Title:
METHOD FOR SELECTING ENZYME INHIBITORS
Document Type and Number:
WIPO Patent Application WO2001088530
Kind Code:
A3
Abstract:
The present invention relates to a method for selecting enzyme inhibitors and for using inhibitors selected as treatment and/or prevention agents. The invention also relates to a mutant form that can be used within said method as well as a method used to check an inhibitor specificity in a model system.
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Inventors:
WARMUTH MARKUS (DE)
MATHES RUTH (DE)
HALLEK MICHAEL (DE)
MATHES RUTH (DE)
HALLEK MICHAEL (DE)
Application Number:
PCT/EP2001/005661
Publication Date:
November 14, 2002
Filing Date:
May 17, 2001
Export Citation:
Assignee:
GSF FORSCHUNGSZENTRUM UMWELT (DE)
WARMUTH MARKUS (DE)
MATHES RUTH (DE)
HALLEK MICHAEL (DE)
WARMUTH MARKUS (DE)
MATHES RUTH (DE)
HALLEK MICHAEL (DE)
International Classes:
C12N9/12; C12Q1/48; G01N33/68; (IPC1-7): G01N33/68; C12Q1/48; C12N9/12
Domestic Patent References:
| WO1998035048A2 | 1998-08-13 |
Other References:
ERNEST ISABELLE ET AL: "Pyruvate kinase of Trypanosoma brucei: Overexpression, purification, and functional characterization of wild-type and mutated enzyme.", PROTEIN EXPRESSION AND PURIFICATION, vol. 13, no. 3, August 1998 (1998-08-01), pages 373 - 382, XP001066571, ISSN: 1046-5928
IKEDA YOSHITAKA ET AL: "Allosteric regulation of pyruvate kinase M2 isozyme involves a cysteine residue in the intersubunit contact.", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 273, no. 20, 15 May 1998 (1998-05-15), pages 12227 - 12233, XP001066226, ISSN: 0021-9258
UENO YOSHIHISA ET AL: "Regulatory phosphorylation of plant phosphoenolpyruvate carboxylase: Role of a conserved basic residue upstream of the phosphorylation site.", FEBS LETTERS, vol. 417, no. 1, 3 November 1997 (1997-11-03), pages 57 - 60, XP001066232, ISSN: 0014-5793
BISHOP ANTHONY C ET AL: "Acquisition of inhibitor-sensitive protein kinases through protein design.", PHARMACOLOGY & THERAPEUTICS, vol. 82, no. 2-3, May 1999 (1999-05-01), pages 337 - 346, XP000974993, ISSN: 0163-7258
BISHOP A C ET AL: "Generation of monospecific nanomolar tyrosine kinase inhibitors via a chemical genetic approach", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, DC, US, vol. 121, no. 4, 1999, pages 627 - 631, XP002142032, ISSN: 0002-7863
LIU Y ET AL: "STRUCTURAL BASIS FOR SELECTIVE INHIBITION OF SRC FAMILY KINASES BY PP1", CHEMISTRY AND BIOLOGY, CURRENT BIOLOGY, LONDON, GB, vol. 6, no. 9, September 1999 (1999-09-01), pages 671 - 678, XP000978065, ISSN: 1074-5521
BISHOP A C ET AL: "DESIGN OF ALLELE-SPECIFIC INHIBITORS TO PROBE PROTEIN KINASE SIGNALING", CURRENT BIOLOGY, CURRENT SCIENCE,, GB, vol. 8, no. 5, 26 February 1998 (1998-02-26), pages 257 - 266, XP000974996, ISSN: 0960-9822
WARMUTH MARKUS ET AL: "Genetic analysis of the ATP binding sites of Hck and ABL kinases reveal distinct and overlapping determinants for the specificity of the tyrosine kinase inhibitors PP1 and STI571.", BLOOD, vol. 96, no. 11 Part 1, 16 November 2000 (2000-11-16), 42nd Annual Meeting of the American Society of Hematology;San Francisco, California, USA; December 01-05, 2000, pages 510a, XP001064435, ISSN: 0006-4971
BOND CHRISTOPHER J ET AL: "Determinants of allosteric activation of yeast pyruvate kinase and identification of novel effectors using computational screening.", BIOCHEMISTRY, vol. 39, no. 50, 19 December 2000 (2000-12-19), pages 15333 - 15343, XP001066224, ISSN: 0006-2960
IKEDA YOSHITAKA ET AL: "Allosteric regulation of pyruvate kinase M2 isozyme involves a cysteine residue in the intersubunit contact.", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 273, no. 20, 15 May 1998 (1998-05-15), pages 12227 - 12233, XP001066226, ISSN: 0021-9258
UENO YOSHIHISA ET AL: "Regulatory phosphorylation of plant phosphoenolpyruvate carboxylase: Role of a conserved basic residue upstream of the phosphorylation site.", FEBS LETTERS, vol. 417, no. 1, 3 November 1997 (1997-11-03), pages 57 - 60, XP001066232, ISSN: 0014-5793
BISHOP ANTHONY C ET AL: "Acquisition of inhibitor-sensitive protein kinases through protein design.", PHARMACOLOGY & THERAPEUTICS, vol. 82, no. 2-3, May 1999 (1999-05-01), pages 337 - 346, XP000974993, ISSN: 0163-7258
BISHOP A C ET AL: "Generation of monospecific nanomolar tyrosine kinase inhibitors via a chemical genetic approach", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, DC, US, vol. 121, no. 4, 1999, pages 627 - 631, XP002142032, ISSN: 0002-7863
LIU Y ET AL: "STRUCTURAL BASIS FOR SELECTIVE INHIBITION OF SRC FAMILY KINASES BY PP1", CHEMISTRY AND BIOLOGY, CURRENT BIOLOGY, LONDON, GB, vol. 6, no. 9, September 1999 (1999-09-01), pages 671 - 678, XP000978065, ISSN: 1074-5521
BISHOP A C ET AL: "DESIGN OF ALLELE-SPECIFIC INHIBITORS TO PROBE PROTEIN KINASE SIGNALING", CURRENT BIOLOGY, CURRENT SCIENCE,, GB, vol. 8, no. 5, 26 February 1998 (1998-02-26), pages 257 - 266, XP000974996, ISSN: 0960-9822
WARMUTH MARKUS ET AL: "Genetic analysis of the ATP binding sites of Hck and ABL kinases reveal distinct and overlapping determinants for the specificity of the tyrosine kinase inhibitors PP1 and STI571.", BLOOD, vol. 96, no. 11 Part 1, 16 November 2000 (2000-11-16), 42nd Annual Meeting of the American Society of Hematology;San Francisco, California, USA; December 01-05, 2000, pages 510a, XP001064435, ISSN: 0006-4971
BOND CHRISTOPHER J ET AL: "Determinants of allosteric activation of yeast pyruvate kinase and identification of novel effectors using computational screening.", BIOCHEMISTRY, vol. 39, no. 50, 19 December 2000 (2000-12-19), pages 15333 - 15343, XP001066224, ISSN: 0006-2960
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