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WO2007120463A3 - Compositions and methods for modulation of nek2 kinase activity - Google Patents

Compositions and methods for modulation of nek2 kinase activity Download PDF

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Publication number
WO2007120463A3
WO2007120463A3 PCT/US2007/008087 US2007008087W WO2007120463A3 WO 2007120463 A3 WO2007120463 A3 WO 2007120463A3 US 2007008087 W US2007008087 W US 2007008087W WO 2007120463 A3 WO2007120463 A3 WO 2007120463A3
Authority
WO
WIPO (PCT)
Prior art keywords
nek2
kinase activity
modulation
compositions
methods
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/US2007/008087
Other languages
French (fr)
Other versions
WO2007120463A2 (en
Inventor
Deepak Sampath
Jennifer Pocas
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.)
Wyeth LLC
Original Assignee
Wyeth LLC
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 Wyeth LLC filed Critical Wyeth LLC
Publication of WO2007120463A2 publication Critical patent/WO2007120463A2/en
Publication of WO2007120463A3 publication Critical patent/WO2007120463A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/4738—Cell cycle regulated proteins, e.g. cyclin, CDC, INK-CCR
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases

Landscapes

  • Life Sciences & Earth Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Wood Science & Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • Toxicology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Described are serine and threonine-containing peptides derived from the proteins c-NAPl and NEK2 that constitute phosphorylation substrates for the serine/threonine kinase NEK2. These peptides can be used to measure kinase activity of a NEK2 protein and to identify compounds that modulate phosphorylation of a NEK2 substrate by a NEK2 protein. The peptides can also be used as competitive inhibitors of NEK2 kinase activity.
PCT/US2007/008087 2006-04-03 2007-04-02 Compositions and methods for modulation of nek2 kinase activity Ceased WO2007120463A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US78908706P 2006-04-03 2006-04-03
US60/789,087 2006-04-03

Publications (2)

Publication Number Publication Date
WO2007120463A2 WO2007120463A2 (en) 2007-10-25
WO2007120463A3 true WO2007120463A3 (en) 2008-02-21

Family

ID=38610042

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2007/008087 Ceased WO2007120463A2 (en) 2006-04-03 2007-04-02 Compositions and methods for modulation of nek2 kinase activity

Country Status (1)

Country Link
WO (1) WO2007120463A2 (en)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003000903A2 (en) * 2001-06-25 2003-01-03 Bayer Healthcare Ag Regulation of human nek-like serine/threonine protein kinase
WO2003062197A2 (en) * 2002-01-24 2003-07-31 Chiron Corporation Nek2 inhibitors
WO2004033666A2 (en) * 2002-10-11 2004-04-22 Board Of Regents, The University Of Texas System Method and compounds for inhibiting hec1 activity for the treatment of proliferative diseases

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003000903A2 (en) * 2001-06-25 2003-01-03 Bayer Healthcare Ag Regulation of human nek-like serine/threonine protein kinase
WO2003062197A2 (en) * 2002-01-24 2003-07-31 Chiron Corporation Nek2 inhibitors
WO2004033666A2 (en) * 2002-10-11 2004-04-22 Board Of Regents, The University Of Texas System Method and compounds for inhibiting hec1 activity for the treatment of proliferative diseases

Non-Patent Citations (13)

