ANIMAL EXPERIMENT;
ANIMAL MODEL;
ANTINEOPLASTIC ACTIVITY;
AREA UNDER THE CURVE;
ARTICLE;
CANCER CELL CULTURE;
CELL GROWTH;
CONTROLLED STUDY;
DRUG CLEARANCE;
DRUG DESIGN;
DRUG DISTRIBUTION;
DRUG ELIMINATION;
DRUG HALF LIFE;
DRUG STRUCTURE;
DRUG SYNTHESIS;
MOUSE;
NONHUMAN;
RAT;
TUMOR REGRESSION;
ANIMALS;
ANTINEOPLASTIC AGENTS;
AREA UNDER CURVE;
AZOCINES;
BLOTTING, WESTERN;
CARRIER PROTEINS;
CASPASE 3;
CASPASE 9;
CELL DEATH;
CELL LINE, TUMOR;
CELL PROLIFERATION;
DOSE-RESPONSE RELATIONSHIP, DRUG;
HUMANS;
INDICATORS AND REAGENTS;
INHIBITOR OF APOPTOSIS PROTEINS;
MALE;
MICE;
MICE, NUDE;
MITOCHONDRIAL PROTEINS;
PHENYLENEDIAMINES;
RATS;
RATS, SPRAGUE-DAWLEY;
X-LINKED INHIBITOR OF APOPTOSIS PROTEIN;
XENOGRAFT MODEL ANTITUMOR ASSAYS;
LaCasse, E. C.; Mahoney, D. J.; Cheung, H. H.; Plenchette, S.; Baird, S.; Korneluk, R. G. IAP-targeted therapies for cancer Oncogene 2008, 27, 6252-6275
Smac, a mitochondrial protein that promotes cytochrome c-dependent caspase activation by eliminating IAP inhibition
Du, C.; Fang, M.; Li, Y.; Li, L.; Wang, X. Smac, a mitochondrial protein that promotes cytochrome c-dependent caspase activation by eliminating IAP inhibition Cell 2000, 102, 33-42
Identification of DIABLO, a mammalian protein that promotes apoptosis by binding to and antagonizing IAP proteins
Verhagen, A. M.; Ekert, P. G.; Pakusch, M.; Silke, J.; Connolly, L. M.; Reid, G. E.; Moritz, R. L.; Simpson, R. J.; Vaux, D. L. Identification of DIABLO, a mammalian protein that promotes apoptosis by binding to and antagonizing IAP proteins Cell 2000, 102, 43-53
Structural basis for binding of Smac/DIABLO to the XIAP BIR3 domain
Liu, Z.; Sun, C.; Olejniczak, E. T.; Meadows, R.; Betz, S. F.; Oost, T.; Herrmann, J.; Wu, J. C.; Fesik, S. W. Structural basis for binding of Smac/DIABLO to the XIAP BIR3 domain Nature 2000, 408, 1004-1008
Targeting Inhibitors of Apoptosis Proteins (IAPs) for New Breast Cancer Therapeutics
Wang, S.; Bai, L.; Lu, J.; Liu, L.; Yang, C. Y.; Sun, H. Targeting Inhibitors of Apoptosis Proteins (IAPs) For New Breast Cancer Therapeutics J. Mammary Gland Biol. Neoplasia 2012, 17, 217-228
Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis protein/caspase-9 interaction site
Sun, H.; Nikolovska-Coleska, Z.; Yang, C. Y.; Xu, L.; Tomita, Y.; Krajewski, K.; Roller, P. P.; Wang, S. Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis protein/caspase-9 interaction site J. Med. Chem. 2004, 47, 4147-4150
A small molecule Smac mimic potentiates TRAIL- and TNF alpha-mediated cell death
Li, L.; Thomas, R. M.; Suzuki, H.; De Brabander, J. K.; Wang, X.; Harran, P. G. A small molecule Smac mimic potentiates TRAIL- and TNF alpha-mediated cell death Science 2004, 305, 1471-1474
Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer
Oost, T. K.; Sun, C.; Armstrong, R. C.; Al-Assaad, A. S.; Betz, S. F.; Deckwerth, T. L.; Ding, H.; Elmore, S. W.; Meadows, R. P.; Olejniczak, E. T.; Oleksijew, A.; Oltersdorf, T.; Rosenberg, S. H.; Shoemaker, A. R.; Tomaselli, K. J.; Zou, H.; Fesik, S. W. Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer J. Med. Chem. 2004, 47, 4417-4426
Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic
Sun, H.; Nikolovska-Coleska, Z.; Lu, J.; Qiu, S.; Yang, C.-Y.; Gao, W.; Meagher, J.; Stuckey, J.; Wang, S. Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic J. Med. Chem. 2006, 49, 7916-7920
Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP)
Sun, H.; Stuckey, J. A.; Nikolovska-Coleska, Z.; Qin, D.; Meagher, J. L.; Qiu, S.; Lu, J.; Yang, C. Y.; Saito, N. G; Wang, S. Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP) J. Med. Chem. 2008, 51, 7169-7180
Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs
Zobel, K.; Wang, L.; Varfolomeev, E.; Franklin, M. C.; Elliott, L. O.; Wallweber, H. J.; Okawa, D. C.; Flygare, J. A.; Vucic, D.; Fairbrother, W. J.; Deshayes, K. Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs ACS Chem. Biol. 2006, 1, 525-533
IAP antagonists induce autoubiquitination of c-IAPs, NF-kappaB activation, and TNFalpha-dependent apoptosis
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
IAP antagonists target cIAP1 to induce TNFalpha-dependent apoptosis
Vince, J. E.; Wong, W. W.; Khan, N.; Feltham, R.; Chau, D.; Ahmed, A. U.; Benetatos, C. A.; Chunduru, S. K.; Condon, S. M.; McKinlay, M.; Brink, R.; Leverkus, M.; Tergaonkar, V.; Schneider, P.; Callus, B. A.; Koentgen, F.; Vaux, D. L.; Silke, J. IAP antagonists target cIAP1 to induce TNFalpha-dependent apoptosis Cell 2007, 131, 682-693
Design, synthesis, and characterization of a potent, nonpeptide, cell-permeable, bivalent Smac mimetic that concurrently targets both the BIR2 and BIR3 domains in XIAP
Sun, H.; Nikolovska-Coleska, Z.; Lu, J.; Meagher, J. L.; Yang, C.- Y.; Qiu, S.; Tomita, Y.; Ueda, Y.; Jiang, S.; Krajewski, K.; Roller, P. P.; Stuckey, J. A.; Wang, S. Design, synthesis, and characterization of a potent, nonpeptide, cell-permeable, bivalent Smac mimetic that concurrently targets both the BIR2 and BIR3 domains in XIAP J. Am. Chem. Soc. 2007, 129, 15279-15294
SM-164: A novel, bivalent Smac mimetic that induces apoptosis and tumor regression by concurrent removal of the blockade of cIAP-1/2 and XIAP
Lu, J.; Bai, L.; Sun, H.; Nikolovska-Coleska, Z.; McEachern, D.; Qiu, S.; Miller, R. S.; Yi, H.; Shangary, S.; Sun, Y.; Meagher, J. L.; Stuckey, J. A.; Wang, S. SM-164: A novel, bivalent Smac mimetic that induces apoptosis and tumor regression by concurrent removal of the blockade of cIAP-1/2 and XIAP Cancer Res. 2008, 68, 9384-9393
Interaction of a cyclic, bivalent Smac mimetic with the X-linked inhibitor of apoptosis protein
Nikolovska-Coleska, Z.; Meagher, J. L.; Jiang, S.; Yang, C.-Y.; Qiu, S.; Roller, P. P.; Stuckey, J. A.; Wang, S. Interaction of a cyclic, bivalent Smac mimetic with the X-linked inhibitor of apoptosis protein Biochemistry 2008, 47, 9811-9824
Cleavage of human inhibitor of apoptosis protein XIAP results in fragments with distinct specificities for caspases
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