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WO2003034071A3 - A method of forming a dynamic combinatorial library using a scaffold - Google Patents

A method of forming a dynamic combinatorial library using a scaffold Download PDF

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Publication number
WO2003034071A3
WO2003034071A3 PCT/EP2002/011520 EP0211520W WO03034071A3 WO 2003034071 A3 WO2003034071 A3 WO 2003034071A3 EP 0211520 W EP0211520 W EP 0211520W WO 03034071 A3 WO03034071 A3 WO 03034071A3
Authority
WO
WIPO (PCT)
Prior art keywords
scaffold
functionality
target
carrying
molecules
Prior art date
Application number
PCT/EP2002/011520
Other languages
French (fr)
Other versions
WO2003034071A2 (en
Inventor
Christoph Steeneck
Alexey V Eliseev
Matthias Hochguertel
Heiko Kroth
Original Assignee
Therascope Ag
Christoph Steeneck
Alexey V Eliseev
Matthias Hochguertel
Heiko Kroth
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 Therascope Ag, Christoph Steeneck, Alexey V Eliseev, Matthias Hochguertel, Heiko Kroth filed Critical Therascope Ag
Priority to AU2002346915A priority Critical patent/AU2002346915A1/en
Publication of WO2003034071A2 publication Critical patent/WO2003034071A2/en
Publication of WO2003034071A3 publication Critical patent/WO2003034071A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B30/00—Methods of screening libraries
    • C40B30/04—Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/52—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/16—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
    • C07K1/047—Simultaneous synthesis of different peptide species; Peptide libraries
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • 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
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6803—General methods of protein analysis not limited to specific proteins or families of proteins
    • G01N33/6845—Methods of identifying protein-protein interactions in protein mixtures
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/16—Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90—Enzymes; Proenzymes
    • G01N2333/914—Hydrolases (3)
    • G01N2333/924—Hydrolases (3) acting on glycosyl compounds (3.2)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/20—Screening for compounds of potential therapeutic value cell-free systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicinal Chemistry (AREA)
  • Biophysics (AREA)
  • Immunology (AREA)
  • Analytical Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Physics & Mathematics (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • General Engineering & Computer Science (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Cell Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Food Science & Technology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)

Abstract

The present invention relates to a method of forming a library of components which are potentially capable of binding to a target, which method comprises i) selecting a plurality of molecules carrying a functionality which may interact with a binding site of the said target, said molecules furthermore having a linking group which is capable of interacting with other linking groups under the formation of reversible bonds; ii) selecting a scaffold carrying two or more linking groups which are capable of interacting with the linking groups on the compound carrying a functionality; iii) reacting the scaffold and the molecules carrying the functionality in the presence of the target, under conditions where a formation of reversible bonds between the functionalities on the scaffold and on the molecules carrying a functionality occurs. In one embodiment of the present invention, the scaffold is designed to potentially interact with a binding site of known structure in a known target. The design, or pre-tailoring, of the scaffold will occur with respect to its size, three dimensional structure and/or flexibility. In a further embodiment of the present invention, the scaffold is designed to permit a screening against targets having a binding site of unknown structure, in particular to find components which are active in protein-protein-interactions.
PCT/EP2002/011520 2001-10-15 2002-10-15 A method of forming a dynamic combinatorial library using a scaffold WO2003034071A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002346915A AU2002346915A1 (en) 2001-10-15 2002-10-15 A method of forming a dynamic combinatorial library using a scaffold

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US32880201P 2001-10-15 2001-10-15
US60/328,802 2001-10-15
US35673102P 2002-02-15 2002-02-15
US60/356,731 2002-02-15

Publications (2)

Publication Number Publication Date
WO2003034071A2 WO2003034071A2 (en) 2003-04-24
WO2003034071A3 true WO2003034071A3 (en) 2004-03-11

Family

ID=26986521

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/EP2002/011526 WO2003033437A2 (en) 2001-10-15 2002-10-15 A method of forming neuraminidase inhibitors by dynamic combinatorial chemistry and compounds obtained
PCT/EP2002/011520 WO2003034071A2 (en) 2001-10-15 2002-10-15 A method of forming a dynamic combinatorial library using a scaffold

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/011526 WO2003033437A2 (en) 2001-10-15 2002-10-15 A method of forming neuraminidase inhibitors by dynamic combinatorial chemistry and compounds obtained

Country Status (2)

