PDBsum entry 1i4o

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Apoptosis/hydrolase PDB id
Protein chains
235 a.a. *
17 a.a. *
Waters ×199
* Residue conservation analysis
PDB id:
Name: Apoptosis/hydrolase
Title: Crystal structure of the xiap/caspase-7 complex
Structure: Caspase-7. Chain: a, b. Synonym: apoptotic protease mch-3. Engineered: yes. Baculoviral iap repeat-containing protein 4. Chain: c, d. Fragment: residues 120-260. Synonym: x-linked iap. Engineered: yes
Source: Homo sapiens. Human. Organism_taxid: 9606. Expressed in: escherichia coli. Expression_system_taxid: 562. Expression_system_taxid: 562
Biol. unit: Dimer (from PQS)
2.40Å     R-factor:   0.224     R-free:   0.260
Authors: Y.Huang,Y.C.Park,R.L.Rich,D.Segal,D.G.Myszka,H.Wu
Key ref: Y.Huang et al. (2001). Structural basis of caspase inhibition by XIAP: differential roles of the linker versus the BIR domain. Cell, 104, 781-790. PubMed id: 11257231
22-Feb-01     Release date:   21-Mar-01    
Go to PROCHECK summary

Protein chains
Pfam   ArchSchema ?
P55210  (CASP7_HUMAN) -  Caspase-7
303 a.a.
235 a.a.
Protein chains
Pfam   ArchSchema ?
P98170  (XIAP_HUMAN) -  E3 ubiquitin-protein ligase XIAP
497 a.a.
17 a.a.
Key:    PfamA domain  PfamB domain  Secondary structure  CATH domain

 Enzyme reactions 
   Enzyme class: Chains A, B: E.C.  - Caspase-7.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
 Gene Ontology (GO) functional annotation 
  GO annot!
  Cellular component     cytoplasm   5 terms 
  Biological process     intrinsic apoptotic signaling pathway   12 terms 
  Biochemical function     cysteine-type endopeptidase activity involved in apoptotic process     7 terms  


Cell 104:781-790 (2001)
PubMed id: 11257231  
Structural basis of caspase inhibition by XIAP: differential roles of the linker versus the BIR domain.
Y.Huang, Y.C.Park, R.L.Rich, D.Segal, D.G.Myszka, H.Wu.
The inhibitor of apoptosis proteins (IAPs) represent the only endogenous caspase inhibitors and are characterized by the presence of baculoviral IAP repeats (BIRs). Here, we report the crystal structure of the complex between human caspase-7 and XIAP (BIR2 and the proceeding linker). The structure surprisingly reveals that the linker is the only contacting element for the caspase, while the BIR2 domain is invisible in the crystal. The linker interacts with and blocks the substrate groove of the caspase in a backward fashion, distinct from substrate recognition. Structural analyses suggest that the linker is the energetic and specificity determinant of the interaction. Further biochemical characterizations clearly establish that the linker harbors the major energetic determinant, while the BIR2 domain serves as a regulatory element for caspase binding and Smac neutralization.

Literature references that cite this PDB file's key reference

  PubMed id Reference
22293567 S.Fulda, and D.Vucic (2012).
Targeting IAP proteins for therapeutic intervention in cancer.
  Nat Rev Drug Discov, 11, 109-124.  
21173700 E.A.Worthey, A.N.Mayer, G.D.Syverson, D.Helbling, B.B.Bonacci, B.Decker, J.M.Serpe, T.Dasu, M.R.Tschannen, R.L.Veith, M.J.Basehore, U.Broeckel, A.Tomita-Mitchell, M.J.Arca, J.T.Casper, D.A.Margolis, D.P.Bick, M.J.Hessner, J.M.Routes, J.W.Verbsky, H.J.Jacob, and D.P.Dimmock (2011).
Making a definitive diagnosis: successful clinical application of whole exome sequencing in a child with intractable inflammatory bowel disease.
  Genet Med, 13, 255-262.  
