A homogeneous HTRF assay for the identification of inhibitors of the TWEAK-Fn14 protein interaction

Journal of Biomolecular Screening

Volumn 17, Issue 7, 2012, Pages 933-945

  Benicchi, Tiziana ^a   Iozzi, Sara ^a   Svahn, Andreas ^b   Axelsson, Hanna ^b   Mori, Elisa ^a   Bernocco, Simonetta ^a   Cappelli, Federico ^a   Caramelli, Chiara ^a   Fanti, Paola ^a   Genesio, Eva ^a   MacCari, Laura ^a   Markova, Natalia ^b   Micco, Iolanda ^a   Porcari, Valentina ^a   Schultz, Johan ^b   Fecke, Wolfgang ^a  

^a Siena Biotech SpA   (Italy)

^b INovacia AB ^*  (Sweden)

Author keywords

Fn14; HTRF; inflammatory diseases; protein protein interaction; TWEAK

Indexed keywords

IMMUNOGLOBULIN ENHANCER BINDING PROTEIN; PROTEIN; PROTEIN FN14; PROTEIN TWEAK; UNCLASSIFIED DRUG;

ARTICLE; BIOASSAY; CONCENTRATION RESPONSE; CONTROLLED STUDY; HOMOGENEOUS TIME RESOLVED FLUORESCENCE ASSAY; HUMAN; IC 50; PRIORITY JOURNAL; PROTEIN AGGREGATION; PROTEIN EXPRESSION; PROTEIN PROTEIN INTERACTION; PROTEIN STABILITY; SOLUBILITY;

AUTOIMMUNE DISEASES; CELL LINE; DRUG SCREENING ASSAYS, ANTITUMOR; HEK293 CELLS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; INFLAMMATION; NEOPLASMS; PEPTIDES; RECEPTORS, TUMOR NECROSIS FACTOR; TUMOR NECROSIS FACTORS;

ANIMALIA;

EID: 84863827333     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057112447873     Document Type: Article

References (39)

