메뉴 건너뛰기




Volumn 3, Issue 6, 2008, Pages 607-621

The challenge of selecting protein kinase assays for lead discovery optimization

Author keywords

Drug discovery; Drug profiling; Drug screening; ELISA; Florescence resonance energy transfer; Fluorescence polarization; Kinase assay; Kinase profiling; Luminescence assays; Radioisotope filtration binding assay; Time resolved fluorescence resonance energy transfer

Indexed keywords

BMS 354285; CAPECITABINE; DASATINIB; ERLOTINIB; GEFITINIB; IMATINIB; LAPATINIB; NILOTINIB; PROTEIN KINASE; PROTEIN KINASE INHIBITOR; REAGENT; SORAFENIB; ST 571; SUNITINIB; TEMSIROLIMUS;

EID: 45949106612     PISSN: 17460441     EISSN: None     Source Type: Journal    
DOI: 10.1517/17460441.3.6.607     Document Type: Review
Times cited : (171)

References (53)
  • 1
    • 0037032835 scopus 로고    scopus 로고
    • Protein kinase complement of the human genome
    • Manning G, Whyte DB, Martinez R, et al. Protein kinase complement of the human genome. Sciences 2002;298:1912-34
    • (2002) Sciences , vol.298 , pp. 1912-1934
    • Manning, G.1    Whyte, D.B.2    Martinez, R.3
  • 3
    • 0036527429 scopus 로고    scopus 로고
    • Protein kinases: The major drug targets of the twenty-first century?
    • Cohen P. Protein kinases: the major drug targets of the twenty-first century? Nat Rev Drug Discov 2002;1:309-15
    • (2002) Nat Rev Drug Discov , vol.1 , pp. 309-315
    • Cohen, P.1
  • 5
    • 45949107444 scopus 로고    scopus 로고
    • Fox S, editor. High-throughput screening. new strategies and technologies. Moraga, CA: High-Tech Business Decisions; 2002
    • Fox S, editor. High-throughput screening. new strategies and technologies. Moraga, CA: High-Tech Business Decisions; 2002
  • 6
    • 0037107007 scopus 로고    scopus 로고
    • Novel detection stranoes for drug discovery
    • Hemmila IA, Hurskainen P. Novel detection stranoes for drug discovery. Drug Discov Today 2002;7:150-6
    • (2002) Drug Discov Today , vol.7 , pp. 150-156
    • Hemmila, I.A.1    Hurskainen, P.2
  • 7
    • 33646148263 scopus 로고    scopus 로고
    • Quantitative methods for the analysis of protein phosphorylation in drug development
    • Olive DM. Quantitative methods for the analysis of protein phosphorylation in drug development. Expert Rev Proteomics 2004;1:327-41
    • (2004) Expert Rev Proteomics , vol.1 , pp. 327-341
    • Olive, D.M.1
  • 8
    • 45949097277 scopus 로고    scopus 로고
    • Comely J. Kinase screening and profiling - spoilt for choice. Available from: http://www.ddw-online.com/data/pdfs/2006kinase%20screening.pdf
    • Comely J. Kinase screening and profiling - spoilt for choice. Available from: http://www.ddw-online.com/data/pdfs/2006kinase%20screening.pdf
  • 9
    • 0035991330 scopus 로고    scopus 로고
    • Comparison of assays technologies for a tyrosine kinase assay generates different results in high throughput screening
    • Sills MA, Weiss D, Pham Q, et al. Comparison of assays technologies for a tyrosine kinase assay generates different results in high throughput screening. J Biomol Screen 2002;7:191-9
    • (2002) J Biomol Screen , vol.7 , pp. 191-199
    • Sills, M.A.1    Weiss, D.2    Pham, Q.3
  • 10
    • 0242483911 scopus 로고    scopus 로고
    • Comparison of assay technologies for a nuclear receptor assay screen reveals differences in the sets of identified functional antagonists