20660790 A.H.Filipovich, K.Zhang, A.L.Snow, and R.A.Marsh (2010).
X-linked lymphoproliferative syndromes: brothers or distant cousins?
  Blood, 116, 3398-3408.  
20704571 D.C.Altieri (2010).
Survivin and IAP proteins in cell-death mechanisms.
  Biochem J, 430, 199-205.  
20198502 F.Van Herreweghe, N.Festjens, W.Declercq, and P.Vandenabeele (2010).
Tumor necrosis factor-mediated cell death: to break or to burst, that's the question.
  Cell Mol Life Sci, 67, 1567-1579.  
20397191 K.S.Chung, J.H.Choi, N.I.Back, M.S.Choi, E.K.Kang, H.G.Chung, T.S.Jeong, and K.T.Lee (2010).
Eupafolin, a flavonoid isolated from Artemisia princeps, induced apoptosis in human cervical adenocarcinoma HeLa cells.
  Mol Nutr Food Res, 54, 1318-1328.  
20651737 M.Gyrd-Hansen, and P.Meier (2010).
IAPs: from caspase inhibitors to modulators of NF-kappaB, inflammation and cancer.
  Nat Rev Cancer, 10, 561-574.  
19373243 P.D.Mace, S.Shirley, and C.L.Day (2010).
Assembling the building blocks: structure and function of inhibitor of apoptosis proteins.
  Cell Death Differ, 17, 46-53.  
20148665 R.S.Whelan, V.Kaplinskiy, and R.N.Kitsis (2010).
Cell death in the pathogenesis of heart disease: mechanisms and significance.
  Annu Rev Physiol, 72, 19-44.  
19968284 J.T.Heeres, S.H.Kim, B.J.Leslie, E.A.Lidstone, B.T.Cunningham, and P.J.Hergenrother (2009).
Identifying modulators of protein-protein interactions using photonic crystal biosensors.
  J Am Chem Soc, 131, 18202-18203.  
19217783 M.Broemer, and P.Meier (2009).
Ubiquitin-mediated regulation of apoptosis.
  Trends Cell Biol, 19, 130-140.  
19877056 M.Ferretti, M.Gattorno, A.Chiocchetti, R.Mesturini, E.Orilieri, T.Bensi, M.P.Sormani, G.Cappellano, E.Cerutti, S.Nicola, A.Biava, C.Bardelli, S.Federici, I.Ceccherini, M.Baldi, C.Santoro, I.Dianzani, A.Martini, and U.Dianzani (2009).
The 423Q polymorphism of the X-linked inhibitor of apoptosis gene influences monocyte function and is associated with periodic fever.
  Arthritis Rheum, 60, 3476-3484.  
19495985 M.Orme, and P.Meier (2009).
Inhibitor of apoptosis proteins in Drosophila: gatekeepers of death.
  Apoptosis, 14, 950-960.  
19039324 S.Fulda (2009).
Inhibitor of apoptosis proteins in hematological malignancies.
  Leukemia, 23, 467-476.  
19298593 S.Fulda (2009).
Therapeutic opportunities for counteracting apoptosis resistance in childhood leukaemia.
  Br J Haematol, 145, 441-454.  
18954041 H.Sun, J.A.Stuckey, Z.Nikolovska-Coleska, D.Qin, J.L.Meagher, S.Qiu, J.Lu, C.Y.Yang, N.G.Saito, and S.Wang (2008).
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, 51, 7169-7180.
PDB code: 2jk7
18937395 H.Sun, Z.Nikolovska-Coleska, C.Y.Yang, D.Qian, J.Lu, S.Qiu, L.Bai, Y.Peng, Q.Cai, and S.Wang (2008).
Design of small-molecule peptidic and nonpeptidic Smac mimetics.
  Acc Chem Res, 41, 1264-1277.  
17967870 J.C.Wilkinson, A.S.Wilkinson, S.Galbán, R.A.Csomos, and C.S.Duckett (2008).
Apoptosis-inducing factor is a target for ubiquitination through interaction with XIAP.
  Mol Cell Biol, 28, 237-247.  
