HUE035052T2 - Bakteriális gazdatörzs, amely rekombináns DSBC-t expresszál és csökkentett TSP-aktivitása van - Google Patents

Bakteriális gazdatörzs, amely rekombináns DSBC-t expresszál és csökkentett TSP-aktivitása van Download PDF

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Publication number
HUE035052T2
HUE035052T2 HUE10734333A HUE10734333A HUE035052T2 HU E035052 T2 HUE035052 T2 HU E035052T2 HU E10734333 A HUE10734333 A HU E10734333A HU E10734333 A HUE10734333 A HU E10734333A HU E035052 T2 HUE035052 T2 HU E035052T2
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HU
Hungary
Prior art keywords
allosteric
ssr
binding
fgfr
receptor
Prior art date
Application number
HUE10734333A
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English (en)
Inventor
Peter Carmeliet
Smet Frederik De
Joost Schymkowitz
Frederic Rousseau
Corentin Herbert
Original Assignee
Sanofi Sa
Vib Vzw
Life Sciences Res Partners Vzw
Univ Brussel Vrije
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 Sanofi Sa, Vib Vzw, Life Sciences Res Partners Vzw, Univ Brussel Vrije filed Critical Sanofi Sa
Publication of HUE035052T2 publication Critical patent/HUE035052T2/hu

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/473Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/71Receptors; Cell surface antigens; Cell surface determinants for growth factors; for growth regulators
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00Screening for compounds of potential therapeutic value
    • G01N2500/02Screening 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)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cell Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Toxicology (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Claims (5)

  1. BAKTERIÁLIS GAZÖATÖRZS« AMELY REKOMBINÁNS ÖS8C-T EXPRESSZÁL ÉS CSÖKKENTETT TSP«AKTIVITÁSA VAN Sza bad a hm igény po n tok í, Allosztéríkus inhibitor-kötőhely alkalmazása Í GÉR nem polimer, kisruolekulás, 1000 Da nái kisebb snolekuíaíőmegú inhibitorainak szkrinelésére, ahol az allosztéríkus inhibitor-kötőhely SEQ it) NO. I szerinti szekvenciából vagy SEQ 10 NO. 1 szeriüli szekvenciával legalább 70%-ban, 80%-ban, 90%-ban vagy 95%-ban homológ szekvenciából áll.
  2. 2. Eljárás feltételezett allosztéríkus inhibitor-kötőhely azonosítására FORE c-xtntcelluláris doménjében, amely tartalmazza a kővetkezőket; az exiracelluláris doménben frusztrált doménekre történő szkríneídst egy másodlagos fehérjeszerkezetet predikiáló program alkalmazásával olyan döntenek vagy fragmenseik azonosítására az exiracelluláris doménben, amelyek hajlamosak báta-redő aifa-héítx átmenetre, vagy amelyeknek olyan szerkezetük van, amelyet a másodlagos fehérjeszerkezetet predikiáló program a valós, kristályosítással és rőnlgenűitTntkeióval meghatározóit szerkezettel ellenttriotídónak prediktái, .és az így azonosított dóménak vagy fragmensek kiválasztását további szkrtnefésre a feltételezett bthlhi-torhely funkciójának megerősítésére vcgyületek, így kis molekulák, kis peptidek, pepiidomhnetikumok, anlites-lek vagy nanotesték tervezésével, amelyek kötődnek a helyhez, és amelyekkel az allosztéríkus mhibitortunkeió tesztelhető,
  3. 3, A 2, igénypont szerimi eljárás, ahoi az allosztéríkus kötőhely ínhibitorfunkciója a szabályozóit szignál-reakeiőutak szelektív gátlása.
  4. 4, Eljárás iirozínk máz-receptor extracelluláris doménjében allosztéríkus inhibitorhelyhez RTK-kötődés nem-polimer, kismolekuíás, allosztérikus inhibitorának azonosítására, amely tartalmazza a kővetkezőket: RTK allosztétikus kötőhelyének érinikeztetését a kismolekuíás, allosztéríkus inhibitorként feltételezett ve-gyülettel, és a tirozmkmáz-receptor aktlváíásátói/gátlásáíól lüggo, kél különböző, szabályozott reakcióid: által indukált legalább két különböző riporter állapotában bekövetkező változás összehssouíííását, ahol a nem-polimer, kismolekuíás inhibitor molekulatömege kisebb, mint i 000 Da,
  5. 5. A 4, igénypont szerinti eljárás, ttboi allosztéríkus inhibitort azonosítunk, amikor a receptor ligandkőfö donténjéhez kötődő Ügand jelenlétében legalább egy szabályozott reakcióüt gátolt, miközben legalább egy má-sík, szabályozott reakcióút nem érintett. ő. .A 4, vagy 5 , igénypont szerinti eljárá;;, amelyben a iirozinkÍnáz-inhíbhor FGRP, 7. A 6. igénypont szerinti eljárás, ahol az EGFR a következők egyikeként választott: FGFR-1, FGFR-2. FGFÏG3 vagy FGFR-4. S. A 4-7. igénypontok bármelyike szerinti eljárás RTK allosztéríkus inhibitorának azonosítására. ahol a két különböző, szabályozott reakcióul megfelel az. ERK1/2 szígriái-reakcíóútnnk és a PI.Cv szignál-reakcióütnak.
HUE10734333A 2009-07-03 2010-07-02 Bakteriális gazdatörzs, amely rekombináns DSBC-t expresszál és csökkentett TSP-aktivitása van HUE035052T2 (hu)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09290537A EP2270043A1 (en) 2009-07-03 2009-07-03 Extracellular allosteric inhibitor binding domain from a tyrosine kinase receptor

