Temporal activation of p53 by a specific MDM2 inhibitor is selectively toxic to tumors and leads to complete tumor growth inhibition S Shangary, D Qin, D McEachern, M Liu, RS Miller, S Qiu, ... Proceedings of the National Academy of Sciences 105 (10), 3933-3938, 2008 | 813 | 2008 |
Small-molecule inhibitors of the MDM2–p53 protein–protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment: miniperspective Y Zhao, A Aguilar, D Bernard, S Wang Journal of medicinal chemistry 58 (3), 1038-1052, 2015 | 527 | 2015 |
SAR405838: an optimized inhibitor of MDM2–p53 interaction that induces complete and durable tumor regression S Wang, W Sun, Y Zhao, D McEachern, I Meaux, C Barrière, JA Stuckey, ... Cancer research 74 (20), 5855-5865, 2014 | 337 | 2014 |
A potent small-molecule inhibitor of the MDM2–p53 interaction (MI-888) achieved complete and durable tumor regression in mice Y Zhao, S Yu, W Sun, L Liu, J Lu, D McEachern, S Shargary, D Bernard, ... Journal of medicinal chemistry 56 (13), 5553-5561, 2013 | 280 | 2013 |
Targeting the MDM2–p53 protein–protein interaction for new cancer therapy: progress and challenges S Wang, Y Zhao, A Aguilar, D Bernard, CY Yang Cold Spring Harbor perspectives in medicine 7 (5), a026245, 2017 | 253 | 2017 |
Diastereomeric spirooxindoles as highly potent and efficacious MDM2 inhibitors Y Zhao, L Liu, W Sun, J Lu, D McEachern, X Li, S Yu, D Bernard, ... Journal of the American Chemical Society 135 (19), 7223-7234, 2013 | 239 | 2013 |
High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein–protein interaction H Karatas, EC Townsend, F Cao, Y Chen, D Bernard, L Liu, M Lei, Y Dou, ... Journal of the American Chemical Society 135 (2), 669-682, 2013 | 182 | 2013 |
Activating STAT6 mutations in follicular lymphoma M Yildiz, H Li, D Bernard, NA Amin, P Ouillette, S Jones, K Saiya-Cork, ... Blood, The Journal of the American Society of Hematology 125 (4), 668-679, 2015 | 178 | 2015 |
Discovery of 4-((3′R,4′S,5′R)-6″-Chloro-4′-(3-chloro-2-fluorophenyl)-1′-ethyl-2″-oxodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indoline]-5 … A Aguilar, J Lu, L Liu, D Du, D Bernard, D McEachern, S Przybranowski, ... Journal of medicinal chemistry 60 (7), 2819-2839, 2017 | 175 | 2017 |
Reactivation of p53 by a specific MDM2 antagonist (MI-43) leads to p21-mediated cell cycle arrest and selective cell death in colon cancer S Shangary, K Ding, S Qiu, Z Nikolovska-Coleska, JA Bauer, M Liu, ... Molecular cancer therapeutics 7 (6), 1533-1542, 2008 | 127 | 2008 |
Small molecule inhibitors of MDM2-p53 and MDMX-p53 interactions as new cancer therapeutics Y Zhao, D Bernard, S Wang BioDiscovery 8, e8950, 2013 | 107 | 2013 |
Structure-based design of conformationally constrained, cell-permeable STAT3 inhibitors J Chen, L Bai, D Bernard, Z Nikolovska-Coleska, C Gomez, J Zhang, H Yi, ... ACS medicinal chemistry letters 1 (2), 85-89, 2010 | 103 | 2010 |
Structure-based design of high-affinity macrocyclic peptidomimetics to block the menin-mixed lineage leukemia 1 (MLL1) protein–protein interaction H Zhou, L Liu, J Huang, D Bernard, H Karatas, A Navarro, M Lei, S Wang Journal of Medicinal Chemistry 56 (3), 1113-1123, 2013 | 100 | 2013 |
Cold Spring Harbor Perspect F Wang, Y Zhao, A Aguilar, D Bernard, CY Yang Biol 1, a002980, 2009 | 99 | 2009 |
Discovery of a highly potent, cell-permeable macrocyclic peptidomimetic (MM-589) targeting the WD repeat domain 5 protein (WDR5)–mixed lineage leukemia (MLL) protein–protein … H Karatas, Y Li, L Liu, J Ji, S Lee, Y Chen, J Yang, L Huang, D Bernard, ... Journal of medicinal chemistry 60 (12), 4818-4839, 2017 | 89 | 2017 |
Analysis of the binding of mixed lineage leukemia 1 (MLL1) and histone 3 peptides to WD repeat domain 5 (WDR5) for the design of inhibitors of the MLL1− WDR5 interaction H Karatas, EC Townsend, D Bernard, Y Dou, S Wang Journal of medicinal chemistry 53 (14), 5179-5185, 2010 | 85 | 2010 |
A potent small-molecule inhibitor of the DCN1-UBC12 interaction that selectively blocks cullin 3 neddylation H Zhou, J Lu, L Liu, D Bernard, CY Yang, E Fernandez-Salas, ... Nature communications 8 (1), 1150, 2017 | 83 | 2017 |
Targeting the MDM2-p53 protein-protein interaction for new cancer therapeutics S Wang, Y Zhao, D Bernard, A Aguilar, S Kumar Protein-protein interactions, 57-79, 2012 | 83 | 2012 |
2D conformationally sampled pharmacophore: a ligand-based pharmacophore to differentiate δ opioid agonists from antagonists D Bernard, A Coop, AD MacKerell Journal of the American Chemical Society 125 (10), 3101-3107, 2003 | 78 | 2003 |
Design of chemically stable, potent, and efficacious MDM2 inhibitors that exploit the retro-mannich ring-opening-cyclization reaction mechanism in spiro-oxindoles A Aguilar, W Sun, L Liu, J Lu, D McEachern, D Bernard, JR Deschamps, ... Journal of medicinal chemistry 57 (24), 10486-10498, 2014 | 73 | 2014 |