* Cited by examiner, † Cited by third party
Title
BOGOYEVITCH MARIE A ET AL: "Peptide inhibitors of protein kinases - discovery, characterisation and use", BIOCHIMICA ET BIOPHYSICA ACTA, vol. 1754, no. 1-2, Sp. Iss. SI, December 2005 (2005-12-01), pages 79 - 99, XP002459976, ISSN: 1570-9639 *
CHEN Y ET AL: "Phosphorylation of the mitotic regulator protein Hec1 by Hek2kinase is essential for faithful chromosome segregation", JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY OF BIOLOCHEMICAL BIOLOGISTS, BIRMINGHAM,, US, vol. 277, no. 51, 20 December 2002 (2002-12-20), pages 49408 - 49416, XP002977113, ISSN: 0021-9258 *
DI AGOSTINO SILVIA ET AL: "Phosphorylation of high-mobility group protein A2 by Nek2 kinase during the first meiotic division in mouse spermatocytes.", MOLECULAR BIOLOGY OF THE CELL, vol. 15, no. 3, March 2004 (2004-03-01), pages 1224 - 1232, XP002459979, ISSN: 1059-1524 *
FRY A M ET AL: "ACTIVITY OF THE HUMAN CENTROSOMAL KINASE, NEK2, DEPENDS ON A UNUSUAL LEUCINE ZIPPER DIMERIZATION MOTIF", JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY OF BIOLOCHEMICAL BIOLOGISTS, BIRMINGHAM,, US, vol. 274, no. 23, 4 June 1999 (1999-06-04), pages 16304 - 16310, XP002905326, ISSN: 0021-9258 *
FRY ANDREW M ET AL: "Substrate specificity and cell cycle regulation of the Nek2 protein kinase, a potential human homolog of the mitotic regulatory NIMA of Aspergillus nidulans", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 270, no. 21, 1995, pages 12899 - 12905, XP002459975, ISSN: 0021-9258 *
FRY ANDREW M: "The Nek2 protein kinase: A novel regulator of centrosome structure", ONCOGENE, vol. 21, no. 40 Review Issue 4, 9 September 2002 (2002-09-09), pages 6184 - 6194, XP002459977, ISSN: 0950-9232 *
FRY ET AL: "C-Nap1, a Novel Centrosomal Coiled-Coil Protein and Candidate Substrate of the Cell Cycle-regulated Protein Kinase Nek2", THE JOURNAL OF CELL BIOLOGY, ROCKEFELLER UNIVERSITY PRESS, US, vol. 141, no. 7, 29 June 1998 (1998-06-29), pages 1563 - 1574, XP002133073, ISSN: 0021-9525 *
HELPS NICHOLAS R ET AL: "NIMA-related kinase 2 (Nek2), a cell-cycle-regulated protein kinase localized to centrosomes, is complexed to protein phosphatase 1", BIOCHEMICAL JOURNAL, vol. 349, no. 2, 15 July 2000 (2000-07-15), pages 509 - 518, XP002459990, ISSN: 0264-6021 *
JIN GUIXIAN ET AL: "Development and comparison of nonradioactive in vitro kinase assays for NIMA-related kinase 2", ANALYTICAL BIOCHEMISTRY, vol. 358, no. 1, November 2006 (2006-11-01), pages 59 - 69, XP002459982, ISSN: 0003-2697 *
LOU Y ET AL: "Nek2A specifies the centrosomal localization of Erk2", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, ACADEMIC PRESS INC. ORLANDO, FL, US, vol. 321, no. 2, 20 August 2004 (2004-08-20), pages 495 - 501, XP004522530, ISSN: 0006-291X *
NOGUCHI KOHJI ET AL: "Nucleolar Nek11 is a novel target of Nek2A in G1/S-arrested cells", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 279, no. 31, 30 July 2004 (2004-07-30), pages 32716 - 32727, XP002459980, ISSN: 0021-9258 *
YAO J ET AL: "Nek2A kinase regulates the localization of numatrin to centrosome in mitosis", FEBS LETTERS, ELSEVIER, AMSTERDAM, NL, vol. 575, no. 1-3, 24 September 2004 (2004-09-24), pages 112 - 118, XP004573866, ISSN: 0014-5793 *
YOO JAE CHEAL ET AL: "NIP1/XB51/NECAB3 is a potential substrate of Nek2, suggesting specific roles of Nek2 in Golgi.", EXPERIMENTAL CELL RESEARCH, vol. 292, no. 2, 15 January 2004 (2004-01-15), pages 393 - 402, XP002459978, ISSN: 0014-4827 *

Also Published As

Publication number Publication date
WO2007120463A2 (en) 2007-10-25

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