未登录 Pulsatile induction of the p53 pathway by MDM2 antagonist ASTX295 shows an enhanced therapeutic index in vivo Fazal, L.; Biondo, A.; Ahn, M.; Bevan, L.; Hearn, K.; Howard, S.; Jueliger, S.; Chessari, G.; Kucia-Tran, J.; Shah, A.; Sims, M.; Wilsher, N.; Keer, H.; Organesian, A.; Wedge, S.; Thomas, H.; Zhao, Y.; Newell, D.; Wallis, N.; Courtin, A. 分享 收藏
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Targeting the MDM2-p53 interaction: Time- and concentration-dependent studies in tumor and normal human bone marrow cells reveal strategies for an enhanced therapeutic index Willmore, Elaine; Ahn, Maria; Kyle, Suzanne; Zhao, Yan; Thomas, Huw; Rankin, Kenneth S.; Bevan, Luke; Fazal, Lynsey; Hearn, Keisha; Wilsher, Nicola; Kucia-Tran, Justyna; Ferrari, Nicola; Wallis, Nicola; Thompson, Neil; Lyons, John; Miller, Duncan; Cano, Celine; Noble, Martin E.; Hardcastle, Ian R.; Howard, Steven; Chessari, Gianni; Lunec, John; Newell, David R.; Wedge, Steve R. 分享 收藏
Discovery of ASTX295, a potent, next-generation small molecule antagonist of MDM2 with differentiated pharmacokinetic profile Ahn, Maria; Bevan, Luke; Buck, Ildiko; Cano, Celine; Castro, Juan; Cons, Ben; Endicott, Jane; Fazal, Lynsey; Ferrari, Nicola; Hardcastle, Ian; Hearn, Keisha; Holvey, Rhian; Howard, Steven; Johnson, Chris; Jennings, Claire; Kucia-Tran, Justyna; Kyle, Suzanne; Lunec, John; Lyons, John; Miller, Duncan; Rees, David; Noble, Martin; Newell, David R.; Reeks, Judith; Saini, Harpreet; Denis, Jeffrey St.; Tamanini, Emiliano; Thomas, Huw; Thompson, Neil; Vinkovic, Mladen; Ward, George; Wallis, Nicola; Walton, Hugh; Wedge, Stephen; Williams, Pamela; Willmore, Elaine; Wilshire, Nicola; Zhao, Yan; Chessari, Gianni 分享 收藏
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor Miller, Duncan C.; Reuillon, Tristan; Molyneux, Lauren; Blackburn, Timothy; Cook, Simon J.; Edwards, Noel; Endicott, Jane A.; Golding, Bernard T.; Griffin, Roger J.; Hardcastle, Ian; Harnor, Suzannah J.; Heptinstall, Amy; Lochhead, Pamela; Martin, Mathew P.; Martin, Nick C.; Myers, Stephanie; Newell, David R.; Noble, Richard A.; Phillips, Nicole; Rigoreau, Laurent; Thomas, Huw; Tucker, Julie A.; Wang, Lan-Zhen; Waring, Michael J.; Wong, Ai-Ching; Wedge, Stephen R.; Noble, Martin E. M.; Cano, Celine 分享 收藏
Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein-Protein Interaction Chessari, Gianni; Hardcastle, Ian R.; Ahn, Jong Sook; Anil, Burcu; Anscombe, Elizabeth; Bawn, Ruth H.; Bevan, Luke D.; Blackburn, Timothy J.; Buck, Ildiko; Cano, Celine; Carbain, Benoit; Castro, Juan; Cons, Ben; Cully, Sarah J.; Endicott, Jane A.; Fazal, Lynsey; Golding, Bernard T.; Griffin, Roger J.; Haggerty, Karen; Harnor, Suzannah J.; Hearn, Keisha; Hobson, Stephen; Holvey, Rhian S.; Howard, Steven; Jennings, Claire E.; Johnson, Christopher N.; Lunec, John; Miller, Duncan C.; Newell, David R.; Noble, Martin E. M.; Reeks, Judith; Revill, Charlotte H.; Riedinger, Christiane; St Denis, Jeffrey D.; Tamanini, Emiliano; Thomas, Huw; Thompson, Neil T.; Vinkovic, Mladen; Wedge, Stephen R.; Williams, Pamela A.; Wilsher, Nicola E.; Zhang, Bian; Zhao, Yan 分享 收藏