18406323 J.G.Albeck, J.M.Burke, B.B.Aldridge, M.Zhang, D.A.Lauffenburger, and P.K.Sorger (2008).
Quantitative analysis of pathways controlling extrinsic apoptosis in single cells.
  Mol Cell, 30, 11-25.  
18548102 L.Schyschka, A.Rudy, I.Jeremias, N.Barth, G.R.Pettit, and A.M.Vollmar (2008).
Spongistatin 1: a new chemosensitizing marine compound that degrades XIAP.
  Leukemia, 22, 1737-1745.  
18854135 M.X.O'Riordan, L.D.Bauler, F.L.Scott, and C.S.Duckett (2008).
Inhibitor of apoptosis proteins in eukaryotic evolution and development: a model of thematic conservation.
  Dev Cell, 15, 497-508.  
18359761 N.Khan, F.Afaq, D.N.Syed, and H.Mukhtar (2008).
Fisetin, a novel dietary flavonoid, causes apoptosis and cell cycle arrest in human prostate cancer LNCaP cells.
  Carcinogenesis, 29, 1049-1056.  
18338251 P.Maycotte, S.Blancas, and J.Morán (2008).
Role of inhibitor of apoptosis proteins and Smac/DIABLO in staurosporine-induced cerebellar granule neurons death.
  Neurochem Res, 33, 1534-1540.  
18620520 S.M.Langemeijer, Graaf, and J.H.Jansen (2008).
IAPs as therapeutic targets in haematological malignancies.
  Expert Opin Ther Targets, 12, 981-993.  
19016849 Y.Sasaki, M.Minamizawa, A.Ambo, S.Sugawara, Y.Ogawa, and K.Nitta (2008).
Cell-penetrating peptide-conjugated XIAP-inhibitory cyclic hexapeptides enter into Jurkat cells and inhibit cell proliferation.
  FEBS J, 275, 6011-6021.  
18717598 Z.Nikolovska-Coleska, J.L.Meagher, S.Jiang, C.Y.Yang, S.Qiu, P.P.Roller, J.A.Stuckey, and S.Wang (2008).
Interaction of a cyclic, bivalent smac mimetic with the x-linked inhibitor of apoptosis protein.
  Biochemistry, 47, 9811-9824.
PDB code: 2vsl
17094177 A.Kurakin, and D.E.Bredesen (2007).
An unconventional IAP-binding motif revealed by target-assisted iterative screening (TAIS) of the BIR3-cIAP1 domain.
  J Mol Recognit, 20, 39-50.  
17573556 A.M.Hunter, E.C.LaCasse, and R.G.Korneluk (2007).
The inhibitors of apoptosis (IAPs) as cancer targets.
  Apoptosis, 12, 1543-1568.  
17382285 A.R.Mufti, E.Burstein, and C.S.Duckett (2007).
XIAP: cell death regulation meets copper homeostasis.
  Arch Biochem Biophys, 463, 168-174.  
17294084 B.Nachmias, I.Lazar, M.Elmalech, I.Abed-El-Rahaman, Y.Asshab, O.Mandelboim, R.Perlman, and D.Ben-Yehuda (2007).
Subcellular localization determines the delicate balance between the anti- and pro-apoptotic activity of Livin.
  Apoptosis, 12, 1129-1142.  
18034418 B.Nachmias, S.Mizrahi, M.Elmalech, I.Lazar, Y.Ashhab, R.Gazit, G.Markel, D.Ben-Yehuda, and O.Mandelboim (2007).
Manipulation of NK cytotoxicity by the IAP family member Livin.
  Eur J Immunol, 37, 3467-3476.  
17999504 H.Sun, Z.Nikolovska-Coleska, J.Lu, J.L.Meagher, C.Y.Yang, S.Qiu, Y.Tomita, Y.Ueda, S.Jiang, K.Krajewski, P.P.Roller, J.A.Stuckey, and S.Wang (2007).
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, 129, 15279-15294.  
17450518 J.Y.Liou, N.Matijevic-Aleksic, S.Lee, and K.K.Wu (2007).
Prostacyclin inhibits endothelial cell XIAP ubiquitination and degradation.