    • Wu X, Glickman JF, Bowen BR, Sills MA. Comparison of assay technologies for a nuclear receptor assay screen reveals differences in the sets of identified functional antagonists. J Biomol Screen 2003;8:381-92
    • (2003) J Biomol Screen , vol.8 , pp. 381-392
    • Wu, X.1    Glickman, J.F.2    Bowen, B.R.3    Sills, M.A.4
  • 11
    • 2442482366 scopus 로고    scopus 로고
    • Miniaturization, ultra-high throughput screening of tyrosine kinase using homogeneous, competitive fluorescence immunoassays
    • Beasley JR, McCoy PM, Watker TL, Dunn DA. Miniaturization, ultra-high throughput screening of tyrosine kinase using homogeneous, competitive fluorescence immunoassays. Assay Drug Dev Technol 2004;2:141-52
    • (2004) Assay Drug Dev Technol , vol.2 , pp. 141-152
    • Beasley, J.R.1    McCoy, P.M.2    Watker, T.L.3    Dunn, D.A.4
  • 12
    • 24944484421 scopus 로고    scopus 로고
    • Probing the primary screening efficiency by multiple replicate testing: A quantitative analysis of hit confirmation and false screening results of a biochemical assay
    • Zhang JH, Wu X, Sills MA. Probing the primary screening efficiency by multiple replicate testing: a quantitative analysis of hit confirmation and false screening results of a biochemical assay. J Biomol Screen 2005;10:695-704
    • (2005) J Biomol Screen , vol.10 , pp. 695-704
    • Zhang, J.H.1    Wu, X.2    Sills, M.A.3
  • 13
    • 24944561210 scopus 로고    scopus 로고
    • Further comparison of primary hit identification by different assay technologies and effects of assay measurement variability
    • Wu X, Sills MA, Zhang JH. Further comparison of primary hit identification by different assay technologies and effects of assay measurement variability. J Biomol Screen 2005;9:581-9
    • (2005) J Biomol Screen , vol.9 , pp. 581-589
    • Wu, X.1    Sills, M.A.2    Zhang, J.H.3
  • 14
    • 33748154598 scopus 로고    scopus 로고
    • Assay concordance between SPA and TR-FRET in high-throughput screening
    • Ahsen OV, Schmidt A, Klotz M, Parczyk K. Assay concordance between SPA and TR-FRET in high-throughput screening. J Biomol Screen 2006;11:606-16
    • (2006) J Biomol Screen , vol.11 , pp. 606-616
    • Ahsen, O.V.1    Schmidt, A.2    Klotz, M.3    Parczyk, K.4
  • 15
    • 34249912663 scopus 로고    scopus 로고
    • High-throughput screening by mass spectrometry: Comparison with the scintillation proximity assay with a focused-file screen of AKT1/PKB
    • Quercia AK, Lamarr WA, Myung J, et al. High-throughput screening by mass spectrometry: comparison with the scintillation proximity assay with a focused-file screen of AKT1/PKB. J Biomol Screen 2007;12:473-80
    • (2007) J Biomol Screen , vol.12 , pp. 473-480
    • Quercia, A.K.1    Lamarr, W.A.2    Myung, J.3
  • 16
    • 33846865304 scopus 로고    scopus 로고
    • Three mechanistically distinct kinase assay compared: Measurement of intrinsic ATPase activity identified the most comprehensives set of ITK inhibitors
    • Kashem MA, Nelson RM, Yingling JD, et al. Three mechanistically distinct kinase assay compared: measurement of intrinsic ATPase activity identified the most comprehensives set of ITK inhibitors. J Biomol Screen 2007;12:70-83
    • (2007) J Biomol Screen , vol.12 , pp. 70-83
