ME02935B - Vezujući domen bakterijske atp sintaze - Google Patents

Vezujući domen bakterijske atp sintaze

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Publication number
ME02935B
ME02935B MEP-2017-214A MEP21417A ME02935B ME 02935 B ME02935 B ME 02935B ME P21417 A MEP21417 A ME P21417A ME 02935 B ME02935 B ME 02935B
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ME
Montenegro
Prior art keywords
amino acids
dimensional structure
mutated
atpe
test compound
Prior art date
Application number
MEP-2017-214A
Other languages
English (en)
Inventor
J -M E F M Neefs
Peter K M Verhasselt
Johann Winkler
Hinrich W H Göhlmann
K J L M Andries
Jonge Marc René De
Lucien Maria Henricus Koymans
Original Assignee
Janssen Pharmaceutica Nv
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.)
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Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of ME02935B publication Critical patent/ME02935B/me

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    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09Recombinant DNA-technology
    • C12N15/11DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/52Genes encoding for enzymes or proenzymes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/195Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from bacteria
    • C07K14/35Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from bacteria from Mycobacteriaceae (F)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/06Antibacterial agents for tuberculosis
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09Recombinant DNA-technology
    • C12N15/11DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14Hydrolases (3)
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Medicinal Chemistry (AREA)
  • Wood Science & Technology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Plant Pathology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Analytical Chemistry (AREA)
  • Food Science & Technology (AREA)
  • Epidemiology (AREA)
  • Cell Biology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)

Claims (14)

