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Anticancer peptides

A peptide sequence, selected technology, applied in the field of antitumor compounds

Pending Publication Date: 2020-08-07
IDP DISCOVERY PHARMA SL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the properties shown by the peptides already disclosed in the prior art, such as specificity and sensitivity, need to be further improved

Method used

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  • Anticancer peptides
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Examples

Experimental program
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Effect test

preparation example Construction

[0304] Formulations of the pharmaceutical compositions described herein can be prepared by any method known or later developed in the art of pharmacology. Generally, such preparation methods comprise the steps of associating the active ingredient (the peptide) with excipients and / or one or more other auxiliary ingredients and then, if necessary and / or desired, shaping the product and / or Packaged in the desired single-dose unit or multiple-dose units.

[0305] The pharmaceutical compositions of the present invention may be prepared, packaged and / or sold in batches as a single unit dose, and / or as a plurality of single unit doses. As used herein, a "unit dose" is a discrete quantity of pharmaceutical composition containing a predetermined quantity of active ingredient. The amount of active ingredient is usually equal to the dose of active ingredient to be administered to the subject and / or an appropriate fraction of such a dose, eg half or a third of such dose.

[0306] The re...

Embodiment

[0331] 1. Materials and methods

[0332] General steps of synthesis

[0333] Compounds IDP-wtL05, IDP-intwtL05, IDP-LLCb01 and IDP-LLCb02.

[0334] The materials were purchased as follows: Fmoc-protected α-amino acid (---); Rinkamide MBHA resin (Tianjin Nankai Synthetic Technology Co., Ltd.); HBTU ((2-(1H-benzotriazol-1-yl)-1,1 ,3,3-Tetramethyluronium hexafluorophosphate), GLBiochem); N-methylmorpholine (Sinopharm Chemical Reagent Co., Ltd.); Succinic anhydride (Aladdin); Acetonitrile (Xingke Chemical Fiber); Triketone (Sinopharm Chemical Reagent Co., Ltd.); Piperidine (Vantrus); Dimethylformamide, DMF (Zhejiang Jiangshan Chemical Co., Ltd.); Trifluoroacetic acid, TFA (trifluoroacetic acid, Solvay), TIS (thioanisole, Solvay).

[0335] Briefly, linear peptides were artificially synthesized using Fmoc-based SPPS (solid-phase peptide synthesis) on Rink amide MBHA resin as a support.

[0336] Use the following scheme:

[0337] 1. Remove the Fmoc protecting group with 20% pipe...

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Abstract

The present invention provides a peptide of formula (I) or a pharmaceutical salt thereof, as well as fusion peptides and pharmaceutical compositions comprising it; or, alternatively, the peptide or pharmaceutical salt thereof is one which has an amino acid sequence with an identity from 85% to 95% with respect to sequence SEQ ID NO: 25, 26, 27 or 28. The peptides of the invention show anticancer activity.

Description

[0001] This application claims the benefit of European Patent Application 17382533.2 filed on 02.08.2018. technical field [0002] The present invention relates generally to the field of antineoplastic compounds, and more particularly, to the design and synthesis of peptides with improved anticancer activity. Background technique [0003] Therapeutic uses of proteins and peptides that work inside cells hold great promise for treating cancer and other diseases. [0004] Cancer is the result of many factors. Mutations may occur in proto-oncogenes that lead to increased cell proliferation. Mutations may also occur in tumor suppressors whose normal function is to regulate cell proliferation. Mutations in DNA repair enzymes impair the ability of cells to repair damage before proliferating. [0005] Tumor suppressor genes are normal genes, and the loss (loss or inactivation) of tumor suppressor genes can lead to cancer. Tumor suppressor genes encode proteins that slow cell gro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/82A61K38/00
CPCA61K38/00C07K14/82C07K2319/10
Inventor 劳拉·内沃拉圣地亚哥·埃斯特班·马丁
Owner IDP DISCOVERY PHARMA SL
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