FIELD: medicine.
SUBSTANCE: technique involves presenting an individual having a detectable amount of a compound of formula I administered, enabling the compound of formula I being bound to activated integrin expressing hepatocytes, in the liver, detecting the signals given by the compound of formula I, using the visualisation technique in vivo, and generating an image displaying the location and/or value of the above signals. The compound of formula I represents a compound (I) , wherein: G is glycine; D is aspartic acid; X1 represents an amino acid, X2 and X4 independently represent amino acid residues side chains of which are coupled together and form a cyclising bridge, X3 is arginine, M is methylarginine or an arginine mimetic; X5 is tyrosine, phenylalanine, 3-iosine-tyrosine, C4-6cycloalkylalanine or naphthylalanine; X6 is a thiol containing amino acid. W1 and W2 independently represent an optional linker group, wherein the above linker group represents a radical of formula -(L)1-15-. L independently represents -C(=O)-, -CR'2-, -CR'=CR'-, -C=C-, -CR'2CO2-, -CO2CR'2-, -NR'-, -NR'CO-, -CONR'-, -NR'(C=O)NR', -NR'(C=S)NR'-, -SO2NR'-, -NR'SO2-, -CR'2OCR2, -CR'2SCR'2-, -CR'2NR'CR'2-, C4-8cycloheteroalkylene group, C4-8cycloalkylene group, C6-12arylene group, C3-12 heteroarylene group, an amino acid group, polyalkylene glycol, polylactic acid or polyglycolic acid. Each group R' independently represents H or C1-10alkyl, C3-10alkylaryl, C2-10alkoxyalkyl, C1-10hydroxyalkyl, C1-10fluoroalkyl, or 2 or more groups R' together with the atoms whereto attached form a carbocyclic, heterocyclic saturated or unsaturated ring. Z1 and Z2 independently contain a visualising group, a sugar group or an organic dye group, or hydrogen, provided at least one of Z1 and Z2 contains the visualising group.
EFFECT: diagnosing early hepatic fibrosis.
9 cl, 5 dwg, 6 tbl, 10 ex
Title | Year | Author | Number |
---|---|---|---|
PEPTIDE-BASED COMPOUNDS FOR DIRECTED TRANSPORT TO INTEGRIN RECEPTORS | 2002 |
|
RU2303042C2 |
DIAGNOSTIC COMPOUNDS | 2005 |
|
RU2396272C9 |
PEPTIDE COMPOUNDS | 2005 |
|
RU2393167C2 |
OPTICAL VISUALISATION AGENTS | 2008 |
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RU2484111C9 |
PEPTIDE COMPOSITION OF RADIOACTIVE INDICATORS | 2011 |
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RU2594167C2 |
IMPROVED CONJUGATES N4 OF CHELATING AGENTS | 2005 |
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MARKED PEPTIDES BINDING HEPATOCYTE GROWTH FACTOR (HGF) FOR VISUALISATION | 2008 |
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RU2473361C9 |
IMPROVED CHELATE CONJUGATES | 2002 |
|
RU2298012C2 |
OPTICAL AGENTS OF VISUALISATION | 2008 |
|
RU2475266C2 |
VISUALISATION AGENTS | 2004 |
|
RU2355702C2 |
Authors
Dates
2014-01-27—Published
2008-11-19—Filed