1. Izolovan mutiran atpE protein koji obuhvata polipeptidnu sekvencu izabranu od SEQ ID NO O l koja obuhvata barem jednu tačkastu mutaciju koja se nalazi na bilo kom vezu jućem mestu ATPaze koje se nalazi između aminokiselina 14 do 34 ili između aminokiselina 54 do 69, i SEQ ID NO 03 koja obuhvata barem jednu tačkastu mutaciju koja se nalazi na bilo kojoj aminokiselini 20 do 40, ili ili aminokiselinama 60 do 75, gde navedeni protein indukuje rezistenciju na anti-mikrobsko jedinjenje DARQ J sa Slike l.
2. Izolovan mutiran atpE protein prema patentnom zahtevu l koji obuhvata polipeptidnu sekvencu izabranu iz grupe koju čine SEQ ID NO O 1 koj i obuhvata barem jednu tačkastu mutaciju koja se nalazi na aminokiselini 28 ili aminokiselini 63.
3. Izolovan mutiran atpE protein prema patentnom zahtevu l ili 2, izabran od Mtb_R kako je prikazano u SEQ ID No. 2, Msm R09 kako je prikazano u SEQ ID No.4, Ms m_ Rl O kako je prikazano u SEQ ID No.5.
4. Primena polipeptida prema bilo kom patentnom zahtevu od l do 3 u postupku za identifikovanje jedinjenja koja interakuju saFo delom ATPaze i za njihov potencijal kao antimikrobna jedin jenja.
5. Postupak procene potencijalnog test jedin jenja da interakuje sa atp E proteinom, gde navedeni postupak obuhvata; -tehnike molekularnog modeliranja za generisanje trodimenzionalne strukture mesta vezivanja prema bilo kom patentnom zahtevu od l do 3; - upotreba računskih sredstava za obavljanje operacije uklapanja između test jedinjenja i trodimenzionalne strukture mesta vezivanja; i - analiziranje rezultata pomenute operacije uklapanja za kvantifikaciju udruživanja test jedin jenja sa trodimenzionalnom strukturom mesta vezivanja.
6. Postupak prema patentnom zahtevu 5 gde je trodimenzionalna struktura generisana barem sa aminokiselinama Ala24, Gly27, Phe53, Va157, Gly58, Glu61, Tyr64 i Phe65 jedne C podjedinice i aminokiselinama Ser182, Leu183, Leu185, i Arg186 jedne A podjedinice, koristeći atomske koordinate bilo koje od Tabela 3, 4 ili 5 ili homologne strukturne koordinate koje sadrže koren srednjeg kvadratnog odstupanja ne-vodoničnih atoma od manje od oko 1,5A
7. Postupak prema patentnom zahtevu 5 gde je trodimenzionalna struktura generisana koristeći atomske koordinate ili aminokiseline Ala21, Gly25 od A Lanca bilo koje od Tabela 3, 4 ili 5; aminokiseline Ala24, Gly27, Phe53, Phe54, Val57, Gly58, Glu61 , Tyr64, Phe65 od K Lanca bilo koje od Tabela 3, 4 ili 5; aminokiseline Met17, Gly19 GJ20, AJa21, Ile22, Gly23, Ala24, GJy25, Ile26, Gly27, Asp28, Gly29, Ala31, Phe53, Thr56, VaJI 7, Gly58, Leu59 Val60, Glu61, Ala62, Ala63/Pro63, Tyr64, Phe65 od L Lanca bilo koje od Tabela 3, 4 ili 5; i ili aminokiseline Ser182, Leu 183, Leu185, i Arg186 od M Lanca bilo koje od Tabela 3, 4 ili 5.
8. Izolovanu sekvencu nukleinske kiseline koja kodira izolovan mutiran atpE protein prema bilo kom patentnom zahtevu od l do 3.
9.Vektor koji obuhvata sekvencu nukleinske kiseline prema patentnom zahtevu 8.
10.Ćelija domaćin koja nosi vektor prema patentnom zahtevu 9
11. Postupak za identifikovanje anti-mikrobnog jedin jenja, gde navedeni postupak obuhvata a) dovođenje u dodir ćelije koja eksprimira atpE protein sa test jedin jen jem pod fiziološkim uslovima, i b) određivanje da li testjedinjenje interakuje sa atpE proteinom gde je atpE protein mutiran atpE protein prema bilo kom patentnom zahtevu od 1 do 3.
12. Postupak za procenu potencijalnog test jedin jenja da interakuje sa mutiranim atpE proteinom prema bilo kom patentnom zahtevu od 1 do 3, gde navedeni postupak obuhvata;a) tehnike molekularnog modeliranja za generisanje trodimenzionalne strukture mutiranog atpE proteina prema bilo kom patentnom zahtevu od l do 3, b) upotreba računskih sredstava za obavljanje operacije uklapanja između test jedinjenja i trodimenzionalne strukture mutiranog atpE proteina prema patentnim zahtevima l do 3, i e) analiziranje rezultata pomenute operacije uklapanja za kvantifikaciju udruživanja test jedinjenja sa trodimenzionalnom strukturom mutiranog atpE protein prema patentnim zahtevima 1 do 3.
13. Postupak prema patentnom zahtevu 12 gde je trodimenzionalna struktura atpE proteina generisana koristeći atomske koordinate Ile28, Glu61 i Ile63 od E. coli (Protein Database l QO l) +/- koren srednje srednje kvadratne devijacije kičme atoma navedenih aminokiselina od ne više od l OA.
14. Postupak prema patentnom zahtevu 12 gde je trodimenzionalna struktura atpE proteina generisana koristeći atomske koordinate prema Tabelama 6 ili 7 +/- koren srednje srednje kvadratne devijacije kičme atoma navedenih aminokiselina od ne više od l ,5A.
MEP-2017-214A 2004-09-28 2005-09-28 Vezujući domen bakterijske atp sintaze ME02935B (me)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP04104720 2004-09-28
EP05794520.6A EP1797115B1 (en) 2004-09-28 2005-09-28 A bacterial atp synthase binding domain
PCT/EP2005/054893 WO2006035051A1 (en) 2004-09-28 2005-09-28 A bacterial atp synthase binding domain
US201861620500P 2018-01-10 2018-01-10

Publications (1)

Publication Number Publication Date
ME02935B true ME02935B (me) 2018-04-20

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US (2) US8088891B2 (me)
EP (1) EP1797115B1 (me)
JP (2) JP2008515395A (me)
KR (1) KR101539021B1 (me)
CN (1) CN101065397B (me)
AU (2) AU2005288848A1 (me)
CA (1) CA2579971C (me)
CY (1) CY1119568T1 (me)
DK (1) DK1797115T3 (me)
ES (1) ES2636980T3 (me)
HR (1) HRP20171388T1 (me)
HU (1) HUE033609T2 (me)
IL (1) IL182185A (me)
LT (1) LT1797115T (me)
ME (1) ME02935B (me)
NO (1) NO342699B1 (me)
NZ (1) NZ553693A (me)
PL (1) PL1797115T3 (me)
PT (1) PT1797115T (me)
RS (1) RS56357B1 (me)
RU (1) RU2418001C2 (me)
SI (1) SI1797115T1 (me)
WO (1) WO2006035051A1 (me)
ZA (1) ZA200702540B (me)