1. Chicheportiche Y., Bourdon P., Xu H., Hsu Y., Scott H., Hession C., Garcia I., Browning J. L.. TWEAK, a New Secreted Ligand in the Tumor Necrosis Factor Family That Weakly Induces Apoptosis. J. Biol. Chem. 1997 ; 272: 32401-32410 (Pubitemid 28011923)
2. Schneider P., Schwenzer R., Haas E., Mühlenbeck F., Schubert G., Scheurich P., Tschopp J., Wajant H.. TWEAK Can Induce Cell Death via Endogenous TNF and TNF Receptor 1. Eur. J. Immunol. 1999 ; 29: 1785-1792 (Pubitemid 29265533)
3. Wiley S., Cassiano L., Lofton T., Davis-Smith T., Winkles J., Lindner V., Liu H., Daniel T. O., Smith C. A., Fanslow W. C.. A Novel TNF Receptor Family Member Binds TWEAK and Is Implicated in Angiogenesis. Immunity. 2001 ; 15: 836-846
4. Meighan-Mantha R., Hsu D., Guo Y., Brown S., Feng S., Peifley K., Alberts G. F., Copeland N. G., Gilbert D. J., Jenkins N. A., et al. The Mitogen-Inducible Fn14 Gene Encodes a Type I Transmembrane Protein That Modulates Fibroblast Adhesion and Migration. J. Biol. Chem. 1999 ; 274: 33166-33176 (Pubitemid 129535361)
5. Brown S., Ghosh A., Winkles J.. Full-Length, Membrane-Anchored TWEAK Can Function as a Juxtacrine Signaling Molecule and Activate the NF-kappaB Pathway. J. Biol. Chem. 2010 ; 285: 17432-17441
6. Brown S., Richards C., Hanscom H., Feng S., Winkles J.. The Fn14 Cytoplasmic Tail Binds Tumour-Necrosis-Factor-Receptor-Associated Factors 1, 2, 3 and 5 and Mediates Nuclear Factor-kappaB Activation. Biochem. J. 2003 ; 371: 395-403 (Pubitemid 36547622)
7. Wicovsky A., Salzmann S., Roos C., Ehrenschwender M., Rosenthal T., Siegmund D., Henkler F., Gohlke F., Kneitz C., Wajant H.. TNF-Like Weak Inducer of Apoptosis Inhibits Proinflammatory TNF Receptor-1 Signaling. Cell Death Differ. 2009 ; 16: 1445-1459
8. Lynch C., Wang Y., Lund J., Chen Y., Leal J., Wiley S.. TWEAK Induces Angiogenesis and Proliferation of Endothelial Cells. J. Biol. Chem. 1999 ; 274: 8455-8459 (Pubitemid 29164634)
9. Ikner A., Ashkenazi A.. TWEAK Induces Apoptosis through a Death-Signaling Complex Comprising Receptor-interacting Protein 1 (RIP1), Fas-Associated Death Domain (FADD), and Caspase-8. J. Biol. Chem. 2011 ; 286: 21546-21554
10. Perper S., Browning B., Burkly L., Weng S., Gao C., Giza K., Su L., Tarilonte L., Crowell T., Rajman L., et al. TWEAK Is a Novel Arthritogenic Mediator. J. Immunol. 2006 ; 177: 2610-2620 (Pubitemid 44201020)
11. Serafini B., Magliozzi R., Rosicarelli B., Reynolds R., Zheng T., Aloisi F.. Expression of TWEAK and Its Receptor Fn14 in the Multiple Sclerosis Brain: Implications for Inflammatory Tissue Injury. J. Neuropathol. Exp. Neurol. 2008 ; 67: 1137-1148
12. Haile W., Echeverry R., Wu F., Guzman J., An J., Wu J., Yepes M.. Tumor Necrosis Factor-Like Weak Inducer of Apoptosis and Fibroblast Growth Factor-Inducible 14 Mediate Cerebral Ischemia-Induced Poly(ADP-ribose) Polymerase-1 Activation and Neuronal Death. Neuroscience. 2010 ; 171: 1256-1264
13. Ho D., Vu H., Brown S., Donohue P., Hanscom H., Winkles J.. Soluble Tumor Necrosis Factor-Like Weak Inducer of Apoptosis Overexpression in HEK293 Cells Promotes Tumor Growth and Angiogenesis in Athymic Nude Mice. Cancer Res. 2004 ; 64: 8968-8972 (Pubitemid 39665505)
14. Winkles J. A.. The TWEAK-Fn14 Cytokine-Receptor Axis: Discovery, Biology and Therapeutic Targeting. Nat. Rev. Drug Discov. 2008 ; 7: 411-425 (Pubitemid 351619113)
15. Tansey M., Szymkowski D.. The TNF Superfamily in 2009: New Pathways, New Indications, and New Drugs. Drug Discov. Today. 2009 ; 14: 1082-1088
16. Donohue P., Richards C., Brown S., Hanscom H., Buschman J., Thangada S., Hla T., Williams M. S., Winkles J. A.. TWEAK Is an Endothelial Cell Growth and Chemotactic Factor That Also Potentiates FGF-2 and VEGF-A Mitogenic Activity. Arterioscler. Thromb. Vasc. Biol. 2003 ; 23: 594-600 (Pubitemid 36438071)
17. Gotoh Y., Nagata H., Kase H., Shimonishi M., Ido M.. A Homogeneous Time-Resolved Fluorescence-Based High-Throughput Screening System for Discovery of Inhibitors of IKKβ-NEMO Interaction. Anal. Biochem. 2010 ; 405: 19-27
18. Zinzalla G., Thurston D. E.. Targeting Protein-Protein Interactions for Therapeutic Intervention: A Challenge for the Future. Future Med. Chem. 2009 ; 1: 65-93
19. He M., Smith A., Oslob J., Flanagan W., Braisted A., Whitty A., Cancilla M. T., Wang J., Lugovskoy A. A., Yoburn J. C., et al. Small-Molecule Inhibition of TNF-alpha. Science. 2005 ; 310: 1022-1025