2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase Matheson, Christopher J.; Coxon, Christopher R.; Bayliss, Richard; Boxall, Kathy; Carbain, Benoit; Fry, Andrew M.; Hardcastle, Ian R.; Harnor, Suzannah J.; Mas-Droux, Corine; Newell, David R.; Richards, Mark W.; Sivaprakasam, Mangaleswaran; Turner, David; Griffin, Roger J.; Golding, Bernard T.; Cano, Celine 分享 收藏
Selective DNA-PKcs inhibition extends the therapeutic index of localized radiotherapy and chemotherapy Willoughby, Catherine E.; Jiang, Yanyan; Thomas, Huw D.; Willmore, Elaine; Kyle, Suzanne; Wittner, Anita; Phillips, Nicole; Zhao, Yan; Tudhope, Susan J.; Prendergast, Lisa; Junge, Gesa; Lourenco, Luiza Madia; Finlay, M. Raymond V.; Turner, Paul; Munck, Joanne M.; Griffin, Roger J.; Rennison, Tommy; Pickles, James; Cano, Celine; Newell, David R.; Reeves, Helen L.; Ryan, Anderson J.; Wedge, Stephen R. 分享 收藏
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4 Myers, Stephanie M.; Miller, Duncan C.; Molyneux, Lauren; Arasta, Mercedes; Bawn, Ruth H.; Blackburn, Timothy J.; Cook, Simon J.; Edwards, Noel; Endicott, Jane A.; Golding, Bernard T.; Griffin, Roger J.; Hammonds, Tim; Hardcastle, Ian R.; Harnor, Suzannah J.; Heptinstall, Amy B.; Lochhead, Pamela A.; Martin, Mathew P.; Martin, Nick C.; Newell, David R.; Owen, Paul J.; Pang, Leon C.; Reuillo, Tristan; Rigoreau, Laurent J. M.; Thomas, Huw D.; Tucker, Julie A.; Wang, Lan-Zhen; Wong, Ai-Ching; Noble, Martin E. M.; Wedge, Stephen R.; Cano, Celine 分享 收藏
Glucocorticoids and selumetinib are highly synergistic in RAS pathway-mutated childhood acute lymphoblastic leukemia through upregulation of BIM Matheson, Elizabeth C.; Thomas, Huw; Case, Marian; Blair, Helen; Jackson, Rosanna K.; Masic, Dino; Veal, Gareth; Halsey, Chris; Newell, David R.; Vormoor, Josef; Irving, Julie A. E. 分享 收藏
Preclinical evaluation of the first intravenous small molecule MDM2 antagonist alone and in combination with temozolomide in neuroblastoma Chen, Lindi; Pastorino, Fabio; Berry, Philip; Bonner, Jennifer; Kirk, Calum; Wood, Katrina M.; Thomas, Huw D.; Zhao, Yan; Daga, Antonio; Veal, Gareth J.; Lunec, John; Newell, David R.; Ponzoni, Mirco; Tweddle, Deborah A. 分享 收藏
Highly Potent Clickable Probe for Cellular Imaging of MDM2 and Assessing Dynamic Responses to MDM2-p53 Inhibition Lebraud, Honorine; Noble, Richard A.; Phillips, Nicole; Heam, Keisha; Castro, Juan; Zhao, Yan; Newell, David R.; Lunec, John; Wedge, Stephen R.; Heightman, Tom D. 分享 收藏