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GB2440736A (en) * 2006-08-10 2008-02-13 Medical Res Council Crystals of mutant p53 polypeptidtes
JO2970B1 (en) 2006-12-06 2016-03-15 جانسين فارماسوتيكا ان. في Quinoline antibacterial derivatives
JO3271B1 (ar) 2006-12-06 2018-09-16 Janssen Pharmaceutica Nv مشتقات الكوينولين المضادة للجراثيم
JO2685B1 (en) 2006-12-06 2013-03-03 جانسين فارماسوتيكا ان في Quinoline antibacterial derivatives
CN104254528B (zh) 2012-04-27 2017-06-06 詹森药业有限公司 抗菌的喹啉衍生物
US9133167B2 (en) 2012-04-27 2015-09-15 Janssen Pharmaceutica Nv Antibacterial quinoline derivatives
US8454434B1 (en) * 2012-06-15 2013-06-04 Igt Gaming system and method for providing an offer and acceptance game with progressive awards associated with a quantity of progressive tokens
JP5580383B2 (ja) 2012-10-05 2014-08-27 株式会社 資生堂 美容機器及び通電方法及び記録媒体
KR101522087B1 (ko) * 2013-06-19 2015-05-28 삼성에스디에스 주식회사 미스매치를 고려한 염기 서열 정렬 시스템 및 방법
CN110373399B (zh) * 2019-07-09 2021-05-28 湖南省植物保护研究所 一种沼泽红假单胞菌Atps2蛋白及其制备方法和应用

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KR100257418B1 (ko) 1991-11-01 2000-05-15 로렌스 티. 마이젠헬더 치환된 아릴-및 헤테로아릴-페닐옥사졸리디논
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AU2002951853A0 (en) * 2002-10-04 2002-10-24 Commonwealth Scientific And Industrial Research Organisation Crystal structure of erbb2 and uses thereof

Also Published As

Publication number Publication date
RU2007116144A (ru) 2008-11-10
EP1797115A1 (en) 2007-06-20
CA2579971C (en) 2018-02-13
HRP20171388T1 (hr) 2017-11-03
CY1119568T1 (el) 2018-03-07
EP1797115B1 (en) 2017-06-21
KR101539021B1 (ko) 2015-07-23
NO342699B1 (no) 2018-07-09
US8378085B2 (en) 2013-02-19
PT1797115T (pt) 2017-08-29
IL182185A (en) 2017-12-31
WO2006035051A1 (en) 2006-04-06
AU2012216368A1 (en) 2012-09-13
HK1114619A1 (zh) 2008-11-07
CN101065397A (zh) 2007-10-31
NZ553693A (en) 2012-05-25
US8088891B2 (en) 2012-01-03
RS56357B1 (sr) 2017-12-29
PL1797115T3 (pl) 2017-12-29
KR20070073823A (ko) 2007-07-10
JP5837852B2 (ja) 2015-12-24
SI1797115T1 (sl) 2017-10-30
JP2012210210A (ja) 2012-11-01
RU2418001C2 (ru) 2011-05-10
US20090298874A1 (en) 2009-12-03
JP2008515395A (ja) 2008-05-15
ES2636980T3 (es) 2017-10-10
NO20072237L (no) 2007-06-25
CA2579971A1 (en) 2006-04-06
AU2012216368B2 (en) 2017-04-13
IL182185A0 (en) 2007-07-24
LT1797115T (lt) 2017-10-10
ZA200702540B (en) 2008-08-27
CN101065397B (zh) 2015-10-21
US20120219964A1 (en) 2012-08-30
AU2005288848A1 (en) 2006-04-06
DK1797115T3 (en) 2017-10-02
HUE033609T2 (en) 2017-12-28

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