  J Cell Physiol, 212, 840-848.  
17465723 K.Drosopoulos, and A.Pintzas (2007).
Multifaceted targeting in cancer: the recent cell death players meet the usual oncogene suspects.
  Expert Opin Ther Targets, 11, 641-659.  
17560374 M.Lu, S.C.Lin, Y.Huang, Y.J.Kang, R.Rich, Y.C.Lo, D.Myszka, J.Han, and H.Wu (2007).
XIAP induces NF-kappaB activation via the BIR1/TAB1 interaction and BIR1 dimerization.
  Mol Cell, 26, 689-702.
PDB codes: 2poi 2pom 2pop
18166655 P.S.Ribeiro, E.Kuranaga, T.Tenev, F.Leulier, M.Miura, and P.Meier (2007).
DIAP2 functions as a mechanism-based regulator of drICE that contributes to the caspase activity threshold in living cells.
  J Cell Biol, 179, 1467-1480.  
17698078 S.C.Lin, Y.Huang, Y.C.Lo, M.Lu, and H.Wu (2007).
Crystal structure of the BIR1 domain of XIAP in two crystal forms.
  J Mol Biol, 372, 847-854.
PDB code: 2qra
17896835 U.Fischer, K.Janssen, and K.Schulze-Osthoff (2007).
Cutting-edge apoptosis-based therapeutics: a panacea for cancer?
  BioDrugs, 21, 273-297.  
17724022 Z.Gao, Y.Tian, J.Wang, Q.Yin, H.Wu, Y.M.Li, and X.Jiang (2007).
A dimeric Smac/diablo peptide directly relieves caspase-3 inhibition by XIAP. Dynamic and cooperative regulation of XIAP by Smac/Diablo.
  J Biol Chem, 282, 30718-30727.  
16322751 A.D.Schimmer, S.Dalili, R.A.Batey, and S.J.Riedl (2006).
Targeting XIAP for the treatment of malignancy.
  Cell Death Differ, 13, 179-188.  
17040621 A.D.Schimmer (2006).
Induction of apoptosis in lymphoid and myeloid leukemia.
  Curr Oncol Rep, 8, 430-436.  
17016456 B.P.Eckelman, G.S.Salvesen, and F.L.Scott (2006).
Human inhibitor of apoptosis proteins: why XIAP is the black sheep of the family.
  EMBO Rep, 7, 988-994.  
16339151 B.P.Eckelman, and G.S.Salvesen (2006).
The human anti-apoptotic proteins cIAP1 and cIAP2 bind but do not inhibit caspases.
  J Biol Chem, 281, 3254-3260.  
16567363 F.Ortuso, T.Langer, and S.Alcaro (2006).
GBPM: GRID-based pharmacophore model: concept and application studies to protein-protein recognition.
  Bioinformatics, 22, 1449-1455.  
16608851 M.A.Salako, M.J.Carter, and G.E.Kass (2006).
Coxsackievirus protein 2BC blocks host cell apoptosis by inhibiting caspase-3.
  J Biol Chem, 281, 16296-16304.  
16353131 M.Grzmil, S.Kaulfuss, P.Thelen, B.Hemmerlein, S.Schweyer, S.Obenauer, T.W.Kang, and P.Burfeind (2006).
Expression and functional analysis of Bax inhibitor-1 in human breast cancer cells.
  J Pathol, 208, 340-349.  
19617919 S.K.Sharma, C.Straub, and L.Zawel (2006).
Development of Peptidomimetics Targeting IAPs.
  Int J Pept Res Ther, 12, 21-32.  
16847054 X.H.Peng, P.Karna, Z.Cao, B.H.Jiang, M.Zhou, and L.Yang (2006).
Cross-talk between epidermal growth factor receptor and hypoxia-inducible factor-1alpha signal pathways increases resistance to apoptosis by up-regulating survivin gene expression.
  J Biol Chem, 281, 25903-25914.  
16313474 B.Fadeel, and S.Orrenius (2005).
Apoptosis: a basic biological phenomenon with wide-ranging implications in human disease.
