WO2003104481A3 - Method for designing pdk1 modulators - Google Patents
Method for designing pdk1 modulators Download PDFInfo
- Publication number
- WO2003104481A3 WO2003104481A3 PCT/GB2003/002509 GB0302509W WO03104481A3 WO 2003104481 A3 WO2003104481 A3 WO 2003104481A3 GB 0302509 W GB0302509 W GB 0302509W WO 03104481 A3 WO03104481 A3 WO 03104481A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- protein kinase
- compound
- dimensional structure
- catalytic domain
- pdk1
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- 101100351314 Caenorhabditis elegans pdk-1 gene Proteins 0.000 title 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 4
- 230000003197 catalytic effect Effects 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 108060006633 protein kinase Proteins 0.000 abstract 4
- 101001031598 Dictyostelium discoideum Probable serine/threonine-protein kinase fhkC Proteins 0.000 abstract 1
- 101000600756 Homo sapiens 3-phosphoinositide-dependent protein kinase 1 Proteins 0.000 abstract 1
- 101100029888 Homo sapiens PKD1 gene Proteins 0.000 abstract 1
- 101001117146 Homo sapiens [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial Proteins 0.000 abstract 1
- 102100024148 [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial Human genes 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000012634 fragment Substances 0.000 abstract 1
- 230000004927 fusion Effects 0.000 abstract 1
- 238000000302 molecular modelling Methods 0.000 abstract 1
- 150000003906 phosphoinositides Chemical class 0.000 abstract 1
- 108700009994 polycystic kidney disease 1 Proteins 0.000 abstract 1
- 229920001184 polypeptide Polymers 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
- C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
-
- C—CHEMISTRY; METALLURGY
- C22—METALLURGY; FERROUS OR NON-FERROUS ALLOYS; TREATMENT OF ALLOYS OR NON-FERROUS METALS
- C22C—ALLOYS
- C22C43/00—Alloys containing radioactive materials
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Mechanical Engineering (AREA)
- Microbiology (AREA)
- Molecular Biology (AREA)
- Biotechnology (AREA)
- Biophysics (AREA)
- Analytical Chemistry (AREA)
- Biochemistry (AREA)
- Physics & Mathematics (AREA)
- General Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Materials Engineering (AREA)
- Immunology (AREA)
- Metallurgy (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Enzymes And Modification Thereof (AREA)
- Liquid Crystal Substances (AREA)
- Materials For Photolithography (AREA)
- Liquid Developers In Electrophotography (AREA)
- Manufacture And Refinement Of Metals (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrane Compounds (AREA)
- Peptides Or Proteins (AREA)
Abstract
Priority Applications (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU2003241038A AU2003241038A1 (en) | 2002-06-08 | 2003-06-09 | Method for designing pdk1 modulators |
US10/517,225 US7792665B2 (en) | 2002-06-08 | 2003-06-09 | Method for designing a compound based on the three dimensional structure of phosphoinositide dependent protein kinase 1 (PDK1) |
EP03730356A EP1513947B1 (en) | 2002-06-08 | 2003-06-09 | Method for designing pdk1 modulators |
DE60313967T DE60313967T2 (en) | 2002-06-08 | 2003-06-09 | PROCESS FOR DEVELOPING PDK1 MODULATORS |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB0213186.0A GB0213186D0 (en) | 2002-06-08 | 2002-06-08 | Methods |
GB0213186.0 | 2002-06-08 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2003104481A2 WO2003104481A2 (en) | 2003-12-18 |
WO2003104481A3 true WO2003104481A3 (en) | 2004-09-23 |
Family
ID=9938208
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/GB2003/002509 WO2003104481A2 (en) | 2002-06-08 | 2003-06-09 | Methods |
Country Status (7)
Country | Link |
---|---|
US (1) | US7792665B2 (en) |
EP (1) | EP1513947B1 (en) |
AT (1) | ATE362993T1 (en) |
AU (1) | AU2003241038A1 (en) |
DE (1) | DE60313967T2 (en) |
GB (1) | GB0213186D0 (en) |
WO (1) | WO2003104481A2 (en) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2006020755A2 (en) * | 2004-08-10 | 2006-02-23 | Beth Israel Deaconess Medical Center, Inc. | Methods for identifying inhibitors of the mtor pathway as diabetes therapeutics |
US20110152166A1 (en) * | 2006-08-18 | 2011-06-23 | Ricardo M. Biondi | Method of modulation of protein phosphorylation-dependent conformational transitions with low molecular weight compounds |
EP2182058A1 (en) * | 2008-10-17 | 2010-05-05 | Universität des Saarlandes | High resolution complex structure and allosteric effects of low molecular weight activators on the protein kinase PDK1 |
NZ620174A (en) | 2009-09-16 | 2016-08-26 | Celgene Avilomics Res Inc | Protein kinase conjugates and inhibitors |
WO2011082285A1 (en) * | 2009-12-30 | 2011-07-07 | Avila Therapeutics, Inc. | Ligand-directed covalent modification of protein |
WO2011149874A2 (en) * | 2010-05-26 | 2011-12-01 | Schering Corporation | N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1 |
EP2865757A1 (en) | 2013-10-22 | 2015-04-29 | Sylentis, S.A.U. | siRNA and their use in methods and compositions for inhibiting the expression of the PDK1 gene. |