Treating cat allergy with monoclonal IgG antibodies that bind allergen and prevent IgE engagement Orengo, J. M.; Radin, A. R.; Kamat, V.; Badithe, A.; Ben, L. H.; Bennett, B. L.; Zhong, S.; Birchard, D.; Limnander, A.; Rafique, A.; Bautista, J.; Kostic, A.; Newell, D.; Duan, X.; Franklin, M. C.; Olson, W.; Huang, T.; Gandhi, N. A.; Lipsich, L.; Stahl, N.; Papadopoulos, N. J.; Murphy, A. J.; Yancopoulos, G. D. 分享 收藏
In vivo evaluation of the intravenous MDM2-p53 antagonist RO6839921 alone and in combination with temozolomide in TP53 wild-type orthotopic models of neuroblastoma Chen, Lindi; Pastorino, Fabio; Berry, Philip; Bonner, Jennifer; Wood, Katrina; Veal, Gareth; Ponzoni, Mirco; Lunec, John; Newell, David R.; Tweddle, Deborah A. 分享 收藏
Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor Perera, Timothy P. S.; Jovcheva, Eleonora; Mevellec, Laurence; Vialard, Jorge; De lange, Desiree; Verhulst, Tinne; Paulussen, Caroline; Van De Ven, Kelly; King, Peter; Freyne, Eddy; Rees, David C.; Squires, Matthew; Saxty, Gordon; Page, Martin; Murray, Christopher W.; Gilissen, Ron; Ward, George; Thompson, Neil T.; Newell, David R.; Cheng, Na; Xie, Liang; Yang, Jennifer; Platero, Suso J.; Karkera, Jayaprakash D.; Moy, Christopher; Angibaud, Patrick; Laquerre, Sylvie; Lorenzi, Matthew V. 分享 收藏
Cyclin-Dependent Kinase (CDK) Inhibitors: Structure Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines Coxon, Christopher R.; Anscombe, Elizabeth; Harnor, Suzannah J.; Martin, Mathew P.; Carbain, Benoit; Golding, Bernard T.; Hardcastle, Ian R.; Harlow, Lisa K.; Korolchuk, Svitlana; Matheson, Christopher J.; Newel, David R.; Noble, Martin E. M.; Sivaprakasam, Mangaleswaran; Tudhope, Susan J.; Turner, David M.; Wang, Lan Z.; Wedge, Stephen R.; Wong, Christopher; Griffin, Roger J.; Endicott, Jane A.; Cano, Celine 分享 收藏
Sulfatase-2: a prognostic biomarker and candidate therapeutic target in patients with pancreatic ductal adenocarcinoma Sulfatase-2: 胰腺导管腺癌患者的预后生物标志物和候选治疗靶点 Alhasan, Sari F.; Haugk, Beate; Ogle, Laura F.; Beale, Gary S.; Long, Anna; Burt, Alastair D.; Tiniakos, Dina; Televantou, Despina; Coxon, Fareeda; Newell, David R.; Charnley, Richard; Reeves, Helen L. 分享 收藏
Combined PI3K and CDK2 inhibition induces cell death and enhances in vivo antitumour activity in colorectal cancer Beale, Gary; Haagensen, Emma J.; Thomas, Huw D.; Wang, Lan-Zhen; Revill, Charlotte H.; Payne, Sara L.; Golding, Bernard T.; Hardcastle, Ian R.; Newell, David R.; Griffin, Roger J.; Cano, Celine 分享 收藏
Tumor cells with KRAS or BRAF mutations or ERK5/MAPK7 amplification are not addicted to ERK5 activity for cell proliferation Lochhead, Pamela A.; Clark, Jonathan; Wang, Lan-Zhen; Gilmour, Lesley; Squires, Matthew; Gilley, Rebecca; Foxton, Caroline; Newell, David R.; Wedge, Stephen R.; Cook, Simon J. 分享 收藏
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