未登录 分享 收藏
Fragment-Based Discovery of Allosteric Inhibitors of SH2 Domain-Containing Protein Tyrosine Phosphatase-2 (SHP2) (vol 67, pg 4655, 2024) 基于片段的SH2结构域蛋白酪氨酸磷酸酶-2（SHP2）别构抑制剂的发现（vol 67, pg 4655, 2024） Day, James E. H.; Berdini, Valerio; Castro, Joan; Chessari, Gianni; Davies, Thomas G.; Day, Philip J.; Denis, Jeffrey D. St; Fujiwara, Hideto; Fukaya, Satoshi; Hamlett, Christopher C. F.; Hearn, Keisha; Hiscock, Steven D.; Holvey, Rhian S.; Ito, Satoru; Kandola, Navrohit; Kodama, Yasuo; Liebeschuetz, John W.; Martins, Vanessa; Matsuo, Kenichi; Mortenson, Paul N.; Muench, Sandra; Nakatsuru, Yoko; Ochiiwa, Hiroaki; Palmer, Nicholas; Peakman, Torren; Price, Amanda; Reader, Michael; Rees, David C.; Rich, Sharna J.; Shah, Alpesh; Shibata, Yoshihiro; Smyth, Tomoko; Twigg, David G.; Wallis, Nicola G.; Williams, Glyn; Wilsher, Nicola E.; Woodhead, Andrew; Shimamura, Tadashi; Johnson, Christopher N. 分享 收藏
Detecting the footprint of selection on the genome of Girgentana goat, a popular ancient breed Criscione, A.; Ben Jemaa, S.; Chessari, G.; Riggio, S.; Tumino, S.; Cammilleri, G.; Lastra, A.; Carta, F.; Sardina, M. T.; Portolano, B.; Bordonaro, S.; Cesarani, A.; Mastrangelo, S. 分享 收藏
Targeting the catalytic HAT domain of CBP/p300 for the treatment of hormone-dependent breast and prostate cancers Hearn, K.; Bevan, L.; Chessari, G.; Clark, M.; Cons, B.; Espana-agusti, J.; Ferro, K.; Hamlett, C.; Howard, A.; Lyons, J.; Martins, V.; Morgillo, C.; Palmer, N.; Rapti, M.; Shah, A.; Smyth, T.; Unbekandt, M.; Varshney, D.; Ahn, M. 分享 收藏
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
A novel small-molecule CBP/p300 HAT domain inhibitor demonstrates potent in vivo activity and a favorable safety profile in preclinical species Hearn, K.; Ahn, M.; Bevan, L.; Chessari, G.; Clark, M.; Cons, B.; Espana-agusti, J.; Ferro, K.; Howard, A.; Lyons, J.; Martins, V.; Morgillo, C.; Palmer, N.; Rapti, M.; Shah, A.; Smyth, T.; Unbekandt, M.; Varshney, D.; Hamlett, C. 分享 收藏
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; Schopf, Patrick; St-Denis, Jeffrey D.; Valenzano, Chiara; Wallis, Nicola G.; Walser, Reto; Weir, Heather; Wilsher, Nicola E.; Woodhead, Andrew; Bento, Carla F.; Tisi, Dominic 分享 收藏
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
Identification of biomarkers of response to MDM2 inhibition in solid tumours using computational, multi-omics approaches Saini, Harpreet Kaur; Ahn, Maria; Ward, George; Kucia-Tran, Justyna; Gewinner, Christina; Ferrari, Nicola; Brothwood, Jessica; Bevan, Luke; Davis, Matthew; Fazal, Lynsey; Sims, Martin; O'Reilly, Marc; Chessari, Gianni; Ferraldeschi, Roberta; Lyons, John; Wallis, Nicola; Thompson, Neil 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
