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Peptide as antagonist of VEGF receptor Flt-1

An antagonist, flt-1 technology, applied in the direction of receptors/cell surface antigens/cell surface determinants, peptides, specific peptides, etc., can solve the problem of unsatisfactory angiogenesis inhibitors, weak systemic toxicity and anti-angiogenesis effect And other issues

Inactive Publication Date: 2007-08-22
BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Since the angiogenesis inhibitors currently used clinically are unsatisfactory, such as severe systemic toxicity (Suramin) or weak anti-angiogenic effects (interferon, anti-estrogen, etc.), it is necessary to find more angiogenesis inhibitors

Method used

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  • Peptide as antagonist of VEGF receptor Flt-1

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0097] h 2 N-Trp-His-Ser-Asp-Met-Glu-Trp-Trp-Tyr-Leu-Leu-Gly-COOH (F56)

[0098] Put the peptide synthesis column packed with 4-(2',4'-dimethoxyphenyl-Fmoc-aminomethyl)phenoxyacetamidoethyl resin in the PioneerTM peptide synthesizer, and in nitrogen atmosphere in the following order: The peptide synthesis was carried out as follows:

[0099] 1. Solvate the resin in DMF for 5 minutes;

[0100] 2. Treat the resin with 20% piperidine in DMF for about 15 minutes to remove the protecting group Fmoc on the resin grafted group (or on the resin-bound amino acid α-amino group);

[0101] 3. Wash the resin with DMF for about 1 minute;

[0102] 4. Activate the first amino acid Gly at the C-terminus with a 0.2M solution of HBTU and HOBT in DMSO-NMP (N-methylpyrrolidone) and a 0.4M solution of diisopropylethylamine in DMSO-NMP (Fmoc-Gly ) of the α-carboxyl group;

[0103] 5. Coupling the activated amino acid obtained in step 4 with the resin (or resin-bound amino acid) of step 2 in DMF...

Embodiment 2

[0110] h 2 N-Trp-His-Val-Asp-Glu-Thr-Trp-Trp-Leu-Leu-Met-Leu-COOH (F87)

[0111] The title peptide was prepared according to the procedure described in Example 1. The first amino acid is Fmoc-Leu, and the following amino acids are added sequentially according to the conditions: Fmoc-Met→Fmoc-Leu→Fmoc-Leu→Fmoc-Trp→Fmoc-Trp→Fmoc-Thr(tBu)→Fmoc-Glu(γ -OtBu)→Fmoc-Asp(β-OtBu)→Fmoc-Val→Fmoc-His(Trt)→Fmoc-Trp. This gave 35 mg of the title peptide.

Embodiment 3

[0113] h 2 N-Trp-His-Asp-Pro-Thr-Pro-Trp-Trp-Ser-Trp-Glu-Ile-COOH (F90)

[0114] The title peptide was prepared according to the procedure described in Example 1. The first amino acid is Fmoc-Ile, and the following amino acids are added sequentially according to the conditions: Fmoc-Glu(γ-OtBu)→Fmoc-Trp→Fmoc-Ser(tBu)→Fmoc-Trp→Fmoc-Trp→Fmoc-Pro→ Fmoc-Thr(tBu)→Fmoc-Pro→Fmoc-Asp(β-OtBu)→Fmoc-His(Trt)→Fmoc-Trp. 44 mg of the title peptide were obtained.

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Abstract

The present invention provides a polypeptide or a pharmacologically acceptable salt thereof comprising one or more, identical or different, amino acid sequences of A-W-H-X1-D-X2-X3-X4-W-W-X5-X6-X7-X8-B (the meaning of each symbol in the formula is defined in the description) and a pharmaceutical composition for treating an angiogenic disease such as a solid tumor comprising said polypeptide. The present invention also relates to a polynucleotide encoding the above-mentioned polypeptide and use of the polynucleotide in gene therapy.

Description

technical field [0001] The present invention relates to small peptides that are antagonists of the VEGF receptor Flt-1 and thus useful in the treatment of angiogenic diseases, polynucleotides encoding these peptides, vectors and cells containing the polynucleotides, and the use of these peptides , polynucleotide, carrier or cell method and pharmaceutical composition for treating angiogenic diseases. Background technique [0002] Angiogenesis is required for normal body activities, including reproduction, development and wound healing. Although angiogenesis is a highly regulated process under normal conditions, many diseases are driven by persistent dysregulated angiogenesis, and these diseases are called angiogenic diseases. In other words, dysregulation of angiogenesis can directly cause a particular disease, or exacerbate an already existing disease. For example, neovascularization of the eye is the most common cause of blindness. In pre-existing diseases such as arthri...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/08C12N15/32A61K38/10A61K48/00A61P35/00C07K14/71
CPCA61K48/00A61K38/10C07K14/71A61P35/00
Inventor 寿成超雷和田安平吴健孟麟刘晓颖
Owner BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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