IAP antagonists induce autoubiquitination of c-IAPs, NF-κB activation, and TNFα-dependent apoptosis E Varfolomeev, JW Blankenship, SM Wayson, AV Fedorova, N Kayagaki, ... Cell 131 (4), 669-681, 2007 | 1429 | 2007 |
Novel antibody–antibiotic conjugate eliminates intracellular S. aureus SM Lehar, T Pillow, M Xu, L Staben, KK Kajihara, R Vandlen, L DePalatis, ... Nature 527 (7578), 323-328, 2015 | 799 | 2015 |
P-TEFb kinase is required for HIV Tat transcriptional activation in vivo and in vitro HSY Mancebo, G Lee, J Flygare, J Tomassini, P Luu, Y Zhu, J Peng, ... Genes & development 11 (20), 2633-2644, 1997 | 696 | 1997 |
Structure-guided design of a selective BCL-XL inhibitor G Lessene, PE Czabotar, BE Sleebs, K Zobel, KN Lowes, JM Adams, ... Nature chemical biology 9 (6), 390-397, 2013 | 431 | 2013 |
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity ZF Tao, L Hasvold, L Wang, X Wang, AM Petros, CH Park, ER Boghaert, ... ACS medicinal chemistry letters 5 (10), 1088-1093, 2014 | 311 | 2014 |
Antibody‐drug conjugates for the treatment of cancer JA Flygare, TH Pillow, P Aristoff Chemical biology & drug design 81 (1), 113-121, 2013 | 273 | 2013 |
Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152) JA Flygare, M Beresini, N Budha, H Chan, IT Chan, S Cheeti, F Cohen, ... Journal of medicinal chemistry 55 (9), 4101-4113, 2012 | 271 | 2012 |
Pyrrolobenzodiazepines and conjugates thereof PW Howard, L Masterson, A Tiberghien, JA Flygare, JL Gunzner, ... US Patent App. 13/087,575, 2011 | 246 | 2011 |
Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs K Zobel, L Wang, E Varfolomeev, MC Franklin, LO Elliott, HJA Wallweber, ... ACS chemical biology 1 (8), 525-533, 2006 | 241 | 2006 |
Solid-phase synthesis of 2-aminothiazoles PC Kearney, M Fernandez, JA Flygare The Journal of Organic Chemistry 63 (1), 196-200, 1998 | 199 | 1998 |
Targeting LGR5+ cells with an antibody-drug conjugate for the treatment of colon cancer MR Junttila, W Mao, X Wang, BE Wang, T Pham, J Flygare, SF Yu, S Yee, ... Science translational medicine 7 (314), 314ra186-314ra186, 2015 | 165 | 2015 |
A novel ruthenium-catalyzed tandem cyclization-reconstitutive addition of propargyl alcohols with allyl alcohols BM Trost, JA Flygare Journal of the American Chemical Society 114 (13), 5476-5477, 1992 | 160 | 1992 |
Targeted drug delivery through the traceless release of tertiary and heteroaryl amines from antibody–drug conjugates LR Staben, SG Koenig, SM Lehar, R Vandlen, D Zhang, J Chuh, SF Yu, ... Nature chemistry 8 (12), 1112-1119, 2016 | 148 | 2016 |
Antagonism of c-IAP and XIAP proteins is required for efficient induction of cell death by small-molecule IAP antagonists C Ndubaku, E Varfolomeev, L Wang, K Zobel, K Lau, LO Elliott, B Maurer, ... ACS chemical biology 4 (7), 557-566, 2009 | 143 | 2009 |
Pyrimidine derivatives TD Cushing, HL Mellon, JC Jaen, JA Flygare, SC Miao, X Chen, ... US Patent 6,528,513, 2003 | 143 | 2003 |
Small-molecule pan-IAP antagonists: a patent review JA Flygare, WJ Fairbrother Expert opinion on therapeutic patents 20 (2), 251-267, 2010 | 142 | 2010 |
Pyrimidine derivatives TD Cushing, HL Mellon, JC Jaen, JA Flygare, SC Miao, X Chen, ... US Patent 6,200,977, 2001 | 138 | 2001 |
A novel anti-CD22 anthracycline-based antibody–drug conjugate (ADC) that overcomes resistance to auristatin-based ADCs SF Yu, B Zheng, MA Go, J Lau, S Spencer, H Raab, R Soriano, ... Clinical Cancer Research 21 (14), 3298-3306, 2015 | 134 | 2015 |
Structure and function analysis of peptide antagonists of melanoma inhibitor of apoptosis (ML-IAP) MC Franklin, S Kadkhodayan, H Ackerly, D Alexandru, MD Distefano, ... Biochemistry 42 (27), 8223-8231, 2003 | 134 | 2003 |
Decoupling stability and release in disulfide bonds with antibody-small molecule conjugates GD Rosario Chemical Science 8 (1), 366-370, 2017 | 129 | 2017 |