Evaluation of kinase inhibitor selectivity by chemical proteomics

Assay and Drug Development Technologies

Volumn 2, Issue 2, 2004, Pages 215-224

  Daub, Henrik ^a   Godl, Klaus ^a   Brehmer, Dirk ^a   Klebl, Bert ^a   Müller, Gerhard ^a  

^a Axxima Pharmaceuticals AG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

4 (4 FLUOROPHENYL) 2 (4 METHYLSULFINYLPHENYL) 5 (4 PYRIDYL)IMIDAZOLE; ADENOSINE TRIPHOSPHATE; ANTINEOPLASTIC AGENT; ANTIRHEUMATIC AGENT; CYCLIN DEPENDENT KINASE 2; CYCLIN DEPENDENT KINASE INHIBITOR; DORAMAPIMOD; EPIDERMAL GROWTH FACTOR; ERLOTINIB; FLAVOPIRIDOL; GEFITINIB; GLYCOGEN SYNTHASE KINASE 3; IMATINIB; METHOTREXATE; MITOGEN ACTIVATED PROTEIN KINASE; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE P38; N (2 AMINOETHYL) 5 ISOQUINOLINESULFONAMIDE; PHA 539136; PI 51; PROTEIN KINASE; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE INHIBITOR; PROTEOME; PURVALANOL B; PYRROLOPYRIMIDINE DERIVATIVE; QUINAZOLINE DERIVATIVE; SB 242234; SB 242235; TWS 119; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANALYTIC METHOD; BINDING AFFINITY; BINDING SITE; CLINICAL TRIAL; DRUG CLASSIFICATION; DRUG EFFICACY; DRUG INDICATION; DRUG MECHANISM; DRUG RESEARCH; DRUG SCREENING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG TARGETING; ELECTROPHORETIC MOBILITY; ENZYME PURIFICATION; GENETIC CONSERVATION; HUMAN; MASS SPECTROMETRY; MOLECULAR SIZE; NONHUMAN; PEPTIDE MAPPING; PROTEOMICS; REVIEW; SENSITIVITY ANALYSIS; TIME; TREATMENT OUTCOME; VALIDATION PROCESS;

EID: 2442543003     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/154065804323056558     Document Type: Review

References (35)