  J Intern Med, 258, 479-517.  
15650747 F.L.Scott, J.B.Denault, S.J.Riedl, H.Shin, M.Renatus, and G.S.Salvesen (2005).
XIAP inhibits caspase-3 and -7 using two binding sites: evolutionarily conserved mechanism of IAPs.
  EMBO J, 24, 645-655.  
16200200 I.N.Lavrik, A.Golks, and P.H.Krammer (2005).
Caspases: pharmacological manipulation of cell death.
  J Clin Invest, 115, 2665-2672.  
15800951 K.Barczyk, M.Kreuter, J.Pryjma, E.P.Booy, S.Maddika, S.Ghavami, W.E.Berdel, J.Roth, and M.Los (2005).
Serum cytochrome c indicates in vivo apoptosis and can serve as a prognostic marker during cancer therapy.
  Int J Cancer, 116, 167-173.  
16044155 K.M.Bockbrader, M.Tan, and Y.Sun (2005).
A small molecule Smac-mimic compound induces apoptosis and sensitizes TRAIL- and etoposide-induced apoptosis in breast cancer cells.
  Oncogene, 24, 7381-7388.  
16212486 N.Yan, and Y.Shi (2005).
Mechanisms of apoptosis through structural biology.
  Annu Rev Cell Dev Biol, 21, 35-56.  
16246265 N.Zhang, H.Hartig, I.Dzhagalov, D.Draper, and Y.W.He (2005).
The role of apoptosis in the development and function of T lymphocytes.
  Cell Res, 15, 749-769.  
15797833 P.Cashio, T.V.Lee, and A.Bergmann (2005).
Genetic control of programmed cell death in Drosophila melanogaster.
  Semin Cell Dev Biol, 16, 225-235.  
  15791949 P.Clarke, S.M.Richardson-Burns, R.L.DeBiasi, and K.L.Tyler (2005).
Mechanisms of apoptosis during reovirus infection.
  Curr Top Microbiol Immunol, 289, 1.  
15765138 R.S.Foo, K.Mani, and R.N.Kitsis (2005).
Death begets failure in the heart.
  J Clin Invest, 115, 565-571.  
15580265 T.Tenev, A.Zachariou, R.Wilson, M.Ditzel, and P.Meier (2005).
IAPs are functionally non-equivalent and regulate effector caspases through distinct mechanisms.
  Nat Cell Biol, 7, 70-77.  
15665817 U.Fischer, and K.Schulze-Osthoff (2005).
Apoptosis-based therapies and drug targets.
  Cell Death Differ, 12, 942-961.  
14685266 E.Burstein, L.Ganesh, R.D.Dick, B.van De Sluis, J.C.Wilkinson, L.W.Klomp, C.Wijmenga, G.J.Brewer, G.J.Nabel, and C.S.Duckett (2004).
A novel role for XIAP in copper homeostasis through regulation of MURR1.
  EMBO J, 23, 244-254.  
15372573 G.F.Prunell, and C.M.Troy (2004).
Balancing neuronal death.
  J Neurosci Res, 78, 1-6.  
15371430 J.C.Wilkinson, B.W.Richter, A.S.Wilkinson, E.Burstein, J.M.Rumble, B.Balliu, and C.S.Duckett (2004).
VIAF, a conserved inhibitor of apoptosis (IAP)-interacting factor that modulates caspase activation.
  J Biol Chem, 279, 51091-51099.  
15282301 J.C.Wilkinson, E.Cepero, L.H.Boise, and C.S.Duckett (2004).
Upstream regulatory role for XIAP in receptor-mediated apoptosis.
  Mol Cell Biol, 24, 7003-7014.  
14701799 J.Lewis, E.Burstein, S.B.Reffey, S.B.Bratton, A.B.Roberts, and C.S.Duckett (2004).
Uncoupling of the signaling and caspase-inhibitory properties of X-linked inhibitor of apoptosis.
  J Biol Chem, 279, 9023-9029.  
