Solid-phase immunoassays in mechanism-based drug discovery: Their application in the development of inhibitors of the molecular chaperone heat-shock protein 90

Assay and Drug Development Technologies

Volumn 3, Issue 3, 2005, Pages 273-285

  Hardcastle, Anthea ^a   Boxall, Kathy ^a   Richards, Juliet ^a   Tomlin, Peter ^a   Sharp, Swee ^a   Clarke, Paul ^a   Workman, Paul ^a   Aherne, Wynne ^a  

^a INSTITUTE OF CANCER RESEARCH   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

17 ALLYLAMINO 17 DEMETHOXYGELDANAMYCIN; ADENOSINE TRIPHOSPHATASE; ANTINEOPLASTIC AGENT; CCT 016391; CCT 018159; CHAPERONE; EPIDERMAL GROWTH FACTOR RECEPTOR 2; ETOPOSIDE; GELDANAMYCIN; HEAT SHOCK PROTEIN 70; HEAT SHOCK PROTEIN 90; METHOTREXATE; MITOGEN ACTIVATED PROTEIN KINASE; PACLITAXEL; PROTEIN INHIBITOR; RAF PROTEIN; UNCLASSIFIED DRUG;

ANGIOGENESIS; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CELL ASSAY; CELL DIFFERENTIATION; CELL MOTILITY; CELL PROLIFERATION; CELL SURVIVAL; CONTROLLED STUDY; DRUG DETERMINATION; DRUG MECHANISM; DRUG RESEARCH; DRUG SCREENING; DRUG SYNTHESIS; DRUG TARGETING; ENZYME LINKED IMMUNOSORBENT ASSAY; EXPERIMENTAL NEOPLASM; FLOW CYTOMETRY; FLUORESCENCE ANALYSIS; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IMMUNOASSAY; IMMUNOHISTOCHEMISTRY; INTERMETHOD COMPARISON; METASTASIS; MOLECULAR DYNAMICS; MOUSE; NONHUMAN; PROTEIN CONFORMATION; PROTEIN FUNCTION; PROTEIN STABILITY; SIGNAL TRANSDUCTION; SOLID PHASE IMMUNOASSAY; TIME; VALIDATION PROCESS; WESTERN BLOTTING;

ANIMALS; BENZOQUINONES; BLOTTING, WESTERN; CARRIER PROTEINS; CELL EXTRACTS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; EIF-2 KINASE; ENZYME INHIBITORS; HCT116 CELLS; HETEROCYCLIC COMPOUNDS, 2-RING; HSP70 HEAT-SHOCK PROTEINS; HSP90 HEAT-SHOCK PROTEINS; HT29 CELLS; HUMANS; IMMUNOASSAY; LACTAMS, MACROCYCLIC; LYMPHOCYTES; MICE; NEOPLASM TRANSPLANTATION; PROTO-ONCOGENE PROTEINS C-RAF; PYRAZOLES; QUINONES; RIFABUTIN; TECHNOLOGY, PHARMACEUTICAL; TRANSPLANTATION, HETEROLOGOUS;

EID: 23144445834     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2005.3.273     Document Type: Article

References (47)

