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1. WO2011132938 - GPCR-BPB SPECIFICALLY BINDING TO GPCR

Publication Number WO/2011/132938
Publication Date 27.10.2011
International Application No. PCT/KR2011/002838
International Filing Date 20.04.2011
IPC
C07K 1/107 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
107by chemical modification of precursor peptides
C40B 30/04 2006.1
CCHEMISTRY; METALLURGY
40COMBINATORIAL TECHNOLOGY
BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICO LIBRARIES
30Methods of screening libraries
04by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
C40B 40/10 2006.1
CCHEMISTRY; METALLURGY
40COMBINATORIAL TECHNOLOGY
BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICO LIBRARIES
40Libraries per se, e.g. arrays, mixtures
04Libraries containing only organic compounds
10Libraries containing peptides or polypeptides, or derivatives thereof
C12N 15/63 2006.1
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09Recombinant DNA-technology
63Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
CPC
A61K 47/64
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
62the modifying agent being a protein, peptide or polyamino acid
64Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 49/0002
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
0002General or multifunctional contrast agents, e.g. chelated agents
A61K 49/0056
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
001Preparation for luminescence or biological staining
0013Luminescence
0017Fluorescence in vivo
005characterised by the carrier molecule carrying the fluorescent agent
0056Peptides, proteins, polyamino acids
C07K 1/107
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
107by chemical modification of precursor peptides
C07K 14/705
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
705Receptors; Cell surface antigens; Cell surface determinants
C12N 15/63
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09Recombinant DNA-technology
63Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
Applicants
  • 광주과학기술원 GWANGJU INSTITUTE OF SCIENCE AND TECHNOLOGY [KR]/[KR] (AllExceptUS)
  • 전상용 JON, Sang Yong [KR]/[KR] (UsOnly)
  • 김성현 KIM, Sung Hyun [KR]/[KR] (UsOnly)
  • 박세호 PARK, Se Ho [KR]/[KR] (UsOnly)
  • 김대진 KIM, Dae Jin [KR]/[KR] (UsOnly)
  • 이상헌 LEE, Sang Heon [KR]/[KR] (UsOnly)
Inventors
  • 전상용 JON, Sang Yong
  • 김성현 KIM, Sung Hyun
  • 박세호 PARK, Se Ho
  • 김대진 KIM, Dae Jin
  • 이상헌 LEE, Sang Heon
Agents
  • 양부현 YANG, Boo-Hyun
Priority Data
10-2010-003659920.04.2010KR
Publication Language Korean (ko)
Filing Language Korean (KO)
Designated States
Title
(EN) GPCR-BPB SPECIFICALLY BINDING TO GPCR
(FR) GPCR-BPB SE LIANT SPÉCIFIQUEMENT À GPCR
(KO) GPCR에 특이적으로 결합하는 GPCR-BPB
Abstract
(EN) The present invention relates to a GPCR-bipodal peptide binder specifically binding to GPCR, comprising: (a) a structure stabilizing region comprising parallel, antiparallel, or parallel and antiparallel amino acid strands in which an interstrand noncovalent bond is formed; and (b) a GPCR-target binding region I and a GPCR-target binding region II which bind respectively to both ends of the structure stabilizing region and comprise randomly selected n and m amino acids, respectively. The GPCR-bipodal peptide binder of the present invention shows a very low level (for example, nM level) of KD value (dissociation constant) to GPCR, thereby showing very high affinity to a GPCR target. The GPCR-bipodal peptide binder of the present invention has medical use, can be used for in vivo molecular imaging, in vitro cell imaging and targeting for drug delivery, and also can be very usefully used as an escort molecule.
(FR) La présente invention concerne un lieur peptidique bipied de GPCR se liant spécifiquement à GPCR, comprenant : (a) une région de stabilisation de structure comprenant des brins d'acides aminés parallèles, antiparallèles, ou parallèles et antiparallèles dans lesquels une liaison non covalente inter-brins est formée ; et (b) une région de liaison cible de GPCR I et une région de liaison cible de GPCR II qui se lient respectivement aux deux extrémités de la région de stabilisation de structure et comprennent n et m acides aminés sélectionnés de façon aléatoire, respectivement. Le lieur peptidique bipied de GPCR de la présente invention présente un niveau très faible (par exemple, au niveau nM) de la valeur de KD (constante de dissociation) pour GPCR, de manière à présenter une affinité très élevée pour une cible GPCR. Le lieur peptidique bipied de GPCR de la présente invention a une utilisation médicale, peut être utilisé pour l'imagerie moléculaire in vivo, l'imagerie cellulaire in vitro et le ciblage pour administration de médicament, et peut également être utilisé très utilement en tant que molécule escorte.
(KO) 본 발명은 (a) 가닥간(interstrand) 비공유결합이 형성된 패러럴(parallel), 안티패러럴(antiparallel) 또는 패러럴(parallel)과 안티패러럴(antiparallel) 아미노산 가닥들을 포함하는 구조 안정화 부위(structure stabilizing region); 및 (b) 상기 구조 안정화 부위의 양 말단에 결합되어 있고 무작위적으로 선택된 각각 n 및 m개의 아미노산을 포함하는 GPCR-타겟 결합 부위 I(GPCR-target binding region I) 및 GPCR-타겟 결합 부위 Ⅱ(GPCR-target binding region Ⅱ)를 포함하는 GPCR에 특이적으로 결합하는 GPCR-바이포달 펩타이드 바인더에 관한 것으로서, 본 발명의 GPCR-바이포달 펩타이드 바인더는 GPCR에 대하여 매우 낮은 수준(예컨대, nM 수준)의 KD 값(해리상수)을 나타내어, GPCR 타겟에 매우 높은 친화도를 나타낸다. 본 발명의 GPCR-바이포달 펩타이드 바인더는 의약으로서의 용도를 가질 뿐만 아니라, 인 비보 분자 이미징, 인 비트로 세포 이미징 및 약물전달용 타겟팅을 하는 데 이용될 수 있으며, 에스코트 분자로도 매우 유용하게 이용될 수 있다.
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