Country Link
AU (1) AU2002346915A1 (en)
WO (2) WO2003033437A2 (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003290304A1 (en) 2002-12-23 2004-07-14 Astex Technology Limited Synthesis and screening of ligands using x-ray crystallography
JP2007521252A (en) * 2003-04-11 2007-08-02 エスジーエックス ファーマシューティカルズ，インコーポレイティド Compound library and drug discovery method
EP1496039B1 (en) * 2003-07-11 2018-02-14 Kirschfeld, Andreas A method for the generation of a dynamic combinatorial library
EP1496038A1 (en) * 2003-07-11 2005-01-12 Therascope AG A method for the generation of a dynamic combinatorial library using nitrones
WO2009068321A1 (en) * 2007-11-26 2009-06-04 Forschungsverbund Berlin E.V. Site-directed high throughput screening
DE102011117128A1 (en) * 2011-10-28 2013-05-02 Christian-Albrechts-Universität Zu Kiel Compounds for the treatment of influenza
JP6754997B2 (en) * 2013-08-26 2020-09-16 国立大学法人 東京大学 A large cyclic peptide, a method for producing the same, and a screening method using a large cyclic peptide library.
CN107325040B (en) * 2016-04-28 2019-05-03 广州市恒诺康医药科技有限公司 Cyclohexene derivative or its pharmaceutically acceptable salt and application thereof

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995034577A1 (en) * 1994-06-16 1995-12-21 Smithkline Beecham Corporation Template directed cyclization
WO1997043232A1 (en) * 1996-05-14 1997-11-20 Hoechst Research & Technology Deutschland Gmbh & Co.Kg Novel substance library and supramolecular complexes produced therewith
WO1998054577A1 (en) * 1997-05-28 1998-12-03 Beth Israel Deaconess Medical Center, Inc. Cyclic peptide libraries and methods of use thereof to identify binding motifs
US5958702A (en) * 1995-02-06 1999-09-28 Benner; Steven Albert Receptor-assisted combinatorial chemistry
US6008058A (en) * 1993-06-18 1999-12-28 University Of Louisville Cyclic peptide mixtures via side chain or backbone attachment and solid phase synthesis
WO2001025257A2 (en) * 1999-10-04 2001-04-12 Neokimia, Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
EP1130009A1 (en) * 2000-03-01 2001-09-05 Therascope AG Generation and screening of a dynamic combinatorial library

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW477783B (en) * 1997-12-12 2002-03-01 Gilead Sciences Inc Novel compounds useful as neuraminidase inhibitors and pharmaceutical compositions containing same

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6008058A (en) * 1993-06-18 1999-12-28 University Of Louisville Cyclic peptide mixtures via side chain or backbone attachment and solid phase synthesis
WO1995034577A1 (en) * 1994-06-16 1995-12-21 Smithkline Beecham Corporation Template directed cyclization
US5958702A (en) * 1995-02-06 1999-09-28 Benner; Steven Albert Receptor-assisted combinatorial chemistry
WO1997043232A1 (en) * 1996-05-14 1997-11-20 Hoechst Research & Technology Deutschland Gmbh & Co.Kg Novel substance library and supramolecular complexes produced therewith
WO1998054577A1 (en) * 1997-05-28 1998-12-03 Beth Israel Deaconess Medical Center, Inc. Cyclic peptide libraries and methods of use thereof to identify binding motifs
WO2001025257A2 (en) * 1999-10-04 2001-04-12 Neokimia, Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
EP1130009A1 (en) * 2000-03-01 2001-09-05 Therascope AG Generation and screening of a dynamic combinatorial library

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
COUSINS G R L ET AL: "Molecular evolution: Dynamic combinatorial libraries, autocatalytic networks and the quest for molecular function", CURRENT OPINION IN CHEMICAL BIOLOGY 2000 UNITED KINGDOM, vol. 4, no. 3, 2000, pages 270 - 279, XP002256730, ISSN: 1367-5931 *
HUC IVAN ET AL: "Dynamic combinatorial chemistry", COMBINATORIAL CHEMISTRY AND HIGH THROUGHPUT SCREENING, vol. 4, no. 1, February 2001 (2001-02-01), pages 53 - 74, XP008022942, ISSN: 1386-2073 *
LEHN J-M: "DYNAMIC COMBINATORIAL CHEMISTRY AND VIRTUAL COMBINATORIAL LIBRARIES", PHYSICAL CHEMISTRY CHEMICAL PHYSICS, ROYAL SOCIETY OF CHEMISTRY, CAMBRIDGE, GB, vol. 5, no. 9, 1999, pages 2455 - 2463, XP009015591, ISSN: 1463-9076 *
SWANN P G ET AL: "NONSPECIFIC PROTEASE-CATALYZED HYDROLYSIS/SYNTHESIS OF A MIXTURE OF PEPTIDES: PRODUCT DIVERSITY AND LIGAND AMPLIFICATION BY A MOLECULAR TRAP", BIOPOLYMERS, NEW YORK, NY, US, vol. 40, no. 6, 1996, pages 617 - 625, XP009015590, ISSN: 0006-3525 *

Also Published As

Publication number Publication date
WO2003033437A2 (en) 2003-04-24
AU2002346915A1 (en) 2003-04-28
WO2003034071A2 (en) 2003-04-24
WO2003033437A3 (en) 2003-12-18

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