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John A Flygare
John A Flygare
Verified email at merck.com
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Year
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
14212007
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
7792015
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
6951997
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
4222013
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
3072014
Antibody‐drug conjugates for the treatment of cancer
JA Flygare, TH Pillow, P Aristoff
Chemical biology & drug design 81 (1), 113-121, 2013
2662013
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
2662012
Pyrrolobenzodiazepines and conjugates thereof
PW Howard, L Masterson, A Tiberghien, JA Flygare, JL Gunzner, ...
US Patent App. 13/087,575, 2011
2412011
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
2412006
Solid-phase synthesis of 2-aminothiazoles
PC Kearney, M Fernandez, JA Flygare
The Journal of Organic Chemistry 63 (1), 196-200, 1998
2001998
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
1592015
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
1581992
Small-molecule pan-IAP antagonists: a patent review
JA Flygare, WJ Fairbrother
Expert opinion on therapeutic patents 20 (2), 251-267, 2010
1432010
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
1432009
Pyrimidine derivatives
TD Cushing, HL Mellon, JC Jaen, JA Flygare, SC Miao, X Chen, ...
US Patent 6,528,513, 2003
1432003
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
1382016
Pyrimidine derivatives
TD Cushing, HL Mellon, JC Jaen, JA Flygare, SC Miao, X Chen, ...
US Patent 6,200,977, 2001
1382001
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
1342003
Decoupling stability and release in disulfide bonds with antibody-small molecule conjugates
GD Rosario
Chemical Science 8 (1), 366-370, 2017
1282017
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
1282015
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