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WO2001025410A3 - SONDES DE DIAGNOSTIC ET AGENTS THERAPEUTIQUES DESTINES A CIBLER uPA ET uPAR - Google Patents

SONDES DE DIAGNOSTIC ET AGENTS THERAPEUTIQUES DESTINES A CIBLER uPA ET uPAR Download PDF

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Publication number
WO2001025410A3
WO2001025410A3 PCT/US2000/026502 US0026502W WO0125410A3 WO 2001025410 A3 WO2001025410 A3 WO 2001025410A3 US 0026502 W US0026502 W US 0026502W WO 0125410 A3 WO0125410 A3 WO 0125410A3
Authority
WO
WIPO (PCT)
Prior art keywords
upa
residues
peptide
terminal fragment
upar
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/US2000/026502
Other languages
English (en)
Other versions
WO2001025410A2 (fr
Inventor
Andrew P Mazar
Terence R Jones
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.)
Angstrom Pharmaceuticals Inc
Original Assignee
Angstrom Pharmaceuticals Inc
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 Angstrom Pharmaceuticals Inc filed Critical Angstrom Pharmaceuticals Inc
Priority to JP2001528564A priority Critical patent/JP2003528035A/ja
Priority to CA002406882A priority patent/CA2406882A1/fr
Priority to AU79868/00A priority patent/AU780730B2/en
Priority to EP00970496A priority patent/EP1218496A2/fr
Publication of WO2001025410A2 publication Critical patent/WO2001025410A2/fr
Publication of WO2001025410A3 publication Critical patent/WO2001025410A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424—Serine endopeptidases (3.4.21)
    • C12N9/6456—Plasminogen activators
    • C12N9/6459—Plasminogen activators t-plasminogen activator (3.4.21.68), i.e. tPA
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/006—Biological staining of tissues in vivo, e.g. methylene blue or toluidine blue O administered in the buccal area to detect epithelial cancer cells, dyes used for delineating tissues during surgery
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/81—Protease inhibitors
    • C07K14/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
    • C07K14/811—Serine protease (E.C. 3.4.21) inhibitors
    • 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
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424—Serine endopeptidases (3.4.21)
    • C12N9/6456—Plasminogen activators
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21—Serine endopeptidases (3.4.21)
    • C12Y304/21069—Protein C activated (3.4.21.69)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Optics & Photonics (AREA)
  • Microbiology (AREA)
  • Oncology (AREA)
  • Biodiversity & Conservation Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biophysics (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

L'invention concerne une protéine ou un peptide destinés à cibler uPAR, qui est marqué(e) pour le diagnostic ou la thérapie et qui est utilisé(e) dans des procédés de diagnostic de thérapie. La protéine marquée ou le peptide marqué présente, de préférence, les propriétés suivantes: il/elle comprend au moins 38 restes d'acide aminé, dont les restes 13-30 du site de liaison à uPAR de uPA; il/elle est en compétition avec DFP-uPa marqué pour se lier à une cellule ou une molécule qui présente un site de liaison à uPA, et possède une valeur IC50 d'environ 10nM ou moins; et il n'est pas une protéine hybride dans laquelle le peptide uPA est fusionné avec une autre protéine ou un autre peptide non-uPA. Les molécules préférées sont uPA, scuPA, tcuPA, un fragment N-terminal de uPA, correspondant aux restes 1-135, un fragment N-terminal de uPA, correspondant aux restes 1-143, un fragment N-terminal de uPA, des restes 1-43 ; ou un fragment N-terminal de uPA, correspondant aux restes 4-43. Les marqueurs qui peuvent être détectés comprennent un radionucléide, un agent imageable par TEP, un agent imageable IRM, un agent fluorescent, un fluorogène, un chromophore, un chromogène, un agent phosphorescent, un chimiluminescent ou un bioluminescent. Les procédés selon la présente invention sont utilisés afin d'inhiber la migration cellulaire, l'invasion cellulaire, la prolifération cellulaire ou l'angiogenèse ou afin de produire l'apoptose, de préférence pour traiter un patient ayant une maladie ou un état pathologique liés à une migration cellulaire, une invasion cellulaire, une prolifération cellulaire ou une angiogenèse non désirées.
PCT/US2000/026502 1999-10-01 2000-09-27 SONDES DE DIAGNOSTIC ET AGENTS THERAPEUTIQUES DESTINES A CIBLER uPA ET uPAR Ceased WO2001025410A2 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
JP2001528564A JP2003528035A (ja) 1999-10-01 2000-09-27 ｕＰＡおよびｕＰＡＲを標的化する診断プロ−ブおよび治療薬
CA002406882A CA2406882A1 (fr) 1999-10-01 2000-09-27 Sondes de diagnostic et agents therapeutiques destines a cibler upa et upar
AU79868/00A AU780730B2 (en) 1999-10-01 2000-09-27 Diagnostic probes and therapeutics targeting uPA and uPAR
EP00970496A EP1218496A2 (fr) 1999-10-01 2000-09-27 SONDES DE DIAGNOSTIC ET AGENTS THERAPEUTIQUES DESTINES A CIBLER uPA ET uPAR

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15701299P 1999-10-01 1999-10-01
US60/157,012 1999-10-01

Publications (2)

Publication Number Publication Date
WO2001025410A2 WO2001025410A2 (fr) 2001-04-12
WO2001025410A3 true WO2001025410A3 (fr) 2002-01-10

Family

ID=22562008

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/026502 Ceased WO2001025410A2 (fr) 1999-10-01 2000-09-27 SONDES DE DIAGNOSTIC ET AGENTS THERAPEUTIQUES DESTINES A CIBLER uPA ET uPAR

Country Status (5)