    • Kashem, M.A.1    Nelson, R.M.2    Yingling, J.D.3
  • 17
    • 45949083748 scopus 로고    scopus 로고
    • Available from
    • Available from: http://reactionbiology.com/pages/kinase.htm
  • 18
    • 45949093659 scopus 로고    scopus 로고
    • Available from
    • Available from: http://www.millipore.com/drugdiscovery/dd2/kinasetarget
  • 19
    • 45949094158 scopus 로고    scopus 로고
    • Available from
    • Available from: http://www.rcxg.mdlc.com/aptrix./upp01077.nsf/Content/ Products?OpenDocument&parentid=658513&moduleid=166937
  • 20
    • 45949104385 scopus 로고    scopus 로고
    • Available from
    • Available from: http://las.perkinelmer.com/Catalog/ default.htm?CategoryID=Scintillation+Proximity+Assay+%5BSPA%5D
  • 21
    • 45949097429 scopus 로고    scopus 로고
    • Available from
    • Available from: http://www.proqinase.com/pages/service/p2_1_4.html
  • 22
    • 33744912806 scopus 로고    scopus 로고
    • Charter NW, Kauffman L, Singh R, Eglen RM. A generic, homogenous method for measuring kinase and inhibitor activity via adenosine 5′-diphosphate accumulation. J Biomol Screen 2006;11(4):390-9 [Epub 28 Apr 2006]
    • Charter NW, Kauffman L, Singh R, Eglen RM. A generic, homogenous method for measuring kinase and inhibitor activity via adenosine 5′-diphosphate accumulation. J Biomol Screen 2006;11(4):390-9 [Epub 28 Apr 2006]
  • 23
    • 45949102619 scopus 로고    scopus 로고
    • Available from
    • Available from: http://www.promega.com/paguide/chap7.pdf
  • 24
    • 20544440319 scopus 로고    scopus 로고
    • Nanoliter homogeneous ultra-high throughput screening microarray for lead discoveries and IC50 profiling
    • Ma H, Horiuchi KY, Wang Y, et al. Nanoliter homogeneous ultra-high throughput screening microarray for lead discoveries and IC50 profiling. Assay Drug Dev Technol 2005;3;177-87
    • (2005) Assay Drug Dev Technol , vol.3 , pp. 177-187
    • Ma, H.1    Horiuchi, K.Y.2    Wang, Y.3
  • 25
    • 33746257209 scopus 로고    scopus 로고
    • The evolution of Phosphatidylinositol 3-kinases as regulators of growth and metabolism
    • Engelman JA, Luo J, Candey LC. The evolution of Phosphatidylinositol 3-kinases as regulators of growth and metabolism. Nat Rev 2006;7:606-19
    • (2006) Nat Rev , vol.7 , pp. 606-619
    • Engelman, J.A.1    Luo, J.2    Candey, L.C.3
  • 26
    • 45949109758 scopus 로고    scopus 로고
    • Available from
    • Available from: http://www.invitrogen.com/downloads/ Redder_formated_poster.pdf
  • 27
    • 45949101131 scopus 로고    scopus 로고
    • Available from
    • Available from: http://www.invitrogen.com/ content.cfm?pageid=10413#selection
  • 28
    • 45949085428 scopus 로고    scopus 로고
    • Available from
    • Available from: http://www.invitrogen.com/content.cfm?pageid=9866
  • 29
    • 32844464076 scopus 로고    scopus 로고
    • Microarrays for the functional analysis of the chemical kinase interactome
    • Horiuchi KY, Wang Y, Diamond SL, Ma H. Microarrays for the functional analysis of the chemical kinase interactome. J Biomol Screen 2006;11:48-56
    • (2006) J Biomol Screen , vol.11 , pp. 48-56
    • Horiuchi, K.Y.1    Wang, Y.2    Diamond, S.L.3    Ma, H.4
  • 30
    • 33745220936 scopus 로고    scopus 로고
    • Chemical microarray: A new tool for drug screening and discovery
