未登录 Pharmacological inhibition of PMS2 increases tumor mutational burden, induces microsatellite instability and elicits immune mediated rejection in vivo Piumatti, Eleonora; Hervieu, Alexia; Riou, Philippe; Blagg, Julian; Peall, Adam; Weeks, Sam; Rodriguez-Plata, Maria T.; Rospo, Giuseppe; Arunachalam, Sasi; Meier, Bettina; Tongue, Paige; McLaren, Tessa; Parmar, Kalpesh; Patel, Pradip; Clark, David; Langley, Gareth; Nichols, Charles; Rousseau, Benoit; Winship, Paul; Baker, Matthew; Drysdale, Martin; Germano, Giovanni; Bardelli, Alberto 分享 收藏
Design, Synthesis, and Evaluation of Inhibitors of Hedgehog Acyltransferase Ritzefeld, Markus; Zhang, Leran; Xiao, Zhangping; Andrei, Sebastian A.; Boyd, Olivia; Masumoto, Naoko; Rodgers, Ursula R.; Artelsmair, Markus; Sefer, Lea; Hayes, Angela; Gavriil, Efthymios-Spyridon; Raynaud, Florence I.; Burke, Rosemary; Blagg, Julian; Rzepa, Henry S.; Siebold, Christian; Magee, Anthony I.; Lanyon-Hogg, Thomas; Tate, Edward W. 分享 收藏
NP1867, a potent, selective, covalent small molecule inhibitor of DNA Mismatch Repair (MMR) protein PMS2, functionally inhibits MMR in cells and elicits COSMIC mutational signatures consistent with MMR-deficient patient samples Blagg, Julian; Riou, Philippe; Hervieu, Alexia; Piumatti, Eleonora; Rospo, Giuseppe; Arunachalam, Sasi; Meier, Bettina; Weeks, Sam; Rodriguez, Maria; Parmar, Kalpesh; Patel, Pradip; Peall, Adam; Tongue, Paige; McLaren, Tess; Workman, Robert; Bago, Ruzica; Robjohns, Stuart; Beaumont, Rebecca; Briggs, Mike; Langley, Gareth; Nichols, Charles; Clark, David; Winship, Paul; Rousseau, Benoit; Baker, Matthew; Drysdale, Martin; Germano, Giovanni; Bardelli, Alberto 分享 收藏
Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma Poon, Evon; Liang, Tong; Jamin, Yann; Walz, Susanne; Kwok, Colin; Hakkert, Anne; Barker, Karen; Urban, Zuzanna; Thway, Khin; Zeid, Rhamy; Hallsworth, Albert; Box, Gary; Ebus, Marli E.; Licciardello, Marco P.; Sbirkov, Yordan; Lazaro, Glori; Calton, Elizabeth; Costa, Barbara M.; Valenti, Melanie; Brandon, Alexis De Haven; Webber, Hannah; Tardif, Nicolas; Almeida, Gilberto S.; Christova, Rossitza; Boysen, Gunther; Richards, Mark W.; Barone, Giuseppe; Ford, Anthony; Bayliss, Richard; Clarke, Paul A.; De Bono, Johann; Gray, Nathanael S.; Blagg, Julian; Robinson, Simon P.; Eccles, Suzanne A.; Zheleva, Daniella; Bradner, James E.; Molenaar, Jan; Vivanco, Igor; Eilers, Martin; Workman, Paul; Lin, Charles Y.; Chesler, Louis 分享 收藏
Quizartinib-resistant FLT3-ITD acute myeloid leukemia cells are sensitive to the FLT3-Aurora kinase inhibitor CCT241736 Moore, Andrew S.; Faisal, Amir; Mak, Grace W. Y.; Miraki-Moud, Farideh; Bavetsias, Vassilios; Valenti, Melanie; Box, Gary; Hallsworth, Albert; Brandon, Alexis de Haven; Xavier, Cristina P. R.; Stronge, Randal; Pearson, Andrew D. J.; Blagg, Julian; Raynaud, Florence, I; Chopra, Rajesh; Eccles, Suzanne A.; Taussig, David C.; Linardopoulos, Spiros 分享 收藏
Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species Wood, Francesca L.; Shepherd, Sam; Hayes, Angela; Liu, Manjuan; Grira, Katia; Mok, Yi; Atrash, Butrus; Faisal, Amir; Bavetsias, Vassilios; Linardopoulos, Spiros; Blagg, Julian; Raynaud, Florence, I 分享 收藏
High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers Anderhub, Simon J.; Mak, Grace Wing-Yan; Gurden, Mark D.; Faisal, Amir; Drosopoulos, Konstantinos; Walsh, Katie; Woodward, Hannah L.; Innocenti, Paolo; Westwood, Isaac M.; Naud, Sebastien; Hayes, Angela; Theofani, Efthymia; Filosto, Simone; Saville, Harry; Burke, Rosemary; van Montfort, Rob L. M.; Raynaud, Florence, I; Blagg, Julian; Hoeder, Swen; Eccles, Suzanne A.; Linardopoulos, Spiros 分享 收藏
C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays Le Bihan, Yann-Vai; Lanigan, Rachel M.; Atrash, Butrus; McLaughlin, Mark G.; Velupillai, Srikannathasan; Malcolm, Andrew G.; England, Katherine S.; Ruda, Gian Filippo; Mok, N. Yi; Tumber, Anthony; Tomlin, Kathy; Saville, Harry; Shehu, Erald; McAndrew, Craig; Carmichael, LeAnne; Bennett, James M.; Jeganathan, Fiona; Eve, Paul; Donovan, Adam; Hayes, Angela; Wood, Francesca; Raynaud, Florence I.; Fedorov, Oleg; Brennan, Paul E.; Burke, Rosemary; van Montfort, Rob L. M.; Rossanese, Olivia W.; Blagg, Julian; Bavetsias, Vassilios 分享 收藏
De Novo Missense Substitutions in the Gene Encoding CDK8, a Regulator of the Mediator Complex, Cause a Syndromic Developmental Disorder Calpena, Eduardo; Hervieu, Alexia; Kaserer, Teresa; Swagemakers, Sigrid M. A.; Goos, Jacqueline A. C.; Popoola, Olajumoke; Ortiz-Ruiz, Maria Jesus; Barbaro-Dieber, Tina; Bownass, Lucy; Brilstra, Eva H.; Brimble, Elise; Foulds, Nicola; Grebe, Theresa A.; Harder, Aster V. E.; Lees, Melissa M.; Monaghan, Kristin G.; Newbury-Ecob, Ruth A.; Ong, Kai-Ren; Osio, Deborah; Santos, Francis Jeshira Reynoso; Ruzhnikov, Maura R. Z.; Telegrafi, Aida; van Binsbergen, Ellen; van Dooren, Marieke F.; van der Spek, Peter J.; Blagg, Julian; Twigg, Stephen R. F.; Mathijssen, Irene M. J.; Clarke, Paul A.; Wilkie, Andrew O. M. 分享 收藏
Small-molecule targeting of brachyury transcription factor addiction in chordoma Sharifnia, Tanaz; Wawer, Mathias J.; Chen, Ting; Huang, Qing-Yuan; Weir, Barbara A.; Sizemore, Ann; Lawlor, Matthew A.; Goodale, Amy; Cowley, Glenn S.; Vazquez, Francisca; Ott, Christopher J.; Francis, Joshua M.; Sassi, Slim; Cogswell, Patricia; Sheppard, Hadley E.; Zhang, Tinghu; Gray, Nathanael S.; Clarke, Paul A.; Blagg, Julian; Workman, Paul; Sommer, Josh; Hornicek, Francis; Root, David E.; Hahn, William C.; Bradner, James E.; Wong, Kwok K.; Clemons, Paul A.; Lin, Charles Y.; Kotz, Joanne D.; Schreiber, Stuart L. 分享 收藏
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Privileged Structures and Polypharmacology within and between Protein Families Meyers, Joshua; Chessum, Nicola E. A.; Ali, Salyha; Mok, N. Yi; Wilding, Birgit; Pasqua, A. Elisa; Rowlands, Martin; Tucker, Michael J.; Evans, Lindsay E.; Rye, Carl S.; O'Fee, Lisa; Le Bihan, Yann-Vai; Burke, Rosemary; Carter, Michael; Workman, Paul; Blagg, Julian; Brown, Nathan; van Montfort, Rob L. M.; Jones, Keith; Cheeseman, Matthew D. 分享 收藏