15610524 K.C.Ng, E.I.Campos, M.Martinka, and G.Li (2004).
XAF1 expression is significantly reduced in human melanoma.
  J Invest Dermatol, 123, 1127-1134.  
15161430 M.Holcík (2004).
Targeting endogenous inhibitors of apoptosis for treatment of cancer, stroke and multiple sclerosis.
  Expert Opin Ther Targets, 8, 241-253.  
14678329 M.Molmeret, S.D.Zink, L.Han, A.Abu-Zant, R.Asari, D.M.Bitar, and Y.Abu Kwaik (2004).
Activation of caspase-3 by the Dot/Icm virulence system is essential for arrested biogenesis of the Legionella-containing phagosome.
  Cell Microbiol, 6, 33-48.  
15107838 N.Yan, J.W.Wu, J.Chai, W.Li, and Y.Shi (2004).
Molecular mechanisms of DrICE inhibition by DIAP1 and removal of inhibition by Reaper, Hid and Grim.
  Nat Struct Mol Biol, 11, 420-428.
PDB codes: 1sdz 1se0
15086513 O.Tounekti, Y.Zhang, G.Klaiman, C.G.Goodyer, and A.LeBlanc (2004).
Proteasomal degradation of caspase-6 in 17beta-estradiol-treated neurons.
  J Neurochem, 89, 561-568.  
15520809 S.J.Riedl, and Y.Shi (2004).
Molecular mechanisms of caspase regulation during apoptosis.
  Nat Rev Mol Cell Biol, 5, 897-907.  
15146491 S.Piana, and U.Rothlisberger (2004).
Molecular dynamics simulations of structural changes during procaspase 3 activation.
  Proteins, 55, 932-941.  
15189137 X.Jiang, and X.Wang (2004).
Cytochrome C-mediated apoptosis.
  Annu Rev Biochem, 73, 87.  
15040837 Y.Liu, A.Porta, X.Peng, K.Gengaro, E.B.Cunningham, H.Li, L.A.Dominguez, T.Bellido, and S.Christakos (2004).
Prevention of glucocorticoid-induced apoptosis in osteocytes and osteoblasts by calbindin-D28k.
  J Bone Miner Res, 19, 479-490.  
15273300 Y.Shi (2004).
Caspase activation, inhibition, and reactivation: a mechanistic view.
  Protein Sci, 13, 1979-1987.  
15328523 Y.Yan, C.Mahotka, S.Heikaus, T.Shibata, N.Wethkamp, J.Liebmann, C.V.Suschek, Y.Guo, H.E.Gabbert, C.D.Gerharz, and U.Ramp (2004).
Disturbed balance of expression between XIAP and Smac/DIABLO during tumour progression in renal cell carcinomas.
  Br J Cancer, 91, 1349-1357.  
15337764 Z.Wang, M.Cuddy, T.Samuel, K.Welsh, A.Schimmer, F.Hanaii, R.Houghten, C.Pinilla, and J.C.Reed (2004).
Cellular, biochemical, and genetic analysis of mechanism of small molecule IAP inhibitors.
  J Biol Chem, 279, 48168-48176.  
14644196 A.Bergmann, A.Y.Yang, and M.Srivastava (2003).
Regulators of IAP function: coming to grips with the grim reaper.
  Curr Opin Cell Biol, 15, 717-724.  
12576135 A.Clerk, S.M.Cole, T.E.Cullingford, J.G.Harrison, M.Jormakka, and D.M.Valks (2003).
Regulation of cardiac myocyte cell death.
  Pharmacol Ther, 97, 223-261.  
14657035 A.Zachariou, T.Tenev, L.Goyal, J.Agapite, H.Steller, and P.Meier (2003).
IAP-antagonists exhibit non-redundant modes of action through differential DIAP1 binding.
  EMBO J, 22, 6642-6652.  
12887052 C.A.Ryan, and G.S.Salvesen (2003).
Caspases and neuronal development.
  Biol Chem, 384, 855-861.  
12833566 C.Z.Ni, C.Li, J.C.Wu, A.P.Spada, and K.R.Ely (2003).
Conformational restrictions in the active site of unliganded human caspase-3.