Fragment-Based Discovery of Allosteric Inhibitors of SH2 Domain-Containing Protein Tyrosine Phosphatase-2 (SHP2) Day, James E. H.; Berdini, Valerio; Castro, Joan; Chessari, Gianni; Davies, Thomas G.; Day, Philip J.; St. Denis, Jeffrey D.; Fujiwara, Hideto; Fukaya, Satoshi; Hamlett, Christopher C. F.; Hearn, Keisha; Hiscock, Steven D.; Holvey, Rhian S.; Ito, Satoru; Kandola, Navrohit; Kodama, Yasuo; Liebeschuetz, John W.; Martins, Vanessa; Matsuo, Kenichi; Mortenson, Paul N.; Muench, Sandra; Nakatsuru, Yoko; Ochiiwa, Hiroaki; Palmer, Nicholas; Peakman, Torren; Price, Amanda; Reader, Michael; Rees, David C.; Rich, Sharna J.; Shah, Alpesh; Shibata, Yoshihiro; Smyth, Tomoko; Twigg, David G.; Wallis, Nicola G.; Williams, Glyn; Wilsher, Nicola E.; Woodhead, Andrew; Shimamura, Tadashi; Johnson, Christopher N. 分享 收藏
分享 收藏
Enabling synthesis in fragment-based drug discovery (FBDD): microscale high-throughput optimisation of the medicinal chemist's toolbox reactions Townley, Chloe; Branduardi, Davide; Chessari, Gianni; Cons, Benjamin D.; Griffiths-Jones, Charlotte; Hall, Richard J.; Johnson, Christopher N.; Ochi, Yuji; Whibley, Stuart; Grainger, Rachel 分享 收藏
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. 分享 收藏
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
分享 收藏
Fragment-based drug discovery to identify small molecule allosteric inhibitors of SHP2 Day, Philip J.; Berdini, Valerio; Castro, Juan; Chessari, Gianni; Davies, Thomas G.; Day, James E.; Fukaya, Satoshi; Hamlett, Chris; Hearn, Keisha; Hiscock, Steve; Holvey, Rhian; Ito, Satoru; Kodama, Yasuo; Matsuo, Kenichi; Nakatsuru, Yoko; Palmer, Nick; Price, Amanda; Shimamura, Tadashi; St Denis, Jeffrey D.; Wallis, Nicola G.; Williams, Glyn; Johnson, Christopher N. 分享 收藏
A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1H,2H,3H-pyrrolo[3,2-b]pyridin-1-yl)-2-[(2R,5R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660) Johnson, Christopher N.; Ahn, Jong Sook; Buck, Ildiko M.; Chiarparin, Elisabetta; Day, James E. H.; Hopkins, Anna; Howard, Steven; Lewis, Edward J.; Martins, Vanessa; Millemaggi, Alessia; Munck, Joanne M.; Page, Lee W.; Peakman, Torren; Reader, Michael; Rich, Sharna J.; Saxty, Gordon; Smyth, Tomoko; Thompson, Neil T.; Ward, George A.; Williams, Pamela A.; Wilsher, Nicola E.; Chessari, Gianni 分享 收藏
Development of a potent class of small molecule inhibitors of the MDM2-p53 protein-protein interaction Fazal, Lynsey; Ahn, Maria; Bevan, Luke; Buck, Ildiko; Castro, Juan; Chessari, Gianni; Cons, Ben; Hearn, Keisha; Howard, Steven; Johnson, Chris; Reeks, Judith; Tamanini, Emiliano; Thompson, Neil; Walton, Hugh; Williams, Pamela; Bawn, Ruth H.; Blackburn, Tim J.; Cano, Celine; Cully, Sarah J.; Golding, Bernard; Griffin, Roger; Haggerty, Karen; Hardcastle, Ian; Newell, Herbie; Noble, Martin; Thomas, Huw; Willmore, Elaine; Zhao, Yan; Wedge, Steve 分享 收藏
未登录.png){kind=icon}
.png){kind=icon}
.png){kind=icon}
.png){kind=icon}
.png){kind=icon}
.png){kind=icon}
