DK2756310T3 - Screening for proteasom-deubiquitinerende inhibitor - Google Patents

Screening for proteasom-deubiquitinerende inhibitor Download PDF

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Publication number
DK2756310T3
DK2756310T3 DK12831894.6T DK12831894T DK2756310T3 DK 2756310 T3 DK2756310 T3 DK 2756310T3 DK 12831894 T DK12831894 T DK 12831894T DK 2756310 T3 DK2756310 T3 DK 2756310T3
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Denmark
Prior art keywords
proteasome
cells
ubiquitin
treated
activity
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DK12831894.6T
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English (en)
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Slavica Brnjic
Padraig D'arcy
Rolf Larsson
Stig Linder
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Vivolux Ab
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Publication of DK2756310T3 publication Critical patent/DK2756310T3/da

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    • 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
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase
    • 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
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5011—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing antineoplastic activity
    • 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
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/573—Immunoassay; Biospecific binding assay; Materials therefor for enzymes or isoenzymes
    • 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
    • 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
    • G01N2500/02—Screening involving studying the effect of compounds C on the interaction between interacting molecules A and B (e.g. A = enzyme and B = substrate for A, or A = receptor and B = ligand for the receptor)

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • Physics & Mathematics (AREA)
  • General Health & Medical Sciences (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • General Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Cell Biology (AREA)
  • Food Science & Technology (AREA)
  • Medicinal Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Toxicology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Claims (3)

1. Fremgangsmåde til screening af en forbindelse til bestemmelse af, om forbindelsen er en proteasom-deubiquitinerende inhibitor med høj specificitet, hvilken fremgangsmåde omfatter kontakt mellem forbindelsen og humane 19S-regula-toriske partikler (19S-RP) af 26S-proteasom og bestemmelse af, om forbindelsen inhiberer aktivitet af deubiquitinerende (DUB) enzymer UCHL5 og USP14, og et yderligere trin til bestemmelse af, om forbindelsen påvirker aktivitet af ikke-prote-asomale associerede DUB-enzymer, hvor inhibering af UCHL5- og USP14-aktivi-teter og upåvirket aktivitet af ikke-proteasomale associerede DUB-enzymer indikerer, at forbindelsen er en proteasom-deubiquitinerende inhibitor med høj specificitet.
2. Fremgangsmåde ifølge krav 1, ved hvilken de ikke-proteasomale associerede DUB-enzymer omfatter mindst ét medlem af gruppen bestående af UCHL1, UCHL3, USP2, USP7, USP8.
3. Fremgangsmåde ifølge ethvert af kravene 1 eller 2, ved hvilken bestemmelsen af inhiberingen af UCHL5- og USP14-aktiviteter gennemføres med en assay udført med humane 19S-RP, med ubiquitin-AMC eller HA-ubiquitin-vinylsulfon som substrat.
DK12831894.6T 2011-09-16 2012-09-06 Screening for proteasom-deubiquitinerende inhibitor DK2756310T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SE1100678 2011-09-16
PCT/SE2012/000129 WO2013039438A1 (en) 2011-09-16 2012-09-06 Proteasome deubiquinating inhibitor screening

Publications (1)

Publication Number Publication Date
DK2756310T3 true DK2756310T3 (da) 2017-07-17

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DK12831894.6T DK2756310T3 (da) 2011-09-16 2012-09-06 Screening for proteasom-deubiquitinerende inhibitor

Country Status (7)

Country Link
US (1) US9856511B2 (da)
EP (1) EP2756310B1 (da)
JP (1) JP6103722B2 (da)
DK (1) DK2756310T3 (da)
ES (1) ES2632786T3 (da)
PL (1) PL2756310T3 (da)
WO (1) WO2013039438A1 (da)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11092602B2 (en) 2015-07-06 2021-08-17 Whitehead Institute For Biomedical Research Methods and compositions relating to proteasome inhibitor resistance
WO2017066697A1 (en) * 2015-10-14 2017-04-20 Dou Qingping Treatments and diagnostics for cancers
SG11201907844TA (en) * 2017-01-30 2019-09-27 Up Therapeutics Inc Novel spiro and cyclic bis-benzylidine proteasome inhibitor for the treatment of cancer, diabetes and neurological disorders

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070292907A1 (en) 2005-10-03 2007-12-20 Yigong Shi Compositions and method for regulating ubiquitin-specific processing proteases
WO2008147536A1 (en) * 2007-05-24 2008-12-04 President And Fellows For Harvard College Methods and compositions for enhancing proteasome activity
MX336731B (es) * 2010-01-28 2016-01-28 Harvard College Composiciones y metodos para potenciar la actividad de proteasoma.

Also Published As

Publication number Publication date
EP2756310A1 (en) 2014-07-23
EP2756310B1 (en) 2017-05-03
US20140370528A1 (en) 2014-12-18
US9856511B2 (en) 2018-01-02
ES2632786T3 (es) 2017-09-15
JP2014526259A (ja) 2014-10-06
JP6103722B2 (ja) 2017-03-29
EP2756310A4 (en) 2015-04-15
PL2756310T3 (pl) 2017-09-29
WO2013039438A1 (en) 2013-03-21

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