1. Maloney A, Workman P: HSP90 as a new therapeutic target for cancer therapy: the story unfolds. Expert Opin Biol Ther 2002;2:3-24.
2. Neckers L: Hsp90 inhibitors as novel cancer chemotherapeutic agents. Trends Mol Med 2002;8(Suppl):S55-S61.
3. Isaacs JS, Xu W, Neckers L: Heat shock protein 90 as a molecular target for cancer therapeutics. Cancer Cell 2003;3:213-217.
4. Prodromou C, Roe SM, O'Brien R, Ladbury JE, Piper PW, Pearl LH: Identification and structural characterization of the ATP/ADP-binding site in the Hsp90 molecular chaperone. Cell 1997;90:65-75.
5. Panaretou B, Prodromou C, Roe SM, O'Brien R, Ladbury JE, Piper PW, Pearl LH: ATP binding and hydrolysis are essential to the function of the Hsp90 molecular chaperone in vivo. EMBO J 1998;17:4829-4836.
6. Workman P: Altered states: selectively drugging the Hsp90 cancer chaperone. Trends Mol Med 2004;10:47-51.
7. Banerji U, Judson I, Workman P: The clinical applications of heat shock protein inhibitors in cancer - present and future. Curr Cancer Drug Targets 2003;3:385-390.
8. Blagosklonny MV: Hsp-90-associated oncoproteins: multiple targets of geldanamycin and its analogs. Leukaemia 2002; 16:455-462.
9. Kelland LR, Sharp SY, Rogers PM, Myers TG, Workman P: DT-Diaphorase expression and tumor cell sensitivity to 17-allylamino, 17-demethoxygeldanamycin, an inhibitor of heat shock protein 90. J Natl Cancer Inst 1999;91: 1940-1949.
10. Clarke PA, Hostein I, Banerji U, Stefano FD, Maloney A, Walton M, Judson I, Workman P: Gene expression profiling of human colon cancer cells following inhibition of signal transduction by 17-allylamino-17-demethoxygeldanamycin, an inhibitor of the Hsp90 molecular chaperone. Oncogene 2000;19:4125-4133.
11. Workman P: Combinational attack on multistep oncogenesis by inhibiting Hsp90 molecular chaperone. Cancer Lett 2004; 206:149-157.
12. Hanahan D, Weinberg RA: The hallmarks of cancer. Cell 2000;100:57-70.
13. Kamal A, Thao L, Sensintaffar J, Zhang L, Boehm MF, Fritz LC, Burrows FJ: A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors. Nature 2003;425:407-410.
14. Weinstein IB: Addiction to oncogenes - the Achilles heal of cancer. Science 2002;297:63-64.
15. Dymock BW, Drysdale MJ, McDonald E, Workman P: Inhibitors of Hsp90 and other chaperones for the treatment of cancer. Expert Opin Ther Pat 2004;14:837-847.
16. Chiosis G, Huezo H, Rosen N, Mimnaugh E, Whitesell L, Neckers L: 17AAG: low target binding affinity and potent cell activity - finding an explanation. Mol Cancer Ther 1999;2:123-129.
17. Vilenchik M, Solit D, Basso A, Huezo H, Lucas B, He H, Rosen N, Spampinato C, Modrich P, Chiosis G: Targeting wide-range oncogenic transformation via PU24FC1, a specific inhibitor of tumor Hsp90. Chem Biol 2004;11: 787-797.
18. Roe SM, Prodromou C, O'Brien R, Ladbury JE, Piper PW, Pearl LH: Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin. J Med Chem 1999;42:260-266.
19. Stebbins CE, Russo AA, Schneider C, Rosen N, Hartl FU, Pavletich NP: Crystal structure of an Hsp90-geldanamycin complex: targeting of a protein chaperone by an antitumor agent. Cell 1997;89:239-250.
20. Wright L, Barril X, Dymock B, Sheridan L, Surgenor A, Beswick M, Drysdale M, Collier A, Massey A, Davies N, FinkA, Fromont C, Aherne W, Boxall K, Sharp S, Workman P, Hubbard RE: Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms. Chem Biol 2004;11:775-785.
21. Hostein I, Robertson D, DiStefano F, Workman P, Clarke PA: Inhibition of signal transduction by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin results in cytostasis and apoptosis. Cancer Res 2001;61:4003-4009.
22. Whitesell L, Mimnaugh EG, De Costa B, Myers CE, Neckers LM: Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation. Proc Natl Acad Sci USA 1994;91: 8324-8328.
23. Banerji U, O'Donnell A, Scurr M, Benson C, Brock C, Hanwell J, Stapleton S, Raynaud F, Simmons L, Turner A, Walton M, Workman P, Judson IA: Pharmacokinetically (PK) pharmacodynamically (PD) driven phase 1 trial of the Hsp90 molecular chaperone inhibitor 17-(allylamino)-17 demethoxygeldanamycin (17AAG) [abstract]. Proc Am Assoc Cancer Res 2002;43:1352.
24. Supko JG, Hickman MR, Grever MR, Malspeis L: Preclinical pharmacologic evaluation of geldanamycin as an antitumour agent [abstract]. Cancer Chemother Pharmacol 1995;36:305.
25. Sausville EA, Tomaszewski JE, Ivy P: Clinical development of 17-allylamino, 17-demethoxygeldanamycin. Curr Cancer Drug Targets 2003;3:377-383.
26. Bagatell R, Whitesell L: Altered Hsp90 function in cancer: a unique therapeutic opportunity. Mol Cancer Ther 2004;8:1021-1030.