  J Mol Recognit, 16, 121-124.
PDB code: 1qx3
12620238 E.N.Shiozaki, J.Chai, D.J.Rigotti, S.J.Riedl, P.Li, S.M.Srinivasula, E.S.Alnemri, R.Fairman, and Y.Shi (2003).
Mechanism of XIAP-mediated inhibition of caspase-9.
  Mol Cell, 11, 519-527.
PDB code: 1nw9
12648453 I.S.Goping, M.Barry, P.Liston, T.Sawchuk, G.Constantinescu, K.M.Michalak, I.Shostak, D.L.Roberts, A.M.Hunter, R.Korneluk, and R.C.Bleackley (2003).
Granzyme B-induced apoptosis requires both direct caspase activation and relief of caspase inhibition.
  Immunity, 18, 355-365.  
12538646 I.Tamm, M.Trepel, M.Cardó-Vila, Y.Sun, K.Welsh, E.Cabezas, A.Swatterthwait, W.Arap, J.C.Reed, and R.Pasqualini (2003).
Peptides targeting caspase inhibitors.
  J Biol Chem, 278, 14401-14405.  
12752669 J.C.Lee, and M.E.Peter (2003).
Regulation of apoptosis by ubiquitination.
  Immunol Rev, 193, 39-47.  
12565009 M.Los, C.J.Burek, C.Stroh, K.Benedyk, H.Hug, and A.Mackiewicz (2003).
Anticancer drugs of tomorrow: apoptotic pathways as targets for drug design.
  Drug Discov Today, 8, 67-77.  
12446669 M.R.Olson, C.L.Holley, S.J.Yoo, J.R.Huh, B.A.Hay, and S.Kornbluth (2003).
Reaper is regulated by IAP-mediated ubiquitination.
  J Biol Chem, 278, 4028-4034.  
12833545 M.Sulpizi, A.Laio, J.VandeVondele, A.Cattaneo, U.Rothlisberger, and P.Carloni (2003).
Reaction mechanism of caspases: insights from QM/MM Car-Parrinello simulations.
  Proteins, 52, 212-224.  
12668429 M.Sulpizi, U.Rothlisberger, and P.Carloni (2003).
Molecular dynamics studies of caspase-3.
  Biophys J, 84, 2207-2215.  
12767037 P.Hersey, and X.D.Zhang (2003).
Overcoming resistance of cancer cells to apoptosis.
  J Cell Physiol, 196, 9.  
12648450 V.R.Sutton, M.E.Wowk, M.Cancilla, and J.A.Trapani (2003).
Caspase activation by granzyme B is indirect, and caspase autoprocessing requires the release of proapoptotic mitochondrial factors.
  Immunity, 18, 319-329.  
14512414 Y.Huang, R.L.Rich, D.G.Myszka, and H.Wu (2003).
Requirement of both the second and third BIR domains for the relief of X-linked inhibitor of apoptosis protein (XIAP)-mediated caspase inhibition by Smac.
  J Biol Chem, 278, 49517-49522.  
12660240 Z.Song, X.Yao, and M.Wu (2003).
Direct interaction between survivin and Smac/DIABLO is essential for the anti-apoptotic activity of survivin during taxol-induced apoptosis.
  J Biol Chem, 278, 23130-23140.  
11807173 C.D.Bortner, and J.A.Cidlowski (2002).
Cellular mechanisms for the repression of apoptosis.
  Annu Rev Pharmacol Toxicol, 42, 259-281.  
12021770 C.L.Holley, M.R.Olson, D.A.Colón-Ramos, and S.Kornbluth (2002).
Reaper eliminates IAP proteins through stimulated IAP degradation and generalized translational inhibition.
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12111795 C.M.Troy, and G.S.Salvesen (2002).
Caspases on the brain.
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12218061 C.R.Arnt, M.V.Chiorean, M.P.Heldebrant, G.J.Gores, and S.H.Kaufmann (2002).
