WO2002020734A3 - Crystallized cytoplasmic tie2 receptor tyrosine kinase domain and method of determining and designing modulators of the same - Google Patents

Crystallized cytoplasmic tie2 receptor tyrosine kinase domain and method of determining and designing modulators of the same Download PDF

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Publication number
WO2002020734A3
WO2002020734A3 PCT/US2001/027486 US0127486W WO0220734A3 WO 2002020734 A3 WO2002020734 A3 WO 2002020734A3 US 0127486 W US0127486 W US 0127486W WO 0220734 A3 WO0220734 A3 WO 0220734A3
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WO
WIPO (PCT)
Prior art keywords
cytoplasmic
tyrosine kinase
receptor tyrosine
kinase domain
tie2 receptor
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2001/027486
Other languages
French (fr)
Other versions
WO2002020734A2 (en
Inventor
Roderick Gerald Davis
Byron Peters Ellis
Anne Moore Hassell
William D Holmes
Lisa Marie Shewchuk
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Glaxo Group Ltd
Original Assignee
Glaxo Group Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Priority to EP01968491A priority Critical patent/EP1345966A2/en
Priority to AU2001288735A priority patent/AU2001288735A1/en
Publication of WO2002020734A2 publication Critical patent/WO2002020734A2/en
Anticipated expiration legal-status Critical
Publication of WO2002020734A3 publication Critical patent/WO2002020734A3/en
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/71—Receptors; Cell surface antigens; Cell surface determinants for growth factors; for growth regulators

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Zoology (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Cell Biology (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

A solved three-dimensional crystal structure of a cytoplasmic Tie2 receptor tyrosine kinase domain is disclosed, along with four crystal forms of the cytoplasmic Tie2 receptor tyrosine kinase domain. The crystal forms include non- and monophosphorylated forms of the cytoplasmic Tie2 receptor tyrosine kinase domain. Methods of designing modulators of the biological activity of the cytoplasmic Tie2 receptor tyrosine kinase domain are also disclosed.
PCT/US2001/027486 2000-09-08 2001-09-06 Crystallized cytoplasmic tie2 receptor tyrosine kinase domain and method of determining and designing modulators of the same Ceased WO2002020734A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP01968491A EP1345966A2 (en) 2000-09-08 2001-09-06 Crystallized cytoplasmic tie2 receptor tyrosine kinase domain and method of determining and designing modulators of the same
AU2001288735A AU2001288735A1 (en) 2000-09-08 2001-09-06 Crystallized cytoplasmic tie2 receptor tyrosine kinase domain and method of determining and designing modulators of the same

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US23139800P 2000-09-08 2000-09-08
US60/231,398 2000-09-08

Publications (2)

Publication Number Publication Date
WO2002020734A2 WO2002020734A2 (en) 2002-03-14
WO2002020734A3 true WO2002020734A3 (en) 2003-06-19

Family

ID=22869071

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/027486 Ceased WO2002020734A2 (en) 2000-09-08 2001-09-06 Crystallized cytoplasmic tie2 receptor tyrosine kinase domain and method of determining and designing modulators of the same

Country Status (3)

Country Link
EP (1) EP1345966A2 (en)
AU (1) AU2001288735A1 (en)
WO (1) WO2002020734A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7427616B2 (en) 2002-08-06 2008-09-23 Astrazeneca Ab Condensed pyridines and pyrimidines with tie2 (TEK) activity

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004092217A1 (en) * 2003-04-17 2004-10-28 Pfizer Inc. Crystal structure of vegfrkd: ligand complexes and methods of use thereof
AU2009262199B2 (en) 2008-06-27 2012-08-09 Amgen Inc. Ang-2 inhibition to treat multiple sclerosis
CN111172154B (en) * 2020-01-08 2021-11-30 中国科学院华南植物园 Method for extracting total RNA of sandalwood high-content essential oil tissue
CN116183560B (en) * 2021-11-29 2025-10-28 中国科学院大连化学物理研究所 Application of dye molecules in detecting tyrosine phosphorylated peptides and monitoring protein kinase activity

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995013387A1 (en) * 1993-11-12 1995-05-18 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Tie-2, a novel receptor tyrosine kinase
WO2001072778A2 (en) * 2000-03-29 2001-10-04 Knoll Gesellschaft Mit Beschraenkter Haftung Method of identifying inhibitors of tie-2

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995013387A1 (en) * 1993-11-12 1995-05-18 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Tie-2, a novel receptor tyrosine kinase
WO2001072778A2 (en) * 2000-03-29 2001-10-04 Knoll Gesellschaft Mit Beschraenkter Haftung Method of identifying inhibitors of tie-2

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
CALVERT: "Allelic and locus heterogeneity in inherited venous malformations", HUMAN MOLECULAR GENETICS, vol. 8, 1999, pages 1279 - 1289, XP002219717 *
DJORDJEVIC: "Crystallization and preliminary x-ray studies of NADPH-cytochrome P450 reductase", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES, USA, vol. 92, 1995, pages 3214 - 3218, XP002219719 *
HIMANEN ET AL: "Crystal structure of the ligand-binding domain of the receptor tyrosine kinase EphB2", NATURE, vol. 396, 3 December 1998 (1998-12-03), pages 486 - 491, XP002134939, ISSN: 0028-0836 *
MOHAMMADI ET AL: "Structure of the FGF receptor tyrosine kinase domain reveals a novel autoinhibitory mechanism", CELL, vol. 86, 1996, pages 577 - 587, XP002219716 *
ROBERTSON ET AL: "RTK mutations and human syndromes when good receptors turn bad", TIG, vol. 16, June 2000 (2000-06-01), pages 265 - 271, XP004200112 *
SHEWCHUK: "Structure of the Tie2 RTK domain: Self-inhibition by the nucleotide binding loop, activation loop, and C-terminal tail", STRUCTURE, vol. 8, November 2000 (2000-11-01), pages 1105 - 1113, XP001115087 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7427616B2 (en) 2002-08-06 2008-09-23 Astrazeneca Ab Condensed pyridines and pyrimidines with tie2 (TEK) activity

Also Published As

Publication number Publication date
AU2001288735A1 (en) 2002-03-22
WO2002020734A2 (en) 2002-03-14
EP1345966A2 (en) 2003-09-24

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