JP6709273B2 (en) * | 2018-03-28 | 2020-06-10 | 公益財団法人福岡県産業・科学技術振興財団 | Vapor deposition equipment |
Citations (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1998041638A1 (en) * | 1997-03-17 | 1998-09-24 | Medical Research Council | Phosphatidyl-3,4.5-triphosphate-dependent protein kinase |
US5854992A (en) * | 1996-09-26 | 1998-12-29 | President And Fellows Of Harvard College | System and method for structure-based drug design that includes accurate prediction of binding free energy |
WO2000056864A2 (en) * | 1999-03-19 | 2000-09-28 | University Of Dundee | Methods for altering substrate specificity of phosphoinositide-dependent-protein kinase 1 (pdk1) |
WO2000070030A1 (en) * | 1999-05-19 | 2000-11-23 | Amgen Inc. | Crystal of a lymphocyte kinase-ligand complex and methods of use |
EP1096014A2 (en) * | 1999-11-01 | 2001-05-02 | Agouron Pharmaceuticals, Inc. | Catalytic domain of the human effector cell cycle checkpoint protein kinase, Chk1, materials and methods for identification of inhibitors thereof |
WO2001035316A2 (en) * | 1999-11-10 | 2001-05-17 | Structural Bioinformatics, Inc. | Computationally derived protein structures in pharmacogenomics |
WO2001044497A2 (en) * | 1999-12-02 | 2001-06-21 | University Of Dundee | Protein kinase regulation |
WO2001071347A1 (en) * | 2000-03-23 | 2001-09-27 | California Institute Of Technology | Method and apparatus for predicting ligand binding interactions |
WO2002022793A1 (en) * | 2000-09-11 | 2002-03-21 | Astex Technology Limited | Crystal structure of pantothenate synthetase |
US6387641B1 (en) * | 1998-12-16 | 2002-05-14 | Vertex Pharmaceuticals Incorporated | Crystallized P38 complexes |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ATE373676T1 (en) | 1998-12-14 | 2007-10-15 | Univ Dundee | METHOD FOR ACTIVATING SGK BY PHOSPHORYLATION. |
JP2002532100A (en) | 1998-12-14 | 2002-10-02 | メディカル リサーチ カウンシル | Screening method |
US20040137518A1 (en) * | 2002-01-31 | 2004-07-15 | Lambert Millard Hurst | CRYSTALLIZED PPARa LIGAND BINDING DOMAIN POLYPEPTIDE AND SCREENING METHODS EMPLOYING SAME |
-
2002
- 2002-06-08 GB GBGB0213186.0A patent/GB0213186D0/en not_active Ceased
-
2003
- 2003-06-09 DE DE60313967T patent/DE60313967T2/en not_active Expired - Lifetime
- 2003-06-09 WO PCT/GB2003/002509 patent/WO2003104481A2/en active IP Right Grant
- 2003-06-09 AU AU2003241038A patent/AU2003241038A1/en not_active Abandoned
- 2003-06-09 US US10/517,225 patent/US7792665B2/en not_active Expired - Fee Related
- 2003-06-09 EP EP03730356A patent/EP1513947B1/en not_active Expired - Lifetime
- 2003-06-09 AT AT03730356T patent/ATE362993T1/en not_active IP Right Cessation
Patent Citations (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5854992A (en) * | 1996-09-26 | 1998-12-29 | President And Fellows Of Harvard College | System and method for structure-based drug design that includes accurate prediction of binding free energy |
WO1998041638A1 (en) * | 1997-03-17 | 1998-09-24 | Medical Research Council | Phosphatidyl-3,4.5-triphosphate-dependent protein kinase |
US6387641B1 (en) * | 1998-12-16 | 2002-05-14 | Vertex Pharmaceuticals Incorporated | Crystallized P38 complexes |
WO2000056864A2 (en) * | 1999-03-19 | 2000-09-28 | University Of Dundee | Methods for altering substrate specificity of phosphoinositide-dependent-protein kinase 1 (pdk1) |
WO2000070030A1 (en) * | 1999-05-19 | 2000-11-23 | Amgen Inc. | Crystal of a lymphocyte kinase-ligand complex and methods of use |
EP1096014A2 (en) * | 1999-11-01 | 2001-05-02 | Agouron Pharmaceuticals, Inc. | Catalytic domain of the human effector cell cycle checkpoint protein kinase, Chk1, materials and methods for identification of inhibitors thereof |
WO2001035316A2 (en) * | 1999-11-10 | 2001-05-17 | Structural Bioinformatics, Inc. | Computationally derived protein structures in pharmacogenomics |
WO2001044497A2 (en) * | 1999-12-02 | 2001-06-21 | University Of Dundee | Protein kinase regulation |
WO2001071347A1 (en) * | 2000-03-23 | 2001-09-27 | California Institute Of Technology | Method and apparatus for predicting ligand binding interactions |
WO2002022793A1 (en) * | 2000-09-11 | 2002-03-21 | Astex Technology Limited | Crystal structure of pantothenate synthetase |
Non-Patent Citations (1)
Title |
---|
BIONDI RICARDO M ET AL: "High resolution crystal structure of the human PDK1 catalytic domain defines the regulatory phosphopeptide docking site", EMBO (EUROPEAN MOLECULAR BIOLOGY ORGANIZATION) JOURNAL, vol. 21, no. 16, 15 August 2002 (2002-08-15), pages 4219 - 4228, XP002266843, ISSN: 0261-4189 * |
Also Published As
Publication number | Publication date |
---|---|
GB0213186D0 (en) | 2002-07-17 |
DE60313967T2 (en) | 2008-01-17 |
AU2003241038A8 (en) | 2003-12-22 |
US20050232804A1 (en) | 2005-10-20 |
EP1513947A2 (en) | 2005-03-16 |
DE60313967D1 (en) | 2007-07-05 |
US7792665B2 (en) | 2010-09-07 |
EP1513947B1 (en) | 2007-05-23 |
AU2003241038A1 (en) | 2003-12-22 |
WO2003104481A2 (en) | 2003-12-18 |
ATE362993T1 (en) | 2007-06-15 |
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