A Homogeneous, High-Throughput Assay for Phosphatidylinositol 5-Phosphate 4-Kinase with a Novel, Rapid Substrate Preparation

PLoS ONE

Volumn 8, Issue 1, 2013, Pages

  Davis, Mindy I ^a   Sasaki, Atsuo T ^b,c   Shen, Min ^a   Emerling, Brooke M ^b   Thorne, Natasha ^a   Michael, Sam ^a   Pragani, Rajan ^a   Boxer, Matthew ^a   Sumita, Kazutaka ^c   Takeuchi, Koh ^d   Auld, Douglas S ^a,e   Li, Zhuyin ^a   Cantley, Lewis C ^b   Simeonov, Anton ^a  

^a NATIONAL INSTITUTES OF HEALTH   (United States)

^b HARVARD MEDICAL SCHOOL   (United States)

^c UNIVERSITY OF CINCINNATI COLLEGE OF MEDICINE   (United States)

^d NATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE AND TECHNOLOGY AIST   (Japan)

^e NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DIMETHYL SULFOXIDE; I OME TYRPHOSTIN AG 538; LIPOSOME; PHOSPHATIDYLINOSITOL 5 PHOSPHATE 4 KINASE ALPHA; PHOSPHATIDYLINOSITOL KINASE; TYRPHOSTIN; TYRPHOSTIN AG 82; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; ENZYME ASSAY; ENZYME INHIBITION; ENZYME ISOLATION; ENZYME SUBSTRATE; HIGH THROUGHPUT SCREENING; IC 50; LUCIFERASE COUPLED BIOLUMINESCENCE 1536 WELL PHOSPHATIDYLINOSITOL 5 PHOSPHATE 4 KINASE ASSAY;

1-PHOSPHATIDYLINOSITOL 4-KINASE; ADENOSINE TRIPHOSPHATE; CATECHOLS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; PHOSPHATIDYLINOSITOL PHOSPHATES; PHOSPHORUS ISOTOPES; SUBSTRATE SPECIFICITY; TYRPHOSTINS;

EID: 84872242924     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0054127     Document Type: Article

References (41)