Country Link
EP (1) EP1218496A2 (fr)
JP (1) JP2003528035A (fr)
AU (1) AU780730B2 (fr)
CA (1) CA2406882A1 (fr)
WO (1) WO2001025410A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111462491A (zh) * 2019-12-10 2020-07-28 北京航空航天大学 一种基于匝道控制的高速公路合流区交通冲突预警方法

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004527242A (ja) 2001-02-05 2004-09-09 イノベンタス プロジェクト アクチボラゲット ヒスチジンリッチ糖タンパク質
TWI284539B (en) 2001-07-30 2007-08-01 Epix Pharm Inc A method for making a magnetic resonance (MR) imaging agent, a MR imaging contrast agent, a method for altering stability of a peptide and a modified peptide
WO2004099780A1 (fr) * 2003-05-06 2004-11-18 Rigshospitalet Dosages immunologiques pour la detection de formes de recepteur d'urokinase
US6987270B2 (en) 2003-05-07 2006-01-17 General Electric Company Method to account for event losses due to positron range in positron emission tomography and assay of positron-emitting isotopes
AU2005287934B2 (en) * 2004-09-29 2009-03-26 Ge Healthcare As Urokinase plasminogen activator receptor targeted contrast agent
US20070190068A1 (en) * 2005-10-10 2007-08-16 Richard Hart uPAR-binding molecule-drug conjugates and uses thereof
DK1968648T3 (en) 2005-12-16 2015-07-27 Amit Shachaf Diagnostic system for the detection and diagnosis of skin cancer
JP5957085B2 (ja) * 2012-02-07 2016-07-27 Ｊｃｒファーマ株式会社 改善されたバイオアベイラビリティーのためにａｔｆと融合させた薬剤
CN104768573B (zh) 2012-05-08 2017-08-29 Trt创新有限责任公司 用于位点特异性uPAR靶向的177‑Lu标记肽
HUE066607T2 (hu) 2012-12-03 2024-08-28 Curasight As Pozitront emittáló radionukliddal jelölt peptidek humán uPAR PET-tel történõ leképezésére
WO2019067740A1 (fr) 2017-09-27 2019-04-04 Emory University Protéines de fusion comprenant une toxine et un marqueur de cancer, nanoparticules et utilisations associées
EP4610269A1 (fr) 2024-02-29 2025-09-03 3B Pharmaceuticals GmbH Ligands du recepteur de surface de l'activateur du plasminogene de l'urokinase (upar) utilises a des fins diagnostiques ou therapeutiques

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990012091A1 (fr) * 1989-04-07 1990-10-18 Cancerforskningsfondet Af 1989 Recepteur de l'activateur du plasminogene du type urokinase
WO1998021230A1 (fr) * 1996-11-12 1998-05-22 Angstrom Pharmaceuticals, Inc. Peptides cycliques se fixant a un recepteur de l'activateur de plasminogene de type urokinase
EP0890638A2 (fr) * 1996-01-08 1999-01-13 Nissin Food Products Co., Ltd. Inhibiteur de metastases cancereuses
WO1999048509A1 (fr) * 1998-03-23 1999-09-30 Rabbani Shafaat A Utilisation du recepteur des activateurs du plasminogene d'urokinase comme cible pour le depistage des metastases

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990012091A1 (fr) * 1989-04-07 1990-10-18 Cancerforskningsfondet Af 1989 Recepteur de l'activateur du plasminogene du type urokinase
EP0890638A2 (fr) * 1996-01-08 1999-01-13 Nissin Food Products Co., Ltd. Inhibiteur de metastases cancereuses
WO1998021230A1 (fr) * 1996-11-12 1998-05-22 Angstrom Pharmaceuticals, Inc. Peptides cycliques se fixant a un recepteur de l'activateur de plasminogene de type urokinase
WO1999048509A1 (fr) * 1998-03-23 1999-09-30 Rabbani Shafaat A Utilisation du recepteur des activateurs du plasminogene d'urokinase comme cible pour le depistage des metastases

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
APPELLA E ET AL: "THE RECEPTOR-BINDING SEQUENCE OF UROKINASE", JOURNAL OF BIOLOGICAL CHEMISTRY,US,AMERICAN SOCIETY OF BIOLOGICAL CHEMISTS, BALTIMORE, MD, vol. 262, no. 10, 5 April 1987 (1987-04-05), pages 4437 - 4440, XP000881270, ISSN: 0021-9258 *
DATABASE CAPLUS CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 1986, HIGGINS, D.L. ET AL.: "The incorporation of a fluorescent probe into the active sites of one- and two-chain tissue-type plasminogen activator.", XP002178460 *
PLOUG E A: "Photoaffinity labelling of the human receptor for urokinase-type plasminogen activator using a decapeptide antagonist. Evidence for a composite lignad-binding site and a short interdomain separation", BIOCHEMISTRY,US,AMERICAN CHEMICAL SOCIETY. EASTON, PA, vol. 37, no. 11, 17 March 1998 (1998-03-17), pages 3612 - 3622, XP002124882, ISSN: 0006-2960 *
See also references of EP1218496A2 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111462491A (zh) * 2019-12-10 2020-07-28 北京航空航天大学 一种基于匝道控制的高速公路合流区交通冲突预警方法
CN111462491B (zh) * 2019-12-10 2022-03-01 北京航空航天大学 一种基于匝道控制的高速公路合流区交通冲突预警方法

Also Published As

Publication number Publication date
AU780730B2 (en) 2005-04-14
WO2001025410A2 (fr) 2001-04-12
CA2406882A1 (fr) 2001-04-12
EP1218496A2 (fr) 2002-07-03
JP2003528035A (ja) 2003-09-24
AU7986800A (en) 2001-05-10

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