Title:
PROCESS FOR HIGH THROUGHPUT LIQUID OR GAS CHROMATOGRAPHY/MASS SPECTROMETRY-BASED BIOMOLECULAR SCREENING FOR DRUG DISCOVERY
Document Type and Number:
WIPO Patent Application WO/2005/108597
Kind Code:
A2
Abstract:
Methods of achieving realistic hit rates and reducing or eliminating false positive rates in medicinal compound high throughput screening are provided. The methods of the invention include chromatographic resolution, for example by liquid or gas chromatography of biological substrates and/or substrate products, followed by sensitive with mass spectrometry to measure biological activity screening to generate meaningful drug leads. The methods of the invention save significant method development and thus are directly applicable to the high throughput screening time scale while providing high accuracy and sensitivity.
Inventors:
HAYWARD MARK (US)
Application Number:
PCT/US2005/014820
Publication Date:
November 17, 2005
Filing Date:
April 29, 2005
Export Citation:
Assignee:
HAYWARD MARK (US)
International Classes:
G01N30/46; G01N33/573; G01N30/62; G01N30/72; G01N30/86; (IPC1-7): C12Q1/00
Domestic Patent References:
| WO2003054514A2 | 2003-07-03 |
Foreign References:
| US20030211464A1 | 2003-11-13 | |||
| US20020182651A1 | 2002-12-05 | |||
| US20030004653A1 | 2003-01-02 |
Other References:
XU R ET AL: "Application of parallel liquid chromatography/mass spectrometry for high throughput microsomal stability screening of compound libraries" JOURNAL OF THE AMERICAN SOCIETY FOR MASS SPECTROMETRY, ELSEVIER SCIENCE INC., NEW YORK, NY, US, vol. 13, no. 2, February 2001 (2001-02), pages 155-165, XP004334680 ISSN: 1044-0305
DENG Y. ET AL: "high-speed gradient parallel liquid chromatography/tandem mass spectrometry with fully automated sample preparation for bioanalysis: 30 seconds per sample from plasma" 1997, RAPID COMMUNICATIONS IN MASS SPECTROMETRY, HEYDEN, LONDON, GB, PAGE(S) 846-856 , XP008053275 ISSN: 0951-4198 page 1121
YANG L ET AL: "Applications of new liquid chromatography-tandem mass spectrometry technologies for drug development support" JOURNAL OF CHROMATOGRAPHY A, ELSEVIER, AMSTERDAM, NL, vol. 926, no. 1, 10 August 2001 (2001-08-10), pages 43-55, XP004297489 ISSN: 0021-9673
NIESSEN W M A: "Progress in liquid chromatography-mass spectrometry instrumentation and its impact on high-throughput screening" JOURNAL OF CHROMATOGRAPHY A, ELSEVIER, AMSTERDAM, NL, vol. 1000, no. 1-2, 6 June 2003 (2003-06-06), pages 413-436, XP004427306 ISSN: 0021-9673
FANG, L. ET AL.: "High-throughput accurate mass and purity analysis of combinatorial libraries using a nine-way multiplexed electrospray LC/UV/TOFMS system" PROCEEDINGS OF THE 50TH ASMS CONFERENCE ON MASS SPECTROMETRY AND ALLIED TOPICS, 2 June 2002 (2002-06-02), - 6 June 2002 (2002-06-06) pages 605-606, XP008053264 Orlando, Florida, USA
MASIMIREMBWA C M ET AL: "IN VITRO HIGH THROUGHPUT SCREENING OF COMPOUNDS FOR FAVORABLE METABOLIC PROPERTIES IN DRUG DISCOVERY" COMBINATORIAL CHEMISTRY AND HIGH THROUGHPUT SCREENING, HILVERSUM, NL, vol. 4, no. 3, May 2001 (2001-05), pages 245-263, XP008025592 ISSN: 1386-2073
DENG Y. ET AL: "high-speed gradient parallel liquid chromatography/tandem mass spectrometry with fully automated sample preparation for bioanalysis: 30 seconds per sample from plasma" 1997, RAPID COMMUNICATIONS IN MASS SPECTROMETRY, HEYDEN, LONDON, GB, PAGE(S) 846-856 , XP008053275 ISSN: 0951-4198 page 1121
YANG L ET AL: "Applications of new liquid chromatography-tandem mass spectrometry technologies for drug development support" JOURNAL OF CHROMATOGRAPHY A, ELSEVIER, AMSTERDAM, NL, vol. 926, no. 1, 10 August 2001 (2001-08-10), pages 43-55, XP004297489 ISSN: 0021-9673
NIESSEN W M A: "Progress in liquid chromatography-mass spectrometry instrumentation and its impact on high-throughput screening" JOURNAL OF CHROMATOGRAPHY A, ELSEVIER, AMSTERDAM, NL, vol. 1000, no. 1-2, 6 June 2003 (2003-06-06), pages 413-436, XP004427306 ISSN: 0021-9673
FANG, L. ET AL.: "High-throughput accurate mass and purity analysis of combinatorial libraries using a nine-way multiplexed electrospray LC/UV/TOFMS system" PROCEEDINGS OF THE 50TH ASMS CONFERENCE ON MASS SPECTROMETRY AND ALLIED TOPICS, 2 June 2002 (2002-06-02), - 6 June 2002 (2002-06-06) pages 605-606, XP008053264 Orlando, Florida, USA
MASIMIREMBWA C M ET AL: "IN VITRO HIGH THROUGHPUT SCREENING OF COMPOUNDS FOR FAVORABLE METABOLIC PROPERTIES IN DRUG DISCOVERY" COMBINATORIAL CHEMISTRY AND HIGH THROUGHPUT SCREENING, HILVERSUM, NL, vol. 4, no. 3, May 2001 (2001-05), pages 245-263, XP008025592 ISSN: 1386-2073
Attorney, Agent or Firm:
Alstadt, Lynn J. (P.C. One Oxford Centre, 20th floor, 301 Grant Stree, Pittsburgh PA, US)
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