    • Ma H, Horiuchi KY. Chemical microarray: a new tool for drug screening and discovery. Drug Discov Today 2006;11:661-8
    • (2006) Drug Discov Today , vol.11 , pp. 661-668
    • Ma, H.1    Horiuchi, K.Y.2
  • 31
    • 45949109613 scopus 로고    scopus 로고
    • Available from
    • Available from: http://www.carnabio.com/english/product/assay.html
  • 32
    • 34147210060 scopus 로고    scopus 로고
    • Bioluminescent assays for high-throughput screening
    • Fan F, Wood KV. Bioluminescent assays for high-throughput screening. Assay Drug Dev Technol 2007;5:127-36
    • (2007) Assay Drug Dev Technol , vol.5 , pp. 127-136
    • Fan, F.1    Wood, K.V.2
  • 33
    • 45949106107 scopus 로고    scopus 로고
    • Available from
    • Available from: http://www.nanostream.com/support/downloads.html
  • 34
    • 2442503250 scopus 로고    scopus 로고
    • Comparison of on-chip and off-chip microfluidic kinase assay formats
    • Dunne J, Reardon H, Trinh V, et al. Comparison of on-chip and off-chip microfluidic kinase assay formats. Assay Drug Dev Technol 2004;2:121-9
    • (2004) Assay Drug Dev Technol , vol.2 , pp. 121-129
    • Dunne, J.1    Reardon, H.2    Trinh, V.3
  • 35
    • 45949106991 scopus 로고    scopus 로고
    • Available from
    • Available from: http://www.ambitbio.com/technology/
  • 36
    • 19744365702 scopus 로고    scopus 로고
    • A small molecule-kinase interaction map for clinical kinase inhibitors
    • Fabian MA, Biggs WH III, Treiber DK, et al. A small molecule-kinase interaction map for clinical kinase inhibitors. Nat Biotechnol 2005;23:329-36
    • (2005) Nat Biotechnol , vol.23 , pp. 329-336
    • Fabian, M.A.1    Biggs III, W.H.2    Treiber, D.K.3
  • 37
    • 38049018155 scopus 로고    scopus 로고
    • A quantitative analysis of kinase inhibitors selectivity
    • Karaman MW, Herrgard S, Treiber DK, et al. A quantitative analysis of kinase inhibitors selectivity. Nat Biotechnol 2007;26:127-32
    • (2007) Nat Biotechnol , vol.26 , pp. 127-132
    • Karaman, M.W.1    Herrgard, S.2    Treiber, D.K.3
  • 38
    • 0141768651 scopus 로고    scopus 로고
    • A high-throughput, nonisotopic, competitive binding assay For kinases using nonselective inhibitor probes (ED-NSIP™)
    • Vainshtein I, Silveria S, Kaul P, et al. A high-throughput, nonisotopic, competitive binding assay For kinases using nonselective inhibitor probes (ED-NSIP™). J Biomol Screen 2002;6:497-504
    • (2002) J Biomol Screen , vol.6 , pp. 497-504
    • Vainshtein, I.1    Silveria, S.2    Kaul, P.3
  • 39
    • 45949094621 scopus 로고    scopus 로고
    • Fluorescence polarization and time-resolved fluorescence resonance energy transfer techniques for PI3K assays
    • Ana Cecilia Roque, editor, The Humana Press, Inc
    • Horiuchi KY, Ma H. Fluorescence polarization and time-resolved fluorescence resonance energy transfer techniques for PI3K assays. In: Ana Cecilia Roque, editor, Ligand-macromolecule interactions in drug discovery. The Humana Press, Inc.; 2008
    • (2008) Ligand-macromolecule interactions in drug discovery
    • Horiuchi, K.Y.1    Ma, H.2
  • 40
    • 2142830967 scopus 로고    scopus 로고
    • Data concordance from a comparison between filter binding and fluorescence polarization assay formats for identification of ROCK-II inhibitors
