Identification of autophosphorylation inhibitors of the inositol-requiring enzyme 1 alpha (IRE1α) by high-throughput screening using a DELFIA assay

Journal of Biomolecular Screening

Volumn 18, Issue 3, 2013, Pages 298-308

  Newbatt, Yvette ^a   Hardcastle, Anthea ^a   McAndrew, P Craig ^a   Strover, Jade A ^a   Mirza, Amin ^a   Morgan, Gareth J ^a   Burke, Rosemary ^a   Davies, Faith E ^a   Collins, Ian ^a   Van Montfort, Rob L M ^a  

^a INSTITUTE OF CANCER RESEARCH   (United Kingdom)

Author keywords

DELFIA; high throughput screening; inositol requiring enzyme 1 alpha; multiple myeloma; UPR; XBP1

Indexed keywords

ANTINEOPLASTIC AGENT; INOSITOL REQUIRING ENZYME 1 ALPHA; JNJ 7706621; NILOTINIB; OCT 249525; PHOSPHOTRANSFERASE; RIBONUCLEASE; SUNITINIB; UNCLASSIFIED DRUG; X BOX BINDING PROTEIN 1;

ANTIBODY SPECIFICITY; ARTICLE; AUTOPHOSPHORYLATION; CANCER SURVIVAL; CONTROLLED STUDY; DIMERIZATION; DRUG DETERMINATION; DRUG SCREENING; DRUG STRUCTURE; ENDOPLASMIC RETICULUM; ENZYME ACTIVATION; ENZYME ACTIVITY; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC 50; LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY; MULTIPLE MYELOMA; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; PROTEIN UNFOLDING; UNFOLDED PROTEIN RESPONSE; WESTERN BLOTTING;

ANIMALS; CELL LINE; ENDORIBONUCLEASES; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; INSECTS; MEMBRANE PROTEINS; MULTIPLE MYELOMA; PHOSPHORYLATION; PROTEIN FOLDING; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; UNFOLDED PROTEIN RESPONSE;

EID: 84873660457     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057112465647     Document Type: Article

References (28)

