Neurotensin-derived branched peptides and uses thereof

A use and molecular technology, applied in the field of branched peptides, can solve problems such as insufficient activity

Inactive Publication Date: 2011-12-07
路易莎·布拉奇 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, 6-mercaptopurine bound to neurotensin through a 'non-cleavable' linker is completely non-toxic, while the drug bound to neurotensin through a 'cleavable' linker is active, However, the resulting activity was not sufficient to warrant further development

Method used

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  • Neurotensin-derived branched peptides and uses thereof
  • Neurotensin-derived branched peptides and uses thereof
  • Neurotensin-derived branched peptides and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0040] peptide synthesis

[0041] Tetrabranched NT(8-13)-PEG-K(PEG_fluorescein)[NT4(8-13)-Fluo]1, NT(8-13)-PEG-chlorambucil[NT4 (8-13)-CLB] 2, four-branched NT(8-13)-PEG-5-fluorodeoxyuridine [NT4(8-13)-5-FdU]3, four-branched NT(8 -13)-PEG-6-mercaptopurine [NT4(8-13)-6-MP]4, four-branched NT(8-13)-PEG-combretastatin [NT4(8-13)-CBTST] 5. Four-branched NT(8-13)-PEG-monostin [NT4(8-13)-Mon] 6. Four-branched NT(8-13)-PEG-tirapazamine [NT4( 8-13)-TPZ]7, four-branched NT(8-13)-PEG-DOTA [NT4(8-13)-DOTA]8 and four-branched NT(8-13)-PEG-DOTA Statin ether [NT4(8-13)-O-CBTST]9, and tetrabranched NT(8-13)-PEG-monostar ether [NT4(8-13)-O-Mon]10( figure 1 ), Fmoc-Lys(Dde)-OH applied on Novasyn TGR resin as the first amino acid and β-Ala as the second amino acid, wherein the second amino acid of [NT4(8-13)-Fluo]1 is Fmoc-PEG -OH, instead of β-Ala. The tetramer was then constructed as above, but with Boc-Arg(Pbf)-OH as the last amino acid of the neurotensin sequence, so that the last two ...

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Abstract

The present invention relates to a multimeric molecule having the general formula (A) or (B): and its use in the diagnosis and / or therapy of tumors

Description

Field of Invention [0001] The present invention relates to in vivo stable branched peptides derived from the neurotensin (NT) sequence. The peptides can be combined with functional units to specifically target cancer cells. They can therefore be used in the diagnosis and / or treatment of tumors. Background technique [0002] A major problem in classical chemotherapy is the non-specific toxicity of most anticancer agents even to normal cells. Therefore, specific targeting of tumors is an important challenge in cancer therapy and diagnostic research. [0003] Currently, innovative tumor-specific therapies follow the strategy of targeting tumor-associated proteins specifically expressed or overexpressed on tumor cells. [0004] Observation of receptors for different endogenous regulatory peptides expressed in a large number of primary human cancers reveals new perspectives for tumor-selective targeting using synthetic peptides 1-3 . [0005] Neurotensin (NT) is a 13 amino a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48
CPCA61K47/48253A61K49/0043A61K49/0056A61K38/00G01N33/574C07K7/083A61K49/0002A61K47/641A61P1/04A61P1/18A61P13/08A61P35/00
Inventor 路易莎·布拉奇亚历山德罗·皮尼基娅拉·法尔恰尼斯特凡诺·梅尼切蒂
Owner 路易莎·布拉奇
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