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HGF binding peptides labeled for imaging
专利权人:
GE HEALTHCARE AS
发明人:
JOHANNESEN, EDVIN WILHELM,CUTHBERTSON, ALAN
申请号:
ES08750628
公开号:
ES2385066T3
申请日:
2008.05.16
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
An imaging agent comprising a conjugate of Formula I: wherein: Z1 is attached to the N-terminal end of cMBP, and is H or MIG; Z2 is fixed to the C-terminal end of cMBP and is OH, OBC or MIG, in which Bc is a biocompatible cation; cMBP is a cyclic cMet binding peptide of 17 to 30 amino acids comprising the amino acid sequence (SEC-1): Cysa-X1-Cysc-X2-Gly-Pro-Pro-X3-Phe-Glu-Cysd-Trp- Cysb-Tyr-X4-X5-X6; in which X1 is Asn, His or Tyr; X2 is Gly, Ser, Thr or Asn; X3 is Thr or Arg; X4 is Ala, Asp, Glu, Gly or Ser; X5 is Ser or Thr; X6 is Asp or Glu; and Cysa-d are each cysteine residues so that those residues a and b as well as c and d are cycled to form two different disulfide bonds; MIG is a metabolism inhibitor group that is a biocompatible group that inhibits or suppresses the peptide's in vivo metabolism; L is a synthetic linker group of the formula - (A) m- in which each A is independently -CR2-, -CR>; = CR-, -C≡C-, -CR2CO2-, -CO2CR2-, -NRCO- , -CONR-, -NR (C>; = O) NR-, -NR (C>; = S) NR-, -SO2NR-, -NRSO2-, -CR2OCR2-, -CR2SCR2-, -CR2NRCR2-, a cycloheteroalkylene group C4-8, a C4-8 cycloalkylene group, a C5-12 arylene group, or a C3-12 heteroarylene group, an amino acid, a sugar or a single component polyethylene glycol (PEG) basic component; each R is independently selected from H, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, C 1-4 alkoxyalkyl or C 1-4 hydroxyalkyl, m is an integer from 1 to 20; n is an integer of a value of 0 or 1; IM is an optical imaging indicator moiety suitable for imaging the body of mammals in vivo using light of a near-infrared green wavelength of 600-1,200 nm.Un agente de formación de imágenes que comprende un conjugado de Fórmula I: en la que: Z1 está fijado al extremo N-terminal de cMBP, y es H o MIG;Z2 está fijado al extremo C-terminal de cMBP y es OH, OBC o MIG, en la que Bc es un catión biocompatible; cMBP es un péptido cíclico de unión a cMet de 17 a 30 aminoácidos que comprende la secuencia de aminoácidos (SEC-1): Cysa-X1-Cysc-X
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中国工程科技知识中心
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