Potent and selective small-molecule inhibitors of cIAP1/2 proteins reveal that the binding of Smac mimetics to XIAP BIR3 is not required for their effective induction of cell death in tumor cells.

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Potent and selective small-molecule inhibitors of cIAP1/2 proteins reveal that the binding of Smac mimetics to XIAP BIR3 is not required for their effective induction of cell death in tumor cells. is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1021/CB400889A
P932PMC publication ID4324444
P698PubMed publication ID24521431
P5875ResearchGate publication ID260168177

P50authorShaomeng WangQ44006873
Haiying SunQ88797882
P2093author name stringLiu Liu
Chao-Yie Yang
Jianfeng Lu
P2860cites workIAPs: from caspase inhibitors to modulators of NF-kappaB, inflammation and cancerQ24292870
Distinct BIR domains of cIAP1 mediate binding to and ubiquitination of tumor necrosis factor receptor-associated factor 2 and second mitochondrial activator of caspasesQ24294565
IAP antagonists induce autoubiquitination of c-IAPs, NF-kappaB activation, and TNFalpha-dependent apoptosisQ24300707
IAP antagonists target cIAP1 to induce TNFalpha-dependent apoptosisQ24300734
Autocrine TNFalpha signaling renders human cancer cells susceptible to Smac-mimetic-induced apoptosisQ24609324
Structural basis for binding of Smac/DIABLO to the XIAP BIR3 domainQ27629143
Structural basis of IAP recognition by Smac/DIABLOQ27629148
Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPsQ27643305
Structure-Based Design, Synthesis, Evaluation, and Crystallographic Studies of Conformationally Constrained Smac Mimetics as Inhibitors of the X-linked Inhibitor of Apoptosis Protein (XIAP) †Q27652682
Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffoldQ27653852
Antagonism of c-IAP and XIAP proteins is required for efficient induction of cell death by small-molecule IAP antagonistsQ27655724
Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152)Q27678027
Design and synthesis of potent inhibitor of apoptosis (IAP) proteins antagonists bearing an octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline mimeticQ27683730
Smac, a mitochondrial protein that promotes cytochrome c-dependent caspase activation by eliminating IAP inhibitionQ28115131
Identification of DIABLO, a mammalian protein that promotes apoptosis by binding to and antagonizing IAP proteinsQ28117928
Development and validation of a genetic algorithm for flexible dockingQ28236574
IAP family proteins--suppressors of apoptosisQ28297514
Improved protein-ligand docking using GOLDQ29616787
IAP proteins: blocking the road to death's doorQ29619844
Expression and prognostic significance of IAP-family genes in human cancers and myeloid leukemiasQ31379722
Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteinsQ34116053
XIAP: apoptotic brake and promising therapeutic target.Q34303728
A small molecule Smac mimic potentiates TRAIL- and TNFalpha-mediated cell deathQ34346499
Caspases, IAPs and Smac/DIABLO: mechanisms from structural biologyQ35874476
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatmentQ36460712
Design, synthesis, and characterization of a potent, nonpeptide, cell-permeable, bivalent Smac mimetic that concurrently targets both the BIR2 and BIR3 domains in XIAPQ36909606
Inhibitor of apoptosis proteins as targets for anticancer therapyQ36950485
The inhibitor of apoptosis proteins as therapeutic targets in cancerQ36975583
Design, synthesis, and evaluation of tricyclic, conformationally constrained small-molecule mimetics of second mitochondria-derived activator of caspasesQ37143013
Design of small-molecule peptidic and nonpeptidic Smac mimeticsQ37176751
Potent, orally bioavailable diazabicyclic small-molecule mimetics of second mitochondria-derived activator of caspasesQ37185121
A potent bivalent Smac mimetic (SM-1200) achieving rapid, complete, and durable tumor regression in miceQ37249659
IAP-targeted therapies for cancerQ37302745
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.Q37445045
Design, synthesis, and evaluation of potent, nonpeptidic mimetics of second mitochondria-derived activator of caspasesQ37481457
IAP antagonists: promising candidates for cancer therapyQ37680131
Targeting IAP proteins for therapeutic intervention in cancerQ37980321
Requirement of Both the Second and Third BIR Domains for the Relief of X-linked Inhibitor of Apoptosis Protein (XIAP)-mediated Caspase Inhibition by SmacQ39389950
Discovery of aminopiperidine-based Smac mimetics as IAP antagonistsQ39408947
A Smac mimetic rescue screen reveals roles for inhibitor of apoptosis proteins in tumor necrosis factor-alpha signalingQ40033734
Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.Q40192019
Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancerQ40524353
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.Q40528633
IAP family protein expression correlates with poor outcome of multiple myeloma patients in association with chemotherapy-induced overexpression of multidrug resistance genes.Q52009124
Expression of the IAP protein family is dysregulated in pancreatic cancer cells and is important for resistance to chemotherapyQ79801646
Overexpression of XIAP expression in renal cell carcinoma predicts a worse prognosisQ79857928
Design of Small-Molecule Smac Mimetics as IAP AntagonistsQ82436664
Structure-based design of potent, conformationally constrained Smac mimeticsQ95801450
P433issue4
P921main subjectcell deathQ2383867
P304page(s)994-1002
P577publication date2014-02-12
P1433published inACS Chemical BiologyQ165583
P1476titlePotent and selective small-molecule inhibitors of cIAP1/2 proteins reveal that the binding of Smac mimetics to XIAP BIR3 is not required for their effective induction of cell death in tumor cells
P478volume9

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cites work (P2860)
Q40555960Absence of RIPK3 predicts necroptosis resistance in malignant melanoma
Q35774947Avian pathogenic Escherichia coli (APEC) infection alters bone marrow transcriptome in chickens
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Q60302272DEBIO 1143, an IAP inhibitor, reverses carboplatin resistance in ovarian cancer cells and triggers apoptotic or necroptotic cell death
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Q35780628Lipid-conjugated Smac analogues
Q40648639Molecular Pathways: The Balance between Cancer and the Immune System Challenges the Therapeutic Specificity of Targeting Nuclear Factor-κB Signaling for Cancer Treatment
Q34263719Small-molecule inhibitors of protein-protein interactions: progressing toward the reality
Q102075600Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes

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