Synthetic Smac/DIABLO peptides enhance the effects of chemotherapeutic agents by binding XIAP and cIAP1 in situ.
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12042762 G.S.Salvesen, and C.S.Duckett (2002).
IAP proteins: blocking the road to death's door.
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11852247 H.R.Stennicke, C.A.Ryan, and G.S.Salvesen (2002).
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12194817 I.Waizenegger, J.F.Giménez-Abián, D.Wernic, and J.M.Peters (2002).
Regulation of human separase by securin binding and autocleavage.
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12450324 J.Salgado, A.J.García-Sáez, G.Malet, I.Mingarro, and E.Pérez-Payá (2002).
Peptides in apoptosis research.
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11927604 J.Silke, C.J.Hawkins, P.G.Ekert, J.Chew, C.L.Day, M.Pakusch, A.M.Verhagen, and D.L.Vaux (2002).
The anti-apoptotic activity of XIAP is retained upon mutation of both the caspase 3- and caspase 9-interacting sites.
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12427028 L.E.Luque, K.P.Grape, and M.Junker (2002).
A highly conserved arginine is critical for the functional folding of inhibitor of apoptosis (IAP) BIR domains.
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12215447 O.Micheau, M.Thome, P.Schneider, N.Holler, J.Tschopp, D.W.Nicholson, C.Briand, and M.G.Grütter (2002).
The long form of FLIP is an activator of caspase-8 at the Fas death-inducing signaling complex.
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Phosphorylation by protein kinase CK2: a signaling switch for the caspase-inhibiting protein ARC.
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12501157 R.L.Rich, and D.G.Myszka (2002).
Survey of the year 2001 commercial optical biosensor literature.
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12011074 S.Li, Y.Zhao, X.He, T.H.Kim, D.K.Kuharsky, H.Rabinowich, J.Chen, C.Du, and X.M.Yin (2002).
Relief of extrinsic pathway inhibition by the Bid-dependent mitochondrial release of Smac in Fas-mediated hepatocyte apoptosis.
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Bcl-2 and Bcl-xL inhibit CD95-mediated apoptosis by preventing mitochondrial release of Smac/DIABLO and subsequent inactivation of X-linked inhibitor-of-apoptosis protein.
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Mechanisms of caspase activation and inhibition during apoptosis.
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12401491 Z.Huang (2002).
The chemical biology of apoptosis. Exploring protein-protein interactions and the life and death of cells with small molecules.
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Apoptosis and the response to anticancer therapy.
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11733216 D.C.Altieri (2001).
The molecular basis and potential role of survivin in cancer diagnosis and therapy.
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11701129 J.Chai, Q.Wu, E.Shiozaki, S.M.Srinivasula, E.S.Alnemri, and Y.Shi (2001).
Crystal structure of a procaspase-7 zymogen: mechanisms of activation and substrate binding.
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PDB codes: 1k86 1k88
11290317 L.Goyal (2001).
Cell death inhibition: keeping caspases in check.
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11690616 M.Dubois-Dauphin, Y.Pfister, P.G.Vallet, and A.Savioz (2001).
Prevention of apoptotic neuronal death by controlling procaspases? A point of view.
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11489640 P.Huang, and A.Oliff (2001).
Signaling pathways in apoptosis as potential targets for cancer therapy.
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11598496 R.W.Keane, S.Kraydieh, G.Lotocki, O.F.Alonso, P.Aldana, and W.D.Dietrich (2001).
Apoptotic and antiapoptotic mechanisms after traumatic brain injury.
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11752425 S.J.Riedl, P.Fuentes-Prior, M.Renatus, N.Kairies, S.Krapp, R.Huber, G.S.Salvesen, and W.Bode (2001).
Structural basis for the activation of human procaspase-7.
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PDB code: 1gqf
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Structural biology. Controlling the caspases.
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The most recent references are shown first. Citation data come partly from CiteXplore and partly from an automated harvesting procedure. Note that this is likely to be only a partial list as not all journals are covered by either method. However, we are continually building up the citation data so more and more references will be included with time. Where a reference describes a PDB structure, the PDB code is shown on the right.