Journal ArticleDOI
Development and optimization of a binding assay for the XIAP BIR3 domain using fluorescence polarization
Zaneta Nikolovska-Coleska,Renxiao Wang,Xueliang Fang,Hongguang Pan,York Tomita,Peng Li,Peter P. Roller,Krzysztof Krajewski,Naoyuki G. Saito,Jeanne A. Stuckey,Shaomeng Wang +10 more
TLDR
The development of a homogeneous high-throughput assay based on fluorescence polarization for measuring the binding affinities of small-molecule inhibitors to the BIR3 domain of XIAP and results obtained indicated that the FP-based competitive binding assay performs correctly as designed.About:
This article is published in Analytical Biochemistry.The article was published on 2004-09-15. It has received 507 citations till now. The article focuses on the topics: XIAP & Ligand binding assay.read more
Citations
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Journal ArticleDOI
IAP Antagonists Target cIAP1 to Induce TNFα-Dependent Apoptosis
James E Vince,W. Wei-Lynn Wong,Nufail Khan,Rebecca Feltham,Diep Chau,Afsar U. Ahmed,Christopher A. Benetatos,Srinivas K. Chunduru,Stephen M. Condon,Mark A. McKinlay,Robert Brink,Martin Leverkus,Vinay Tergaonkar,Pascal Schneider,Bernard A. Callus,Frank Koentgen,David L. Vaux,John Silke +17 more
TL;DR: It is shown that apoptosis caused by an IAC is blocked by the caspase 8 inhibitor crmA and that IAP antagonists activate NF-κB signaling via inhibtion of cIAP1.
Journal ArticleDOI
The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models
András Kotschy,Szlávik Zoltán,James A. H. Murray,James Edward Paul Davidson,Ana Leticia Maragno,Gaëtane Le Toumelin-Braizat,Maïa Chanrion,Gemma L. Kelly,Gemma L. Kelly,Jia-Nan Gong,Jia-Nan Gong,Donia M Moujalled,Alain Bruno,Csékei Márton,Attila Paczal,Zoltán B. Szabó,Szabolcs Sipos,Gabor Radics,Proszenyák Ágnes,Balázs Bálint,Levente Ondi,Gábor Blasko,Alan P. Robertson,Allan E. Surgenor,Pawel Dokurno,Chen I-Jen,Natalia Matassova,Julia Smith,C. Pedder,Chris Graham,Aurélie Studeny,Gaëlle Lysiak-Auvity,Anne-Marie Girard,Fabienne Gravé,David J. Segal,David J. Segal,Chris D. Riffkin,Chris D. Riffkin,Giovanna Pomilio,Laura C. A. Galbraith,Laura C. A. Galbraith,Brandon J. Aubrey,Brandon J. Aubrey,Brandon J. Aubrey,Margs S. Brennan,Margs S. Brennan,Marco J Herold,Marco J Herold,Catherine Chang,Catherine Chang,Ghislaine Guasconi,Nicolas Cauquil,Fabien Melchiore,Nolwen Guigal-Stephan,Brian Lockhart,Frédéric Colland,John A. Hickman,Andrew W. Roberts,David C.S. Huang,David C.S. Huang,Andrew H. Wei,Andrew H. Wei,Andreas Strasser,Andreas Strasser,Guillaume Lessene,Guillaume Lessene,Olivier Geneste +66 more
TL;DR: It is demonstrated that S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway.
Journal ArticleDOI
IC50-to-Ki: a web-based tool for converting IC50 to Ki values for inhibitors of enzyme activity and ligand binding
TL;DR: A new web-server tool estimates Ki values from experimentally determined IC50 values for inhibitors of enzymes and of binding reactions between macromolecules and ligands to enable end users to help gauge the quality of the underlying assumptions used in these calculations.
Journal ArticleDOI
Fluorescence Polarization Assays in Small Molecule Screening
Wendy A. Lea,Anton Simeonov +1 more
TL;DR: In addition to its continued utilization in high-throughput screening, FP has expanded into new disease and target areas and has been marked by increased use of labeled small molecule ligands for receptor-binding studies.
Journal ArticleDOI
Analysis of protein-ligand interactions by fluorescence polarization
Ana M. Rossi,Colin W. Taylor +1 more
TL;DR: An FP assay in which binding of fluorescein-labeled inositol 1,4,5-trisphosphate (IP3) to N-terminal fragments of IP3 receptors can be characterized at different temperatures and in competition with other ligands is described.
References
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Journal ArticleDOI
Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.
TL;DR: The analysis described shows K I does not equal I 50 when competitive inhibition kinetics apply; however, K I is equal to I 50 under conditions of either noncompetitive or uncompetitive kinetics.
Journal ArticleDOI
A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays.
TL;DR: A screening window coefficient, called "Z- factor," is defined, which is reflective of both the assay signal dynamic range and the data variation associated with the signal measurements, and therefore is suitable for assay quality assessment.
Journal ArticleDOI
A novel anti-apoptosis gene, survivin , expressed in cancer and lymphoma
TL;DR: It is suggested that apoptosis inhibition may be a general feature of neoplasia and survivin is identified as a potential new target for apoptosis-based therapy in cancer and lymphoma.
Journal ArticleDOI
IAP family proteins—suppressors of apoptosis
Quinn Deveraux,John C. Reed +1 more
TL;DR: Although the mechanism used by the IAPs to suppress cell death remains debated, several studies have provided insights into the biochemical functions of these intriguing proteins and a variety of reports have suggested an important role for the I APs in some human diseases.
Journal ArticleDOI
IAP proteins: blocking the road to death's door
Guy S. Salvesen,Colin S. Duckett +1 more
TL;DR: The functional and structural properties of the IAP gene family, a group of structurally related proteins that, in addition to their ability to suppress apoptotic cell death, are involved in an increasing number of seemingly unrelated cellular functions, are reviewed.
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