Publications (1)

Publication Number Publication Date
HUE035052T2 true HUE035052T2 (hu) 2018-05-02

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HUE10734333A HUE035052T2 (hu) 2009-07-03 2010-07-02 Bakteriális gazdatörzs, amely rekombináns DSBC-t expresszál és csökkentett TSP-aktivitása van

Country Status (17)

Country Link
US (2) US9234025B2 (hu)
EP (2) EP2270043A1 (hu)
JP (2) JP6255156B2 (hu)
KR (1) KR101828092B1 (hu)
CN (1) CN102596991B (hu)
AU (1) AU2010267590B2 (hu)
BR (1) BR112012000029B8 (hu)
CA (1) CA2766972C (hu)
DK (1) DK2448964T3 (hu)
ES (1) ES2631452T3 (hu)
HU (1) HUE035052T2 (hu)
IL (1) IL217155B (hu)
MX (1) MX345715B (hu)
MY (1) MY158993A (hu)
RU (1) RU2604805C2 (hu)
SG (2) SG177427A1 (hu)
WO (1) WO2011001413A1 (hu)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2985258A1 (fr) * 2011-12-28 2013-07-05 Sanofi Sa Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
WO2015127242A1 (en) * 2014-02-21 2015-08-27 President And Fellows Of Harvard College De novo design of allosteric proteins
KR102344105B1 (ko) 2014-08-18 2021-12-29 에자이 알앤드디 매니지먼트 가부시키가이샤 모노시클릭 피리딘 유도체의 염 및 이의 결정
WO2018081534A1 (en) 2016-10-28 2018-05-03 President And Fellows Of Harvard College Assay for exo-site binding molecules
CN111107881A (zh) * 2017-06-22 2020-05-05 密执安州立大学董事会 成纤维细胞生长因子受体2特异性肽试剂和方法
US11548931B2 (en) 2017-11-16 2023-01-10 Xl-Protein Gmbh PASylated VEGFR/PDGFR fusion proteins and their use in therapy
MX2020008610A (es) 2018-03-28 2020-09-21 Eisai R&D Man Co Ltd Agente terapeutico para carcinoma hepatocelular.
CN113651662B (zh) * 2020-12-31 2023-10-27 复旦大学附属华山医院 一种靶向fgfr的新型肿瘤pet分子探针及其制备方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20030004397A (ko) * 2000-05-11 2003-01-14 와이어쓰 G-단백질(rgs4)의 구조 및 이를 사용한 효능제 및길항제의 동정 방법
US7393656B2 (en) * 2001-07-10 2008-07-01 The Board Of Trustees Of The Leland Stanford Junior University Methods and compositions for risk stratification
FR2838123B1 (fr) * 2002-04-04 2005-06-10 Sanofi Synthelabo Nouveaux derives d'indolozine-1,2,3 substituee, inhibiteurs selectifs du b-fgf
US7083933B1 (en) * 2003-05-09 2006-08-01 Prosidion Limited Methods for identification of modulators of OSGPR116 activity
CA2550245A1 (en) * 2003-12-19 2005-07-21 Five Prime Therapeutics, Inc. Fibroblast growth factor receptors 1, 2, 3, and 4 as targets for therapeutic intervention
FR2865934B1 (fr) * 2004-02-05 2006-05-05 Sanofi Synthelabo Utilisation de derives d'indolizine 1,2,3 substitues, inhibiteurs des fgfs, pour la preparation de medicaments utiles pour le traitement de maladies liees a une angiogenese pathologique choroidienne
NZ551832A (en) * 2004-06-09 2010-01-29 Univ Edinburgh Neural stem cells
EP1885708A2 (en) * 2005-04-15 2008-02-13 Board of Trustees of Michigan State University Gpcr modulators
FR2896247B1 (fr) 2006-01-13 2008-02-29 Sanofi Aventis Sa Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique
EP1891955A1 (en) * 2006-07-24 2008-02-27 Sanofi-Aventis Use of 1,2,3-substituted indolizine derivatives, inhibitors of FGFs, for the preparation of a medicament intended for the treatment of degenerative joint diseases

Also Published As

Publication number Publication date
DK2448964T3 (en) 2017-07-24
SG10201403778TA (en) 2014-10-30
EP2270043A1 (en) 2011-01-05
EP2448964B1 (en) 2017-04-12
CN102596991A (zh) 2012-07-18
JP2012532121A (ja) 2012-12-13
CN102596991B (zh) 2016-06-08
MX345715B (es) 2017-02-13
AU2010267590A1 (en) 2012-02-02
MX2012000298A (es) 2013-05-30
CA2766972A1 (en) 2011-01-06
IL217155B (en) 2019-01-31
MY158993A (en) 2016-11-30
EP2448964A1 (en) 2012-05-09
WO2011001413A1 (en) 2011-01-06
KR20120093146A (ko) 2012-08-22
US20160193192A1 (en) 2016-07-07
RU2012103542A (ru) 2013-08-10
US20120094864A1 (en) 2012-04-19
IL217155A0 (en) 2012-02-29
JP2017036305A (ja) 2017-02-16
ES2631452T3 (es) 2017-08-31
BR112012000029B1 (pt) 2020-12-08
BR112012000029B8 (pt) 2021-05-25
SG177427A1 (en) 2012-02-28
KR101828092B1 (ko) 2018-02-09
US9234025B2 (en) 2016-01-12
JP6255156B2 (ja) 2017-12-27
AU2010267590B2 (en) 2016-08-04
RU2604805C2 (ru) 2016-12-10
CA2766972C (en) 2019-03-05
BR112012000029A2 (pt) 2016-11-08

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