1. Lee K. P., Sicheri F.. Principles of IRE1 Modulation Using Chemical Tools. Methods Enzymol. 2011 ; 490: 271-292
2. Bernales S., Papa F. R., Walter P.. Intracellular Signaling by the Unfolded Protein Response. Annu. Rev. Cell. Dev. Biol. 2006 ; 22: 487-508
3. Davenport E. L., Morgan G. J., Davies F. E.. Untangling the Unfolded Protein Response. Cell Cycle. 2008 ; 7: 865-869 (Pubitemid 351573778)
4. Zhou J., Liu C. Y., Back S. H., Clark R. L., Peisach D., Xu Z., Kaufman R. J.. The Crystal Structure of Human IRE1 Luminal Domain Reveals a Conserved Dimerization Interface Required for Activation of the Unfolded Protein Response. Proc. Natl. Acad. Sci. U. S. A. 2006 ; 103: 14343-14348 (Pubitemid 44484752)
5. Oikawa D., Kimata Y.. Experimental Approaches for Elucidation of Stress-Sensing Mechanisms of the IRE1 Family Proteins. Methods Enzymol. 2011 ; 409: 195-216
6. Raab M. S., Podar K., Breitkreutz I., Richardson P. G., Anderson K. C.. Multiple Myeloma. Lancet. 2009 ; 374: 324-329
7. Davies F. E., Dring A. M., Li C., Rawson A. C., Shammas M. A., O'Connor S. M., Fenton J. A., Hideshima T., Chauhan D., Tai I. T., et al. Insights into the Multistep Transformation of MGUS to Myeloma Using Microarray Expression Analysis. Blood. 2003 ; 102: 4504-4511 (Pubitemid 37494117)
8. Davenport E. L., Moore H. E., Dunlop A. S., Sharpe S., Workman P., Morgan G. J., Davies F. E.. Heat Shock Protein Inhibition Is Associated with Activation of the Unfolded Protein Response Pathway in Myeloma Plasma Cells. Blood. 2007 ; 110: 2641-2649 (Pubitemid 47523188)
9. Bagratuni T., Wu P., Gonzalez De, Castro D., Davenport E. L., Dickens N. J., Walker B. A., Boyd K., Johnson D. C., Gregory W. M., Morgan G. J., et al. XBP1s Levels Are Implicated in the Biology and Outcome of Myeloma Mediating Differential Clinical Outcomes to Thalidomide-Based Treatments. Blood. 2010 ; 116: 250-253
10. Lee A.-H., Iwakoshi N. N., Anderson K. C., Glimcher L. H.. Proteasome Inhibitors Disrupt the Unfolded Protein Response in Myeloma Cells. Proc. Natl. Acad. Sci. U. S. A. 2003 ; 100: 9946-9951 (Pubitemid 37087048)
11. Ali M. M., Bagratuni T., Davenport E. L., Nowak P. R., Silva-Santisteban M. C., Hardcastle A., McAndrews C., Rowlands M. G., Morgan G. J., Aherne W., et al. Structure of the Ire1 Autophosphorylation Complex and Implications for the Unfolded Protein Response. EMBO J. 2011 ; 30: 894-905
12. Bouchecareilh M., Caruso M., Roby P., Parent S., Rouleau N., Taouji S., Pluquet O., Bosse R., Moenner M., Chevet E.. AlphaScreen-Based Characterization of the Biofunctional Kinase/RNase IRE1α: A Novel and Atypical Drug Target. J. Biomol. Screen. 2010 ; 15: 406-417
13. Newbatt Y., Burns S., Hayward R., Whittaker S., Kirk R., Marshall C., Springer C., McDonald E., Marais R., Workman P., Aherne W.. Identification of Inhibitors of the Kinase Activity of Ocogenic V600E BRAF in an Enzyme Cascade High-Throughput Screen. J. Biomol. Screen. 2006 ; 11 (2). 145-154
14. Zhang Z., Marshall A. G.. A Universal Algorithm for Fast and Automated Charge State Deconvolution of Electrospray Mass-to-Charge Ration Spectra. J. Am. Soc. Mass Spectrom. 1998 ; 9: 225-233 (Pubitemid 128370213)
15. Zhang J. H., Cheung 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)
16. 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
17. McGovern S. L., Helfand D. T., Feng B., Schoichet B. K.. A Specific Mechanism of Nonspecific Inhibition. J. Med. Chem. 2003 ; 46: 4265-4272 (Pubitemid 37153008)
18. Harris C. J., Hill D., Sheppard D. W., Slater M. J., Stouten P. F. W.. The design and Application of Target-Focused Compound Libraries. Comb. Chem. High Throughput Screen. 2011 ; 14: 521-531
19. Copeland R. A. Evaluation of Enzyme Inhibitors in Drug Discovery;. John Wiley: Hoboken, NJ ; 2005 :
20. MisraN. R.KimballD. S.RawlinsB. D.WebsterR. K.BursukerI.Preparation of Benzoylpyrazolo[3,4-b]pyridines and Analogs as Cyclin Dependent Kinase Inhibitors. Int. Patent Appl. WO9930710, 1999.
21. Witherington J., Bordas V., Garland S. L., Hickey D. M. B., Ife R. J., Liddle J., Saunders M., Smith D. G., Ward R. W.. 5-Aryl-pyrazolo[3,4-b] pyridines: Potent Inhibitors of Glycogen Synthase Kinase-3 (GSK-3). Bioorg. Med. Chem. Lett. 2003 ; 13: 1577-1580 (Pubitemid 36428564)
22. Dai Y., Hartandi K., Soni N. B., Pease L. J., Reuter D. R., Olson A. M., Osterling D. J., Doktor S. Z., Albert D. H., Bouska J. J., et al. Identification of Aminopyrazolopyridine Ureas as Potent VEGFR/PDGFR Multitargeted Kinase Inhibitors. Bioorg. Med. Chem. Lett. 2008 ; 18: 386-390
23. BedjeguelalK.RabotR.KalounE. B.MayerP.MarchandA.RahierN.SchambelP. BienaymeH.Preparation of Pyrazolopyridine Derivatives as ALK Kinase Inhibitors for Treating Cancer. Int. Patent Appl. WO2011045344, 2011.
24. Emanuel S., Rugg C. A., Gruninger R. H., Lin R., Fuentes-Pesquera A., Connolly P. J., Wetter S. K., Hollister B., Kruger W. W., Napier C., et al. The In Vitro and In Vivo Effects of JNJ-7706621: A Dual Inhibitor of Cyclin-Dependent Kinases and Aurora Kinases. Cancer Res. 2005 ; 65: 9038-9046 (Pubitemid 41377396)
25. Malerich J. P., Lam J. S., Hart B., Fine R. M., Klebansky B., Tanga M. J., D'Andrea A.. Diamino-1,2,4-triazole Derivatives are Selective Inhibitors of TYK2 and JAK1 over JAK2 and JAK3. Bioorg. Med. Chem. Lett. 2010 ; 20: 7454-7457
26. Wiseman R. L., Zhang Y., Lee K. P., Harding H. P., Haynes C. M., Price J., Sicheri F., Ron D.. Flavonol Activation Defines an Unanticipated Ligand-Binding Site in the Kinase-RNase Domain of IRE1. Mol. Cell. 2010 ; 38: 291-304
27. Manley P. W., Drueckes P., Fendrich G., Furet P., Liebetanz J., Martiny-Baron G., Mestan J., Trappe J., Wartmann M., Fabbro D.. Extended Kinase Profile and Properties of the Protein Kinase Inhibitor Nilotinib. Biochim. Biophys. Acta. 2010 ; 1804: 445-453
28. Capdeville R., Buchdunger E., Zimmermann J., Matter A.. Glivec (STI571, imatinib), a Rationally Developed, Targeted Anticancer Drug. Nat. Rev. Drug Discov. 2002 ; 1: 493-502