BRPI0606515A2 - estrutura de raios x de fpps humana e uso para selecionar compostos de ligação de fpps - Google Patents

estrutura de raios x de fpps humana e uso para selecionar compostos de ligação de fpps

Info

Publication number
BRPI0606515A2
BRPI0606515A2 BRPI0606515-5A BRPI0606515A BRPI0606515A2 BR PI0606515 A2 BRPI0606515 A2 BR PI0606515A2 BR PI0606515 A BRPI0606515 A BR PI0606515A BR PI0606515 A2 BRPI0606515 A2 BR PI0606515A2
Authority
BR
Brazil
Prior art keywords
fpps
human
select
crystals
binding compounds
Prior art date
Application number
BRPI0606515-5A
Other languages
English (en)
Inventor
Wolfgang Jahnke
Martin Geiser
Paul Ramage
Andre Strauss
Jean-Michael Rondeau
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of BRPI0606515A2 publication Critical patent/BRPI0606515A2/pt

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    • 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.)
    • C12N9/1085—Transferases (2.) transferring alkyl or aryl groups other than methyl groups (2.5)
    • 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
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C30—CRYSTAL GROWTH
    • C30B—SINGLE-CRYSTAL GROWTH; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL OR UNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL; REFINING BY ZONE-MELTING OF MATERIAL; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR
    • C30B29/00—Single crystals or homogeneous polycrystalline material with defined structure characterised by the material or by their shape
    • C30B29/54—Organic compounds
    • C30B29/58—Macromolecular compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2299/00—Coordinates from 3D structures of peptides, e.g. proteins or enzymes

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Zoology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Wood Science & Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Microbiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physics & Mathematics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Biophysics (AREA)
  • Plant Pathology (AREA)
  • Analytical Chemistry (AREA)
  • Materials Engineering (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)

Abstract

ESTRUTURA DE RAIOS X DE FPPS HUMANA E USO PARA SELECIONAR COMPOSTOS DE LIGAçãO DE FPPS. A presente invenção refere-se a sintase de difosfato de arnesila humana cristalina (FPPS), para a estrutura tridimensional de FPPS livre bem como as estruturas tridimensionais de FPPS em complexo com substratos tais como IPP (difosfato de isopentenila) e/ou com inibidores tais como Zometa(r) ou Aredia(r). Além disso, são descritos métodos para preparar cristais de FPPS humana. De acordo com a invenção os cristais podem ser usados para determinar as estruturas de homólogos de FPPS, mutantes, complexos com ligantes, formas de cristais de FPPS e moléculas similares de estrutura desconhecida. A invenção refere-se adicionalmente ao uso de cristais de FPPS para selecionar novos ligantes de FPPS, por exemplo, por varredura de raios X e para designar e/ou identificar inibidores contra FPPS. Além disso, a invenção refere-se a métodos de RMN para selecionar e/ou identificar novos ligantes de baixo peso molecular para FPPS, os quais representam novos agentes terapêuticos.
BRPI0606515-5A 2005-01-04 2006-01-02 estrutura de raios x de fpps humana e uso para selecionar compostos de ligação de fpps BRPI0606515A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US64117805P 2005-01-04 2005-01-04
PCT/EP2006/000002 WO2006072561A1 (en) 2005-01-04 2006-01-02 X-ray structure of human fpps and use for selecting fpps binding compounds

Publications (1)

Publication Number Publication Date
BRPI0606515A2 true BRPI0606515A2 (pt) 2009-06-30

Family

ID=35840678

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0606515-5A BRPI0606515A2 (pt) 2005-01-04 2006-01-02 estrutura de raios x de fpps humana e uso para selecionar compostos de ligação de fpps

Country Status (10)

Country Link
US (1) US20080139449A1 (pt)
EP (1) EP1836296A1 (pt)
JP (1) JP2008526185A (pt)
KR (1) KR20070100269A (pt)
CN (1) CN101098960A (pt)
AU (1) AU2006204523A1 (pt)
BR (1) BRPI0606515A2 (pt)
CA (1) CA2593713A1 (pt)
MX (1) MX2007008156A (pt)
WO (1) WO2006072561A1 (pt)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8618355B2 (en) 2008-03-17 2013-12-31 National Research Council Of Canada Aromatic prenyltransferase from hop
CN103172711B (zh) * 2011-12-20 2018-07-31 天津市国际生物医药联合研究院 SARS冠状病毒非结构蛋白nsp2的氨基端区域的表达纯化及其晶体结构

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Also Published As

Publication number Publication date
KR20070100269A (ko) 2007-10-10
MX2007008156A (es) 2007-07-24
EP1836296A1 (en) 2007-09-26
WO2006072561A1 (en) 2006-07-13
CN101098960A (zh) 2008-01-02
US20080139449A1 (en) 2008-06-12
CA2593713A1 (en) 2006-07-13
AU2006204523A1 (en) 2006-07-13
JP2008526185A (ja) 2008-07-24

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Legal Events

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B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]