Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs
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Autocrine TNFalpha signaling renders human cancer cells susceptible to Smac-mimetic-induced apoptosisInteraction of a Cyclic, Bivalent Smac Mimetic with the X-Linked Inhibitor of Apoptosis Protein † ‡Structure-Based Design, Synthesis, Evaluation, and Crystallographic Studies of Conformationally Constrained Smac Mimetics as Inhibitors of the X-linked Inhibitor of Apoptosis Protein (XIAP) †Conformational Changes in Bcl-2 Pro-survival Proteins Determine Their Capacity to Bind LigandsRecognition of Smac-mimetic compounds by the BIR domain of cIAP1Antagonists induce a conformational change in cIAP1 that promotes autoubiquitinationDiscovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152)The structure of XIAP BIR2: understanding the selectivity of the BIR domainsIdentification of a Small Peptide That Inhibits PCSK9 Protein Binding to the Low Density Lipoprotein ReceptorSmall molecules destabilize cIAP1 by activating auto-ubiquitylationExpedient synthesis of highly potent antagonists of inhibitor of apoptosis proteins (IAPs) with unique selectivity for ML-IAPThe Targeted SMAC Mimetic SW IV-134 is a strong enhancer of standard chemotherapy in pancreatic cancerEnabling large-scale design, synthesis and validation of small molecule protein-protein antagonistsA specificity map for the PDZ domain familyNovel Bcl-2 homology-3 domain-like sequences identified from screening randomized peptide libraries for inhibitors of the pro-survival Bcl-2 proteins.Conjugation to a SMAC mimetic potentiates sigma-2 ligand induced tumor cell death in ovarian cancerTargeted pancreatic cancer therapy with the small molecule drug conjugate SW IV-134.Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.SMAC mimetic (JP1201) sensitizes non-small cell lung cancers to multiple chemotherapy agents in an IAP-dependent but TNF-α-independent mannerCyclopeptide Smac mimetics as antagonists of IAP proteins.Smac mimetic SM-164 potentiates APO2L/TRAIL- and doxorubicin-mediated anticancer activity in human hepatocellular carcinoma cellsPotent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.Small-molecule IAP antagonists sensitize cancer cells to TRAIL-induced apoptosis: roles of XIAP and cIAPs.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.X-linked inhibitor of apoptosis positive nuclear labeling: a new independent prognostic biomarker of breast invasive ductal carcinoma.Synthetic mimetics of protein secondary structure domainsSmac mimetic enables the anticancer action of BCG-stimulated neutrophils through TNF-α but not through TRAIL and FasL.Using protein motion to read, write, and erase ubiquitin signals.Nucleotide composition of cellular internal ribosome entry sites defines dependence on NF45 and predicts a posttranscriptional mitotic regulonDesign, synthesis, and characterization of a potent, nonpeptide, cell-permeable, bivalent Smac mimetic that concurrently targets both the BIR2 and BIR3 domains in XIAPInhibitor of apoptosis proteins as targets for anticancer therapy.Both cIAP1 and cIAP2 regulate TNFalpha-mediated NF-kappaB activationDesign, synthesis, and evaluation of tricyclic, conformationally constrained small-molecule mimetics of second mitochondria-derived activator of caspases.Design of small-molecule peptidic and nonpeptidic Smac mimetics.Potent, orally bioavailable diazabicyclic small-molecule mimetics of second mitochondria-derived activator of caspases.IAP proteins as targets for drug development in oncologyA potent bivalent Smac mimetic (SM-1200) achieving rapid, complete, and durable tumor regression in mice.Inhibitor of apoptosis proteins in hematological malignancies.Smac-mimetic-induced epithelial cell death reduces the growth of renal cysts.Importance of ligand reorganization free energy in protein-ligand binding-affinity prediction.
P2860
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P2860
Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs
description
2006 nî lūn-bûn
@nan
2006 թուականի Սեպտեմբերին հրատարակուած գիտական յօդուած
@hyw
2006 թվականի սեպտեմբերին հրատարակված գիտական հոդված
@hy
2006年の論文
@ja
2006年論文
@yue
2006年論文
@zh-hant
2006年論文
@zh-hk
2006年論文
@zh-mo
2006年論文
@zh-tw
2006年论文
@wuu
name
Design, synthesis, and biologi ...... apoptosis by antagonizing IAPs
@ast
Design, synthesis, and biologi ...... apoptosis by antagonizing IAPs
@en
Design, synthesis, and biologi ...... apoptosis by antagonizing IAPs
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type
label
Design, synthesis, and biologi ...... apoptosis by antagonizing IAPs
@ast
Design, synthesis, and biologi ...... apoptosis by antagonizing IAPs
@en
Design, synthesis, and biologi ...... apoptosis by antagonizing IAPs
@nl
prefLabel
Design, synthesis, and biologi ...... apoptosis by antagonizing IAPs
@ast
Design, synthesis, and biologi ...... apoptosis by antagonizing IAPs
@en
Design, synthesis, and biologi ...... apoptosis by antagonizing IAPs
@nl
P2093
P3181
P356
P1433
P1476
Design, synthesis, and biologi ...... apoptosis by antagonizing IAPs
@en
P2093
David C Okawa
Domagoj Vucic
Eugene Varfolomeev
Heidi J A Wallweber
John A Flygare
Kerry Zobel
Kurt Deshayes
Linda O Elliott
Matthew C Franklin
P304
P3181
P356
10.1021/CB600276Q
P577
2006-09-19T00:00:00Z