    • Hubert CL, Sherling SE, Johnston PA, Stancato LF. Data concordance from a comparison between filter binding and fluorescence polarization assay formats for identification of ROCK-II inhibitors. J Biomol Screen 2003;8:399-409
    • (2003) J Biomol Screen , vol.8 , pp. 399-409
    • Hubert, C.L.1    Sherling, S.E.2    Johnston, P.A.3    Stancato, L.F.4
  • 41
    • 27944511539 scopus 로고    scopus 로고
    • Molecular-kinase interaction map, Opinion and comment section
    • Buolamwini JK, Kamath S. Molecular-kinase interaction map, Opinion and comment section. Nat Biotechnol 2005;11:1346-8
    • (2005) Nat Biotechnol , vol.11 , pp. 1346-1348
    • Buolamwini, J.K.1    Kamath, S.2
  • 42
    • 10744233716 scopus 로고    scopus 로고
    • Imatinib compared with interferon and low-dose cytarabine for newly diagnosed chronic-phase chronic myeloid leukemia
    • O'Brien SG, Guilhot F, Larson RA, et al. Imatinib compared with interferon and low-dose cytarabine for newly diagnosed chronic-phase chronic myeloid leukemia. N Engl J Med 2003;348:994-1004
    • (2003) N Engl J Med , vol.348 , pp. 994-1004
    • O'Brien, S.G.1    Guilhot, F.2    Larson, R.A.3
  • 43
    • 0035810148 scopus 로고    scopus 로고
    • Effect of the tyrosine kinase inhibitor STI571 in a patient with a metastatic gastrointestinal stromal tumor
    • Joensuu H, Roberts PJ, Sarlomo-Rikala M, et al. Effect of the tyrosine kinase inhibitor STI571 in a patient with a metastatic gastrointestinal stromal tumor. N Engl J Med 2001;344:1052-6
    • (2001) N Engl J Med , vol.344 , pp. 1052-1056
    • Joensuu, H.1    Roberts, P.J.2    Sarlomo-Rikala, M.3
  • 44
    • 21144457929 scopus 로고    scopus 로고
    • Clinically meaningful improvement in symptoms and quality of life for patients with non-small cell lung cancer receiving gefitinib in a randomized controlled trial
    • Cella D, Herbst RS, Lynch TJ, et al. Clinically meaningful improvement in symptoms and quality of life for patients with non-small cell lung cancer receiving gefitinib in a randomized controlled trial. J Clin Oncol 2005;23:2946-54
    • (2005) J Clin Oncol , vol.23 , pp. 2946-2954
    • Cella, D.1    Herbst, R.S.2    Lynch, T.J.3
  • 45
    • 45949095870 scopus 로고    scopus 로고
    • Shepherd FA, Pereira J, Ciuleanu TE, et al. A randomized placebo-controlled trial of erlotinib in patients with advanced non-small cell lung cancer (NSCLC) following failure of 1st line or 2nd line chemotherapy. A National Cancer Institute of Canada Clinical Trials Group (NCIC CTG) trial. 2004 ASCO Annual Meeting Proceedings (Post-Meeting Edition). J Clin Oncol 2004;22(14S Suppl):7022
    • Shepherd FA, Pereira J, Ciuleanu TE, et al. A randomized placebo-controlled trial of erlotinib in patients with advanced non-small cell lung cancer (NSCLC) following failure of 1st line or 2nd line chemotherapy. A National Cancer Institute of Canada Clinical Trials Group (NCIC CTG) trial. 2004 ASCO Annual Meeting Proceedings (Post-Meeting Edition). J Clin Oncol 2004;22(14S Suppl):7022
  • 46
    • 45949090442 scopus 로고    scopus 로고
    • Ratain MJ, Flaherty KT, Stadler WM, et al. Preliminary antitumor activity of BAY 43-9006 in metastatic renal cell carcinoma and other advanced refractory solid tumors in a phase II randomized discontinuation trial (RDT). ASCO Proceedings. J Clin Oncol 2004;23:A4501