1. Cantley LC, (2002) The phosphoinositide 3-kinase pathway. Science 296: 1655-1657.
2. Bunney TD, Katan M, (2010) Phosphoinositide signalling in cancer: beyond PI3K and PTEN. Nature Reviews Cancer 10: 342-352.
3. Sasaki AT, Firtel RA, (2006) Regulation of chemotaxis by the orchestrated activation of Ras, PI3K, and TOR. European Journal of Cell Biology 85: 873-895.
4. Vanhaesebroeck B, Stephens L, Hawkins P, (2012) PI3K signalling: the path to discovery and understanding. Nature Reviews Molecular Cell Biology 13: 195-203.
5. McCrea HJ, De Camilli P, (2009) Mutations in Phosphoinositide Metabolizing Enzymes and Human Disease. Physiology 24: 8-16.
6. Odorizzi G, Babst M, Emr SD, (2000) Phosphoinositide signaling and the regulation of membrane trafficking in yeast. Trends in Biochemical Sciences 25: 229-235.
7. Balla T, Szentpetery Z, Kim YJ, (2009) Phosphoinositide Signaling: New Tools and Insights. Physiology 24: 231-244.
8. Sasaki T, Sasaki J, Sakai T, Takasuga S, Suzuki A, (2007) The physiology of Phosphoinositides. Biological & Pharmaceutical Bulletin 30: 1599-1604.
9. Tolias KF, Cantley LC, (1999) Pathways for phosphoinositide synthesis. Chemistry and Physics of Lipids 98: 69-77.
10. Rameh LE, Tolias KF, Duckworth BC, Cantley LC, (1997) A new pathway for synthesis of phosphatidylinositol-4,5-bisphosphate. Nature 390: 192-196.
11. Knight ZA, Shokat KM, (2007) Chemically targeting the PI3K family. Biochemical Society Transactions 35: 245-249.
12. Workman P, Clarke PA, Raynaud FI, van Montfort RLM, (2010) Drugging the PI3 Kinome: From Chemical Tools to Drugs in the Clinic. Cancer Research 70: 2146-2157.
13. Grainger DL, Tavelis C, Ryan AJ, Hinchliffe KA, (2011) Involvement of phosphatidylinositol 5-phosphate in insulin-stimulated glucose uptake in the L6 myotube model of skeletal muscle. Pflugers Archiv-European Journal of Physiology 462: 723-732.
14. Kouchi Z, Fujiwara Y, Yamaguchi H, Nakamura Y, Fukami K, (2011) Phosphatidylinositol 5-phosphate 4-kinase type II beta is required for vitamin D receptor-dependent E-cadherin expression in SW480 cells. Biochemical and Biophysical Research Communications 408: 523-529.
15. Lamia KA, Peroni OD, Kim YB, Rameh LE, Kahn BB, et al. (2004) Increased insulin sensitivity and reduced adiposity in phosphatidylinositol 5-phosphate 4-kinase beta-/- mice. Mol Cell Biol 24: 5080-5087.
16. Schulze H, Korpal M, Hurov J, Kim SW, Zhang JH, et al. (2006) Characterization of the megakaryocyte demarcation membrane system and its role in thrombopoiesis. Blood 107: 3868-3875.
17. Demian DJ, Clugston SL, Foster MM, Rameh L, Sarkes D, et al. (2009) High-throughput, cell-free, liposome-based approach for assessing in vitro activity of lipid kinases. J Biomol Screen 14: 838-844.
18. Burden LM, Rao VD, Murray D, Ghirlando R, Doughman SD, et al. (1999) The flattened face of type II beta phosphatidylinositol phosphate kinase binds acidic phospholipid membranes. Biochemistry 38: 15141-15149.
19. Rao VD, Misra S, Boronenkov IV, Anderson RA, Hurley JH, (1998) Structure of type IIbeta phosphatidylinositol phosphate kinase: a protein kinase fold flattened for interfacial phosphorylation. Cell 94: 829-839.
20. Morris JB, Hinchliffe KA, Ciruela A, Letcher AJ, Irvine RF, (2000) Thrombin stimulation of platelets causes an increase in phosphatidylinositol 5-phosphate revealed by mass assay. FEBS Lett 475: 57-60.
21. Bultsma Y, Keune WJ, Divecha N, (2010) PIP4Kbeta interacts with and modulates nuclear localization of the high-activity PtdIns5P-4-kinase isoform PIP4Kalpha. Biochem J 430: 223-235.
22. Ling LE, Schulz JT, Cantley LC, (1989) Characterization and purification of membrane-associated phosphatidylinositol-4-phosphate kinase from human red blood cells. J Biol Chem 264: 5080-5088.
23. Serunian LA, Auger KR, Cantley LC, (1991) Identification and Quantification of Polyphosphoinositides Produced in Response to Platelet-Derived Growth-Factor Stimulation. Methods in Enzymology 198: 78-87.
24. Yasgar A, Shinn P, Jadhav A, Auld D, Michael S, et al. (2008) Compound Management for Quantitative High-Throughput Screening. JALA 13: 79-89.
25. Inglese J, Auld DS, Jadhav A, Johnson RL, Simeonov A, et al. (2006) Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries. Proc Natl Acad Sci U S A 103: 11473-11478.
26. Auld DS, Southall NT, Jadhav A, Johnson RL, Diller DJ, et al. (2008) Characterization of chemical libraries for luciferase inhibitory activity. J Med Chem 51: 2372-2386.
27. Fuchikami K, Togame H, Sagara A, Satoh T, Gantner F, et al. (2002) A versatile high-throughput screen for inhibitors of lipid kinase activity: development of an immobilized phospholipid plate assay for phosphoinositide 3-kinase gamma. J Biomol Screen 7: 441-450.
28. Lingaraj T, Donovan J, Li Z, Li P, Doucette A, et al. (2008) A high-throughput liposome substrate assay with automated lipid extraction process for PI 3-kinase. J Biomol Screen 13: 906-911.
29. Feng BY, Simeonov A, Jadhav A, Babaoglu K, Inglese J, et al. (2007) A high-throughput screen for aggregation-based inhibition in a large compound library. Journal of Medicinal Chemistry 50: 2385-2390.
30. Knight ZA, Shokat KM, (2005) Features of selective kinase inhibitors. Chem Biol 12: 621-637.
31. Tanega C, Shen M, Mott BT, Thomas CJ, MacArthur R, et al. (2009) Comparison of bioluminescent kinase assays using substrate depletion and product formation. Assay Drug Dev Technol 7: 606-614.
32. Eastwood BJ, Farmen MW, Iversen PW, Craft TJ, Smallwood JK, et al. (2006) The minimum significant ratio: A statistical parameter to characterize the reproducibility of potency estimates from concentration-response assays and estimation by replicate-experiment studies. Journal of Biomolecular Screening 11: 253-261.
33. Vidugiriene J, Zegzouti H, Goueli SA, (2009) Evaluating the Utility of a Bioluminescent ADP-Detecting Assay for Lipid Kinases. Assay and Drug Development Technologies 7: 585-597.
34. Zegzouti H, Zdanovskaia M, Hsiao K, Goueli SA, (2009) ADP-Glo: A Bioluminescent and Homogeneous ADP Monitoring Assay for Kinases. Assay and Drug Development Technologies 7: 560-572.
35. Auld DS, Zhang YQ, Southall NT, Rai G, Landsman M, et al. (2009) A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution. Journal of Medicinal Chemistry 52: 1450-1458.
36. Thorne N, Shen M, Lea WA, Simeonov A, Lovell S, et al. (2012) Firefly luciferase in chemical biology: A compendium of inhibitors, mechanistic evaluation of chemotypes, and suggested use as a reporter. Chemistry and Biology 19: 1060-1072.
37. Strelow J, Dewe W, Iversen P, Brooks H, Radding J (2004) Mechanism of Action assays for Enzymes. In: Sittampalam GS, Gal-Edd N, Arkin M, Auld D, Austin C et al., editors. Assay Guidance Manual. Bethesda, MD: Eli Lilly & Company and the National Center for Advancing Translational Sciences. Available: http://www.ncbi.nlm.nih.gov/books/NBK92001/. Accessed 2012 Nov 1.
38. Blum G, Gazit A, Levitzki A, (2000) Substrate competitive inhibitors of IGF-1 receptor kinase. Biochemistry 39: 15705-15712.
39. Kovalenko M, Ronnstrand L, Heldin CH, Loubtchenkov M, Gazit A, et al. (1997) Phosphorylation site-specific inhibition of platelet-derived growth factor beta-receptor autophosphorylation by the receptor blocking tyrphostin AG1296. Biochemistry 36: 6260-6269.
40. Posner I, Engel M, Gazit A, Levitzki A, (1994) Kinetics of inhibition by tyrphostins of the tyrosine kinase activity of the epidermal growth factor receptor and analysis by a new computer program. Mol Pharmacol 45: 673-683.
41. Michael S, Auld D, Klumpp C, Jadhav A, Zheng W, et al. (2008) A Robotic Platform for Quantitative High-Throughput Screening. Assay and Drug Development Technologies 6: 637-657.