27. Egorin MJ, Zuhowski EG, Rosen DM, Sentz DL, Covey JM, Eiseman JL: Plasma pharmacokinetics and tissue distribution of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) in CD2F1 mice1. Cancer Chemother Pharmacol 2001;47:291-302.
28. Rowlands MG, Newbatt YM, Prodromou C, Pearl LH, Workman P, Aherne W: High-throughput screening assay for inhibitors of heat-shock protein 90 ATPase activity. Anal Biochem 2004;327:176-183.
29. Aherne W, Malony A, Sharp S, Clarke P, Walton M, Hardcastle A, Boxall K, Richards J, Rowlands M, Newbatt Y, Raynaud F, Smith N, Nutley B, McDonald E, James K, Cheung J, Matthews T, Roe M, Prodromou, Pearl L, Workman P: Discovery of a novel inhibitor of the Hsp90 molecular chaperone [abstract 4002]. Proc Am Assoc Cancer Res 2003;44:799.
30. Cheung KJ, Matthews TP, James K, Rowlands MG, Boxall KJ, Sharp SY, Maloney A, Roe SM, Prodromou C, Pearl LH, Aherne GW, McDonald E, Workman P. The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors. Bioorg Med Chem Lett 2005 (in press).
31. Stockwell BR, Haggarty SJ, Schreiber SL: High-throughput screening of small molecules in miniaturized mammalian cell-based assays involving post-translational modifications. Chem Biol 1996; 6:71-83.
32. Mayer TU, Kapoor TM, Haggarty SJ, King RW, Schreiber SL, Mitchison TJ: Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen. Science 1999;286:971-974.
33. Haggarty SJ, Koeller KM, Wong JC, Grozinger CM, Schreiber SL: Domain-selective small-molecule inhibitor of histone deacetylase 6 (HDAC6)-mediated tubulin deacetylation. Proc Natl Acad Sci U S A 2003;100: 4389-4394.
34. Blaskovich MA, Sun J, Cantor A, Turkson J, Jove R, Sebti SM: Discovery of JSI-124 (cucurbitacin I), a selective Janus kinase/signal transducer and activator of transcription 3 signaling pathway inhibitor with potent antitumor activity against human and murine cancer cells in mice. Cancer Res 2003;63:270-1279.
35. Barrie SE, Eno-Amooquaye E, Hardcastle A, Platt G, Richards J, Bedford D, Workman P, Aherne W, Mittnacht S, Garrett MD: High-throughput screening for the identification of small-molecule inhibitors of retinoblastoma protein phosphorylation in cells. Anal Biochem 2003;320: 66-74.
36. Skehan P, Storeng R, Scudiero D, Monks A, McMahon J, Vistica D, Warren JT, Bokesch H, Kenney S, Boyd MR: New colorimetric cytotoxicity assay for anti-cancer drug screening. J Natl Cancer Inst 1990;82:1107-1118.
37. Workman P, Twentyman P, Balkwill F, Balmain A, Chaplin D, Double J, Embleton J, Newell D, Ramond R, Stables J, Stephens T: United Kingdom Co-ordinating Committee on Cancer Research (UKCCCR) guidelines for the welfare of animals in experimental neoplasia [second edition]. Br J Cancer 1998;77:1-10.
38. Morimoto RI: Regulation of the heat shock transcriptional response: cross talk between a family of heat shock factors, molecular chaperones, and negative regulators. Genes Dev 1998;12:3788-3796.
39. Huezo H, Vilenchik M, Rosen N, Chiosis G: Microtiter cell-based assay for detection of agents that alter cellular levels of Her2 and EGFR. Chem Biol 2003;10:629-634.
40. Aherne GW, Hardcastle A, Ward E, Dobinson D, Crompton T, Valenti M, Brunton L, Jackman AL: Pharmacokinetic/pharmacodynamic study of ZD9331, a nonpolyglutamatable inhibitor of thymidylate synthase, in a murine model following two curative administration schedules. Clin Cancer Res 2001;7:2923-2930.
41. Workman P: Challenges of PK/PD measurements in modern drug development. Eur J Cancer 2002;38:2189-2193.
42. Gelmon KA, Eisenhauer EA, Harris AL, Ratain MJ, Workman P: Anticancer agents targeting signalling molecules and cancer cell environment: challenges for drug development? J Natl Cancer Inst 1999;91:1281-1287.
43. Workman P: Auditing the pharmacological accounts for Hsp90 molecular chaperone inhibitors: unfolding the relationship between pharmacokinetics and pharmacodynamics. Mol Cancer Ther 2003;2:131-138.
44. Chow S, Patel H, Hedley DW: Measurement of MAP kinase activation by flow cytometry using phospho-specific antibodies to MEK and ERK: potential for pharmacodynamic monitoring of signal transduction inhibitors. Cytometry 2001;46:72-78.
45. Parulekar WR, Eisenbauer EA: Phase 1 trial design for solid tumour studies of targeted, non-cytotoxic agents: theory and practice. J Natl Cancer Inst 2004;96:990-997.
46. Harrington EA, Bebbington D, Moore J, Rasmussen RK, Ajose-Adeogun AO, Nakayama T, Graham JA, Demur C, Hercend T, Diu-Hercend A, Su M, Golec JM, Miller KM: VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumour growth in vivo. Nat Med 2004;10:262-267.
47. Directive 2001/20/EC of the European Parliament and of the Council of 4th April 2001. Office for Official Publications of the European Communities, Luxembourg.