20. Silvian L., Friedman J., Strauch K., Cachero T., Day E., Qian F., Cunningham B., Fung A., Sun L., Shipps G. W., et al. Small Molecule Inhibition of the TNF Family Cytokine CD40 Ligand through a Subunit Fracture Mechanism. ACS Chem. Biol. 2011 ; 6: 636-647
21. Brown A., Hanscom H., Vu H., Shelesa A., Winkles J.. TWEAK Binding to the Fn14 Cysteine-Rich Domain Depends on Charged Residues Located in Both the A1 and D2 Modules. Biochem. J. 2006 ; 397: 297-304 (Pubitemid 44076899)
22. Maloff B. L., Delmendo R. E.. Development of High-Throughput Radioligand Binding Assays for Interleukin-1 alpha (IL-1 alpha) and Tumor Necrosis Factor (TNF-alpha) in Isolated Membrane Preparations. Agents Actions. 1991 ; 34: 132-134
23. Buller F., Zhang Y., Scheuermann J., Schäfer J., Bühlmann P., Neri D.. Discovery of TNF Inhibitors from a DNA-Encoded Chemical Library Based on Diels-Alder Cycloaddition. Chem. Biol. 2009 ; 16: 1075-1086
24. Moore K., Turconi S., Miles-Williams A., Djaballah H., Hurskainen P., Harrop J., Murray K. J., Pope A. J.. A Homogenous 384-Well High Throughput Screen for Novel Tumor Necrosis Factor Receptor: Ligand Interactions Using Time Resolved Energy Transfer. J. Biomol. Screen. 1999 ; 4: 205-214 (Pubitemid 29432007)
25. Wilson J., Rossi C., Carboni S., Fremaux C., Perrin D., Soto C., Kosco-Vilbois M., Scheer A.. A Homogeneous 384-Well High-Throughput Binding Assay for a TNF Receptor Using AlphaScreen Technology. J. Biomol. Screen. 2003 ; 8: 522-532
26. Wiley S. R., Winkles J. A.. TWEAK, a Member of the TNF Superfamily, Is a Multifunctional Cytokine That Binds the TweakR/Fn14 Receptor. Cytokine Growth Factor Rev. 2003 ; 14: 241-249 (Pubitemid 36693144)
27. Lipinski C. A., Lombardo F., Feeney B. W., Dominy P. J.. Experimental and Computational Approaches to Estimate Solubility and Permeability in Drug Discovery and Development Settings. Adv. Drug Deliv. Rev. 2001 ; 46: 3-26 (Pubitemid 33653411)
28. Veber D., Johnson S., Cheng H., Smith B., Ward K., Kopple K.. Molecular Properties That Influence the Oral Bioavailability of Drug Candidates. J. Med. Chem. 2002 ; 45: 2615-2623 (Pubitemid 34595232)
29. Lamanna C., Bellini M., Padova A., Westerberg G., Maccari L.. Straightforward Recursive Partitioning Model for Discarding Insoluble Compounds in the Drug Discovery Process. J. Med. Chem. 2008 ; 51: 2891-2897 (Pubitemid 351711191)
30. Baell J. B., Holloway G. A.. New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays. J. Med. Chem. 2010 ; 53: 2719-2740
31. Ritchie T. J., Macdonald S. J.. The Impact of Aromatic Ring Count on Compound Developability: Are Too Many Aromatic Rings a Liability in Drug Design?. Drug Discov. Today. 2009 ; 14: 1011-1020
32. He F., Dang W., Saito K., Watanabe S., Kobayashi N., Güntert P., Kigawa T., Tanaka A., Muto Y., Yokoyama S.. Solution Structure of the Cysteine-Rich Domain in Fn14, a Member of the Tumor Necrosis Factor Receptor Superfamily. Protein Sci. 2009 ; 18: 650-656
33. Zhang J. H., Chung T. D., Oldenburg K. R.. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays. J. Biomol. Screen. 1999 ; 4: 67-73 (Pubitemid 29278954)
34. Lor L., Schneck J., McNulty D., Diaz E., Brandt M., Thrall S., Schwartz B.. A Simple Assay for Detection of Small-Molecule Redox Activity. J. Biomol. Screen. 2007 ; 12: 881-890 (Pubitemid 47340702)
35. Bover L., Cardó-Vila M., Kuniyasu A., Sun J., Rangel R., Takeya M., Aggarwal B. B., Arap W., Pasqualini R.. A Previously Unrecognized Protein-Protein Interaction between TWEAK and CD163: Potential Biological Implications. J. Immunol. 2007 ; 178: 8183-8194 (Pubitemid 46898091)
36. Mancini F., Toro C., Mabilia M., Giannangeli M., Pinza M., Milanese C.. Inhibition of Tumor Necrosis Factor-alpha (TNF-alpha)/TNF-alpha Receptor Binding by Structural Analogues of Suramin. Biochem. Pharmacol. 1999 ; 58: 851-859 (Pubitemid 29329536)
37. Coan K. E., Shoichet B. K.. Stability and Equilibria of Promiscuous Aggregates in High Protein Milieus. Mol. Biosyst. 2007 ; 3: 208-213 (Pubitemid 46293327)
38. Saitoh T., Nakayama M., Nakano H., Yagita H., Yamamoto N.Y.. TWEAK Induces NF-kappaB2 p100 Processing and Long Lasting NF-kappaB Activation. J. Biol. Chem. 2003 ; 278: 36005-36012 (Pubitemid 37139919)
39. Vince J., Chau D., Callus B., Wong W., Hawkins C., Schneider P., McKinlay M., Benetatos C. A., Condon S. M., Chunduru S. K., et al. TWEAK-FN14 Signaling Induces Lysosomal Degradation of a cIAP1-TRAF2 Complex to Sensitize Tumor Cells to TNFalpha. J. Cell. Biol. 2008 ; 182: 171-184 (Pubitemid 352008630)