High-throughput screening by mass spectrometry: Comparison with the scintillation proximity assay with a focused-file screen of AKT1/PKBα

Journal of Biomolecular Screening

Volumn 12, Issue 4, 2007, Pages 473-480

  Quercia, Andrea K ^a   LaMarr, William A ^b   Myung, Jayhyuk ^a   Özbal, Can C ^b   Landro, James A ^a   Lumb, Kevin J ^a  

^a BAYER CORPORATION   (United States)

^b BioTrove Inc   (United States)

Author keywords

False negatives; False positives; High throughput screening; Mass spectrometry; SPA

Indexed keywords

PHOSPHOTRANSFERASE INHIBITOR; PROTEIN KINASE B; PROTEIN KINASE B ALPHA; UNCLASSIFIED DRUG;

ARTICLE; ASSAY; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; IC 50; MASS SPECTROMETRY; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN TARGETING; SCINTILLATION PROXIMITY ASSAY; SCREENING;

AMINO ACID SEQUENCE; FALSE NEGATIVE REACTIONS; FALSE POSITIVE REACTIONS; MOLECULAR SEQUENCE DATA; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-AKT; SCINTILLATION COUNTING; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION;

EID: 34249912663     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057107300647     Document Type: Article

References (19)

1. Walters WP, Namchuk M.: Designing screens: how to make your hits a hit. Nature Rev Drug Discov 2003 ; 2: 259-266.
2. von Ahsen O., Bomer U.: High-throughput screening for kinase inhibitors. Chembiochem 2005 ; 6: 481-490.
3. Keseru GM, Makara GM: Hit discovery and hit-to-lead approaches. Drug Discov Today 2006 ; 11: 741-748.
4. Hsieh F., Keshishian H., Muir C.: Automated high throughput multiple target screening of molecular libraries by microfluidic MALDI-TOF MS. J Biomol Screen 1998 ; 3: 189-198.
5. Benkestock K., Van Pelt CK, Akerud T., Sterling A., Edlund PO, Roeraade J.: Automated nano-electrospray mass spectrometry for protein-ligand screening by noncovalent interaction applied to human H-FABP and A-FABP. J Biomol Screen 2003 ; 8: 247-256.
6. Min DH, Tang WJ, Mrksich M.: Chemical screening by mass spectrometry to identify inhibitors of anthrax lethal factor. Nature Biotechnol 2004 ; 22: 717-723.
7. Özbal CC, LaMarr WA, Linton JR, Green DF, Katz A., Morrison TB,, et al. High throughput screening via mass spectrometry: a case study using acetylcholinesterase. Assay Drug Dev Technol 2004 ; 2: 373-381.
8. Yang M., Brazier M., Edwards R., Davis BG: High-throughput mass-spectrometry monitoring for multisubstrate enzymes: determining the kinetic parameters and catalytic activities of glycosyltransferases. Chembiochem 2005 ; 6: 346-357.
9. Hennessy BT, Smith DL, Ram PT, Lu Y., Mills GB: Exploiting the PI3K/AKT pathway for cancer drug discovery. Nat Rev Drug Discov 2005 ; 4: 988-1004.
10. Miller JL: Recent developments in focused library design: targeting gene-families. Curr Top Med Chem 2006 ; 6: 19-29.
11. Obata T., Yaffe MB, Leparc GG, Piro ET, Maegawa H., Kashiwagi A.,, et al. Peptide and protein library screening defines optimal substrate motifs for AKT/PKB. J Biol Chem 2000 ; 275: 36108-36115.
12. Zhang JH, Chung TD, Oldenburg KR: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999 ; 4: 67-73.
13. Sills MA, Weiss D., Pham Q., Schweitzer R., Wu X., Wu JJ: Comparison of assay technologies for a tyrosine kinase assay generates different results in high throughput screening. J Biomol Screen 2002 ; 7: 191-214.
14. 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: 381-392.
15. 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 ; 10: 581-589.
16. Turek-Etienne TC, Small EC, Soh SC, Xin TA, Gaitonde PV, Barrabee EB,, et al. Evaluation of fluorescent compound interference in 4 fluorescence polarization assays: 2 kinases, 1 protease, and 1 phosphatase. J Biomol Screen 2003 ; 8: 176-184.
17. 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.
18. Zhu Z., Kim S., Chen T., Lin JH, Bell A., Bryson J.,, et al. Correlation of high-throughput pregnane X receptor (PXR) transactivation and binding assays. J Biomol Screen 2004 ; 9: 533-540.
19. von Ahsen O., Schmidt A., Klotz M., Parczyk K.: Assay concordance between SPA and TR-FRET in high-throughput screening. J Biomol Screen 2006 ; 11: 606-616.