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Cyclic peptides binding CXCR4 receptor and relative medical and diagnostic uses

A technology for receptors, cyclic monomers, and applications in the field of cyclic peptides that bind to the CXCR4 receptor and relative medical and diagnostic applications

Inactive Publication Date: 2013-01-09
CONSIGLIO NAT DELLE RICERCHE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] Although AMD3100, given the data specified above, proved to be a rapid and effective locomotor agent, it was, however, revealed in previous studies, poor bioavailability, hepatic, cardiac and cerebellar toxicity [4]

Method used

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  • Cyclic peptides binding CXCR4 receptor and relative medical and diagnostic uses
  • Cyclic peptides binding CXCR4 receptor and relative medical and diagnostic uses
  • Cyclic peptides binding CXCR4 receptor and relative medical and diagnostic uses

Examples

Experimental program
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Embodiment approach

[0088] The invention will be further illustrated by the following examples. These examples are pure illustrations of the invention and should not be considered as limiting the scope of the invention.

example

[0090] As revealed in the Examples provided below, the subject peptides of the present invention, bind to the CXCR4 receptor and exhibit antagonist and agonist activity on the activation of the receptor in various in vitro biological assays, such as:

[0091] (a) Ca after stimulation with SDF-1α 2+ The released cytofluorescence assessment;

[0092] (b) Regulation of cell migration in the presence or absence of specific ligand SDF-1α;

[0093] (c) Regulation of activation of ERK-1,2.

[0094] As mentioned above, the CXCR4 receptor is overexpressed in different tumor pathologies. One of the functional responses to activation of the CXCR4 receptor with respect to relative metastatic capacity is the induction of migration. Some peptides of the invention showed antagonist effects, almost comparable to the best characterized inhibitor, AMD3100, with respect to induction to ligand-induced migration.

[0095] In vivo studies performed in relation to the melanoma lung metastasis as...

no. 1 Embodiment

[0148]Monomer corresponding to Example 1, but without a protecting group (free carboxylate) at the C-terminus: Ac-KG-asc:[Dap-FHR-E] (SEQ ID NO: 13)

[0149] From the same monomer of the second example, and from a peptide similar to the monomer of the second example except for the central tripeptide (with the sequence Phe-Tyr-Lys, via 1,6-hexamethylenediamine tail-tail two Polymerization) formed dimers:

[0150] N6:{Ac-KG-asc:[Dap-FHR-E]-*}{Ac-KG-asc:[Dap-FYK-E]-*}

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Abstract

The present invention relates to the identification of new peptides and peptidomimetics which bind the CXCR4 receptor, capable of forming complexes with receptors for chemokines, in particular with CXCR4. The invention also relates to the use of these peptides for the treatment, prevention and diagnosis of diseases which involve chemokine receptors (i.e. neoplasias, metastases, HIV-I virus infections), and also the mobilization of stem cells of hemopoietic precursors in the case of autologous transplants. Finally, the invention comprises pharmaceutical compositions and diagnostic kits comprising said peptides.

Description

【Technical field】 [0001] The present invention relates to the identification of novel peptides and peptidomimetics that bind to the CXCR4 receptor and are capable of forming complexes with chemokine receptors, especially CXCR4. The present invention also relates to the use of these peptides in therapy, prophylaxis and diagnosis involving chemokine receptors (i.e. neoplasia, metastasis, HIV-1 virus infection) and also in the case of autologous grafts the mobilization of stem cells of hematopoietic precursors disease use. Ultimately, the invention includes pharmaceutical compositions and diagnostic kits comprising the peptides. 【Background technique】 [0002] Chemokines are a family of small proteins of 8-10 kDa with chemotactic activity. They are characterized by a wide range of biological activities, including regulation of leukocyte trafficking, modulation of hematopoietic cell proliferation and adhesion to extracellular matrix molecules. [0003] A role for the chemokin...

Claims

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Application Information

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IPC IPC(8): C07K7/06
CPCC07K7/06C07K7/64A61K38/00
Inventor P·阿莫德奥R·维塔勒S·德鲁卡S·斯卡拉G·卡斯特罗A·西亚尼
Owner CONSIGLIO NAT DELLE RICERCHE
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