    • Ratain MJ, Flaherty KT, Stadler WM, et al. "Preliminary antitumor activity of BAY 43-9006 in metastatic renal cell carcinoma and other advanced refractory solid tumors in a phase II randomized discontinuation trial (RDT). ASCO Proceedings". J Clin Oncol 2004;23:A4501
  • 47
    • 33846181370 scopus 로고    scopus 로고
    • Sunitinib versus interferon alfa in metastatic renal-cell carcinoma
    • Motzer RJ, Hutson TE, Tomczak P, et al. Sunitinib versus interferon alfa in metastatic renal-cell carcinoma. N Engl J Med 2007;356:115-24
    • (2007) N Engl J Med , vol.356 , pp. 115-124
    • Motzer, R.J.1    Hutson, T.E.2    Tomczak, P.3
  • 48
    • 33749505836 scopus 로고    scopus 로고
    • Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: A randomised controlled trial
    • Demetri GD, van Oosterom AT, Garrett CR, et al. Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial. Lancet 2006;368:1329-38
    • (2006) Lancet , vol.368 , pp. 1329-1338
    • Demetri, G.D.1    van Oosterom, A.T.2    Garrett, C.R.3
  • 49
    • 33745102555 scopus 로고    scopus 로고
    • Dasatinib in imatinib-resistant philadelphia chromosome-positive leukemias
    • Talpaz M, Shah NP, Kantarjian H, et al. Dasatinib in imatinib-resistant philadelphia chromosome-positive leukemias N Engl J Med 2006;354:2531-41
    • (2006) N Engl J Med , vol.354 , pp. 2531-2541
    • Talpaz, M.1    Shah, N.P.2    Kantarjian, H.3
  • 50
    • 45949084379 scopus 로고    scopus 로고
    • Shah N, Sawyers CL, Kantarjian HM, et al. Correlation of clinical response to BMS-354825 with BCR-ABL mutation status in imatinib-resistant patients with chronic myeloid leukemia (CML) and Philadelphia chromosome-associated acute lymphoblastic leukemia (Ph+ ALL). 2005 ASCO Annual Meeting Proceedings. J Clin Oncol 2005;23(16S Suppl Pt I of II):565s [Abstract 6521]
    • Shah N, Sawyers CL, Kantarjian HM, et al. Correlation of clinical response to BMS-354825 with BCR-ABL mutation status in imatinib-resistant patients with chronic myeloid leukemia (CML) and Philadelphia chromosome-associated acute lymphoblastic leukemia (Ph+ ALL). 2005 ASCO Annual Meeting Proceedings. J Clin Oncol 2005;23(16S Suppl Pt I of II):565s [Abstract 6521]
  • 51
    • 33845886440 scopus 로고    scopus 로고
    • Lapatinib plus capecitabine for HER2-positive advanced breast cancer
    • Geyer CE, Forster J, Lindquist D, et al. Lapatinib plus capecitabine for HER2-positive advanced breast cancer. N Engl J Med 2006;355:2733-43
    • (2006) N Engl J Med , vol.355 , pp. 2733-2743
    • Geyer, C.E.1    Forster, J.2    Lindquist, D.3
  • 52
    • 34548388473 scopus 로고    scopus 로고
    • Temsirolimus for advanced renal-cell carcinoma
    • Fazio N, Dettori M, Lorizzo K, et al. Temsirolimus for advanced renal-cell carcinoma. N Engl J Med 2007;357:1050-10
    • (2007) N Engl J Med , vol.357 , pp. 1050-1110
    • Fazio, N.1    Dettori, M.2    Lorizzo, K.3
  • 53
    • 33745086350 scopus 로고    scopus 로고
    • Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive AL
    • Kantarjian H, Giles F, Wunderle L, et al. Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive AL. N Engl J Med 354:2542-51
    • N Engl J Med , vol.354 , pp. 2542-2551
    • Kantarjian, H.1    Giles, F.2    Wunderle, L.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.