Novel promising IAP antagonist on the horizon for clinical translation

Journal of Medicinal Chemistry

Volumn 55, Issue 9, 2012, Pages 4099-4100

  Fulda, Simone ^a  

^a GOETHE UNIVERSITY   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

AMINO ACID; ANTINEOPLASTIC AGENT; CASPASE 9; GDC 0152; INHIBITOR OF APOPTOSIS PROTEIN; SECOND MITOCHONDRIAL ACTIVATOR OF CASPASE; UNCLASSIFIED DRUG; X LINKED INHIBITOR OF APOPTOSIS;

AMINO TERMINAL SEQUENCE; ANTINEOPLASTIC ACTIVITY; BREAST CARCINOMA; CANCER CELL; CANCER INHIBITION; CANCER THERAPY; CONFORMATIONAL TRANSITION; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG RESPONSE; DRUG SYNTHESIS; ENZYME ACTIVITY; HUMAN; NONHUMAN; NOTE; PLASMA PROTEIN BINDING; PROTEIN DEGRADATION; PROTEIN INTERACTION; TRANSLATIONAL RESEARCH;

ANIMALS; ANTINEOPLASTIC AGENTS; APOPTOSIS; CELL LINE, TUMOR; HUMANS; INHIBITOR OF APOPTOSIS PROTEINS; MICE; THIADIAZOLES;

EID: 84861087454     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm300475b     Document Type: Note

References (6)

1. Hanahan, D.; Weinberg, R. A. Hallmarks of cancer: the next generation Cell 2011, 144, 646-674
2. Fulda, S.; Vucic, D. Targeting IAP proteins for therapeutic intervention in cancer Nat. Rev. Drug Discovery 2012, 11, 109-124
3. Flygare, J. A.; Beresini, M.; Budha, N.; Chan, H.; Chan, I. T.; Cheeti, S.; Cohen, F.; Deshayes, K.; Doerner, K.; Eckhardt, S. G.; Elliott, L. O.; Feng, B.; Franklin, M. C.; Reisner, S. F.; Gazzard, L.; Halladay, J.; Hymowitz, S. G.; La, H.; LoRusso, P.; Maurer, B.; Murray, L.; Plise, E.; Quan, C.; Stephan, J.-P.; Young, S. G.; Tom, J.; Tsui, V.; Um, J.; Varfolomeev, E.; Vucic, D.; Wagner, A. J.; Wallweber, H. J. A.; Wang, L.; Ware, J.; Wen, Z.; Wong, H.; Wong, J. M.; Wong, M.; Wong, S.; Yu, R.; Zobel, K.; Fairbrother, W. J. Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152). J. Med. Chem. 2012, DOI: 10.1021/jm300060k.
4. Dueber, E. C.; Schoeffler, A. J.; Lingel, A.; Elliott, J. M.; Fedorova, A. V.; Giannetti, A. M.; Zobel, K.; Maurer, B.; Varfolomeev, E.; Wu, P.; Wallweber, H. J.; Hymowitz, S. G.; Deshayes, K.; Vucic, D.; Fairbrother, W. J. Antagonists induce a conformational change in cIAP1 that promotes autoubiquitination Science 2011, 334, 376-380
5. Varfolomeev, E.; Blankenship, J. W.; Wayson, S. M.; Fedorova, A. V.; Kayagaki, N.; Garg, P.; Zobel, K.; Dynek, J. N.; Elliott, L. O.; Wallweber, H. J.; Flygare, J. A.; Fairbrother, W. J.; Deshayes, K.; Dixit, V. M.; Vucic, D. IAP antagonists induce autoubiquitination of c-IAPs, NF-kappaB activation, and TNFalpha-dependent apoptosis Cell 2007, 131, 669-681 (Pubitemid 350087204)
6. Petersen, S. L.; Wang, L.; Yalcin-Chin, A.; Li, L.; Peyton, M.; Minna, J.; Harran, P.; Wang, X. Autocrine TNFalpha signaling renders human cancer cells susceptible to Smac-mimetic-induced apoptosis Cancer Cell 2007, 12, 445-456 (Pubitemid 350064365)