Waalboer, Dennis, Stubbs, Mark, Adeniji-Popoola, Olajumoke, Wood, Bozena, Smith, Elizabeth, Thai, Ching, Henley, Alan T., Georgi, Katrin, Court, William, Hobbs, Steve, Box, Gary, Ortiz-Ruiz, Maria-Jesus, Valenti, Melanie, De Haven Brandon, Alexis, TePoele, Robert, Leuthner, Birgitta, Workman, Paul, Aherne, Wynne, Poeschke, Oliver, Dale, Trevor, Wienke, Dirk, Esdar, Christina, Rohdich, Felix, Raynaud, Florence, Clarke, Paul A., Eccles, Suzanne A., Stieber, Frank, Schiemann, Kai, Blagg, Julian
Publicado 2015

MIR21 Drives Resistance to Heat Shock Protein 90 Inhibition in Cholangiocarcinoma

por Lampis, Andrea, Carotenuto, Pietro, Vlachogiannis, Georgios, Cascione, Luciano, Hedayat, Somaieh, Burke, Rosemary, Clarke, Paul, Bosma, Else, Simbolo, Michele, Scarpa, Aldo, Yu, Sijia, Cole, Rebecca, Smyth, Elizabeth, Mateos, Javier Fernández, Begum, Ruwaida, Hezelova, Blanka, Eltahir, Zakaria, Wotherspoon, Andrew, Fotiadis, Nicos, Bali, Maria Antonietta, Nepal, Chirag, Khan, Khurum, Stubbs, Mark, Hahne, Jens C., Gasparini, Pierluigi, Guzzardo, Vincenza, Croce, Carlo M., Eccles, Suzanne, Fassan, Matteo, Cunningham, David, Andersen, Jesper B., Workman, Paul, Valeri, Nicola, Braconi, Chiara
Publicado 2018

DIPG Harbors Alterations Targetable by MEK Inhibitors, with Acquired Resistance Mechanisms Overcome by Combinatorial Inhibition

por Izquierdo, Elisa, Carvalho, Diana M., Mackay, Alan, Temelso, Sara, Boult, Jessica K.R., Pericoli, Giulia, Fernandez, Elisabet, Das, Molina, Molinari, Valeria, Grabovska, Yura, Rogers, Rebecca F., Ajmone-Cat, Maria Antonietta, Proszek, Paula Z., Stubbs, Mark, Depani, Sarita, O'Hare, Patricia, Yu, Lu, Roumelioti, Georgia, Choudhary, Jyoti S., Clarke, Matthew, Fairchild, Amy R., Jacques, Thomas S., Grundy, Richard G., Howell, Lisa, Picton, Susan, Adamski, Jenny, Wilson, Shaun, Gray, Juliet C., Zebian, Bassel, Marshall, Lynley V., Carceller, Fernando, Grill, Jacques, Vinci, Maria, Robinson, Simon P., Hubank, Michael, Hargrave, Darren, Jones, Chris
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