1. Cohen P: Protein kinases - the major drug targets of the twenty-first century? Nat Rev Drug Discov 2002;1:309-315.
2. Dancey J, Sausville EA: Issues and progress with protein kinase inhibitors for cancer treatment. Nat Rev Drug Discov 2003;2:296-313.
3. Kumar S, Boehm J, Lee JC: p38 MAP kinases: key signalling molecules as therapeutic targets for inflammatory diseases. Nat Rev Drug Discov 2003;2:717-726.
4. Fischer OM, Streit S, Hart S, Ullrich A: Beyond Herceptin and Gleevec. Curr Opin Chem Biol 2003;7:490-495.
5. 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.
6. Muhsin M, Graham J, Kirkpatrick P: Gefitinib. Nat Rev Drug Discov 2003;2:515-516.
7. de Jong FA, Verweij J: Role of imatinib mesylate (Gleevec/Glivec) in gastrointestinal stromal tumors. Expert Rev Anticancer Ther 2003;3:757-766.
8. George D: Targeting PDGF receptors in cancer - rationales and proof of concept clinical trials. Adv Exp Med Biol 2003;532:141-151.
9. Grunwald V, Hidalgo M: Development of the epidermal growth factor receptor inhibitor Tarceva (OSI-774). Adv Exp Med Biol 2003;532:235-246.
10. Normanno N, Bianco C, De Luca A, Maiello MR, Salomon DS: Target-based agents against ErbB receptors and their ligands: a novel approach to cancer treatment. Endocr Relat Cancer 2003;10:1-21.
11. Senderowicz AM: Small-molecule cyclin-dependent kinase modulators. Oncogene 2003;22:6609-6620.
12. Blagosklonny MV, Darzynkiewicz Z: Why Iressa failed: toward novel use of kinase inhibitors (outlook). Cancer Biol Ther 2003;2:137-140.
13. Cotten M, Stegmueller K, Eickhoff J, Hanke M, Herzberger K, Herget T, Choidas A, Daub H, Godl K: Exploiting features of adenovirus replication to support mammalian kinase production. Nucleic Acids Res 2003;31:e128.
14. Davies SP, Reddy H, Caivano M, Cohen P: Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J 2000; 351:95-105.
15. Bain J, McLauchlan H, Elliott M, Cohen P: The specificities of protein kinase inhibitors: an update. Biochem J 2003; 371:199-204.
16. Manning G, Whyte DB, Martinez R, Hunter T, Sudarsanam S: The protein kinase complement of the human genome. Science 2002;298:1912-1934.
17. Sche PP, McKenzie KM, White JD, Austin DJ: Display cloning: functional identification of natural product receptors using cDNA-phage display. Chem Biol 1999;6:707-716.
18. Becker F, Murthi K, Smith C, Come J, Costa-Roldán N, Kaufmann C, Hanke U, Degenhart C, Baumann S, Wallner W, et al.: A three-hybrid approach to scanning the proteome for targets of small molecule kinase inhibitors. Chem Biol 2004;11:211-223.
19. Knockaert M, Gray N, Damiens E, Chang YT, Grellier P, Grant K, Fergusson D, Mottram J, Soete M, Dubremetz JF, Le Roch K, Doerig C, Schultz P, Meijer L: Intracellular targets of cyclin-dependent kinase inhibitors: identification by affinity chromatography using immobilised inhibitors, Chem Biol 2000;7:411-422.
20. 2+-activated, phospholipid-dependent and other protein kinases. J Biol Chem 1985; 260:2922-2925.
21. Engh RA, Girod A, Kinzel V, Huber R, Bossemeyer D: Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity. J Biol Chem 1996;271:26157-26164.
22. Schnier JB, Kaur G, Kaiser A, Stinson SF, Sausville EA, Gardner J, Nishi K, Bradbury EM, Senderowiez AM: Identification of cytosolic aldehyde dehydrogenase 1 from nonsmall cell lung carcinomas as a flavopiridol-binding protein. FEBS Lett 1999;454:100-104.
23. Kaiser A, Nishi K, Gorin FA, Walsh DA, Bradbury EM, Schnier JB: The cyclin-dependent kinase (CDK) inhibitor flavopiridol inhibits glycogen phosphorylase. Arch Biochem Biophys 2001;386:179-187.
24. De Azevedo WF Jr, Mueller-Dieckmann HJ, Schulze-Gahmen U, Worland PJ, Sausville E, Kim SH: Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2, a cell cycle kinase. Proc Natl Acad Sci U S A 1996;93:2735-2740.
25. Knockaert M, Wieking K, Schmitt S, Leost M, Grant KM, Mottram JC, Kunick C, Meijer L: Intracellular targets of paullones. Identification following affinity purification on immobilized inhibitor. J Biol Chem 2002;277:25493-25501.
26. Wan Y, Hur W, Cho CY, Liu Y, Adrian FJ, Lozach O, Bach S, Mayer T, Fabbro D, Meijer L, Gray NS: Synthesis and target identification of hymenialdisine analogs. Chem Biol 2004;11:247-259.
27. Lolli G, Thaler F, Valsasina B, Roletto F, Knapp S, Uggeri M, Bachi A, Matafora V, Storici P, Stewart A, Kalisz HM, Isacchi A: Inhibitor affinity chromatography: profiling the specific reactivity of the proteome with immobilized molecules. Proteomics 2003;3:1287-1298.
28. Ding S, Wu TY, Brinker A, Peters EC, Hur W, Gray NS, Schultz PG: Synthetic small molecules that control stem cell fate. Proc Natl Acad Sci USA 2003;100:7632-7637.
29. Godl K, Wissing J, Kurtenbach A, Habenberger P, Blencke S, Gutbrod H, Salassidis K, Stein-Gerlach M, Missio A, Cotten M, Daub H: An efficient proteomics method to identify the cellular targets of protein kinase inhibitors. Proc Natl Acad Sci U S A 2003;100:15434-15439.
30. Tong L, Pav S, White DM, Rogers S, Crane KM, Cywin CL, Brown ML, Pargellis CA: A highly specific inhibitor of human p38 MAP kinase binds in the ATP pocket. Nat Struct Biol 1997;4:311-316.
31. Godl K, Daub H: Proteomic analysis of kinase inhibitor selectivity and function. Cell Cycle 2004;3:393-395.
32. Brehmer D, Godl K, Zech B, Wissing J, Daub H: Proteome-wide identification of cellular targets affected by bisindolylmaleimide-type protein kinase C inhibitors. Mol Cell Proteomics 2004;[Epub ahead of print].
33. Haystead CM, Gregory P, Sturgill TW, Haystead TA: Gamma-phosphate-linked ATP-Sepharose for the affinity purification of protein kinases. Rapid purification to homogeneity of skeletal muscle mitogen-activated protein kinase kinase. Eur J Biochem 1993;214:459-467.
34. Graves PR, Kwiek JJ, Fadden P, Ray R, Hardeman K, Coley AM, Foley AM, Haystead TA: Discovery of novel targets of quinoline drugs in the human purine binding proteome. Mol Pharmacol 2002;62:1364-1372.
35. Müller G: Medicinal chemistry of target family-directed masterkeys. Drug Discov Today 2003;8:681-691.