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Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4-d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine (BOS172722) Woodward, Hannah L.; Innocenti, Paolo; Cheung, Kwai-Ming J.; Hayes, Angela; Roberts, Jennie; Henley, Alan T.; Faisal, Amir; Mak, Grace Wing-Yan; Box, Gary; Westwood, Isaac M.; Cronin, Nora; Carter, Michael; Valenti, Melanie; Brandon, Alexis De Haven; O'Fee, Lisa; Saville, Harry; Schmitt, Jessica; Burke, Rosemary; Broccatelli, Fabio; van Montfort, Rob L. M.; Raynaud, Florence, I; Eccles, Suzanne A.; Linardopoulos, Spiros; Blagg, Julian; Hoelder, Swen 分享 收藏
Evaluation of APOBEC3B Recognition Motifs by NMR Reveals Preferred Substrates Liu, Manjuan; Mallinger, Aurelie; Tortorici, Marcello; Newbatt, Yvette; Richards, Meirion; Mirza, Amin; van Montfort, Rob L. M.; Burke, Rosemary; Blagg, Julian; Kaserer, Teresa 分享 收藏
In vitro and in vivo profile of the preclinical candidate and MPS1 kinase inhibitor CCT289346 Woodward, Hannah; Innocenti, Paolo; Cheung, Kwai-Ming J.; Naud, Sebastien; Faisal, Amir; Mak, Grace W.; Hayes, Angela; O'Fee, Lisa; Saville, Harry; Brandon, Alexis De Haven; Roberts, Jennie; Box, Gary; Valenti, Melanie; Heneley, Alan T.; Walsh, Katie; Burke, Rosemary; Eccles, Suzanne A.; Raynaud, Florence I.; Van Montfort, Rob L.; Blagg, Julian; Linardopoulos, Spiros; Hoelder, Swen 分享 收藏
Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor Whittaker, Steven R.; Barlow, Clare; Martin, Mathew P.; Mancusi, Caterina; Wagner, Steve; Self, Annette; Barrie, Elaine; Te Poele, Robert; Sharp, Swee; Brown, Nathan; Wilson, Stuart; Jackson, Wayne; Fischer, Peter M.; Clarke, Paul A.; Walton, Michael I.; McDonald, Edward; Blagg, Julian; Noble, Martin; Garrett, Michelle D.; Workman, Paul 分享 收藏
Exploring isoform-dependent functions of the mediator kinases in colorectal cancer Popoola, Olajumoke O.; Ortiz-Ruiz, Maria J.; Mitsopoulos, Konstantinos; Mallinger, Aurelie; Te-Poele, Robert; Schiemann, Kai; Workman, Paul; Wienke, Dirk; Blagg, Julian; Eccles, Suzanne A.; Clarke, Paul A. 分享 收藏
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Inhibitors of MPS1: Discovery of CCT289346, a highly potent, selective and orally available preclinical candidate Woodward, Hannah L.; Innocenti, Paolo; Cheung, Kwai-Ming J.; Naud, Sebastien; Hayes, Angela; Henley, Alan T.; Faisal, Amir; Mak, Grace; Box, Gary; Westwood, Isaac M.; Carter, Michael; Valenti, Melanie; Brandon, Alexis De Haven; O'Fee, Lisa; Saville, Harry; Burke, Rosemary; Van Montfort, Rob; Raynaud, Florence; Eccles, Suzanne A.; Linardopoulos, Spiros; Blagg, Julian; Hoelder, Swen 分享 收藏
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