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Anti-erythropoietin receptor peptide

A halogen atom and prodrug technology, applied in the field of anti-erythropoietin receptor peptides and compositions containing the peptides, can solve problems such as unclear details, achieve strong EpoR inhibitory ability, high cancer cell killing ability, improve Effects of absorption/distribution/metabolism/excretion kinetics

Pending Publication Date: 2021-07-23
EPO MED INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the details of its mechanism are still unclear, and there are many aspects that should be resolved in the future

Method used

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  • Anti-erythropoietin receptor peptide
  • Anti-erythropoietin receptor peptide
  • Anti-erythropoietin receptor peptide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0418] (Example 1: Synthesis of peptides)

[0419] The following peptides were synthesized (the names of the compounds are indicated in parentheses):

[0420] Ac-SCHFGPLTWVCK-NH 2 (YS12) [SEQ ID NO: 9]

[0421] (Benzoyl)-SCHFGPLTWVCK-NH 2 (GT11255)

[0422] (p-Fluorophenylacetyl)-SCHFGPLTWVCK-NH 2 (GT-11256)

[0423] (Propionyl)-SCHFGPLTWVCK-NH 2 (GT-11257)

[0424] Ac-SCH(p-fluoro-Phe)GPLTWVCK-NH 2 (GT-11258)

[0425] Ac-SCH(p-chloro-Phe)GPLTWVCK-NH 2 (GT-11259)

[0426] Ac-SCH(m-chloro-Phe)GPLTWVCK-NH 2 (GT-11260)

[0427] Ac-SCHYGPLTWVCK-NH 2 (GT11261) [SEQ ID NO: 10]

[0428] Ac-SCH(Phenylglycine)GPLTWVCK-NH 2 (GT-11262)

[0429] Ac-SCH(Phenylethylglycine)GPLTWVCK-NH 2 (GT-11263)

[0430] Ac-SCHFAPLTWVCK-NH 2 (GT-11264) [SEQ ID NO: 11]

[0431] Ac-SCHFaPLTWVCK-NH 2 (GT-11265)

[0432] Ac-SCHFGALTWVCK-NH 2 (GT-11266) [SEQ ID NO: 12]

[0433] Ac-SCHFG (Homoproline) LTWVCK-NH 2 (GT-11267)

[0434] Ac-SCHFGPATWVCK-NH 2 (GT-11268) [SEQ ID NO: 13]

[...

Embodiment 2

[0457] (Example 2: In vitro performance evaluation in human liver cancer cells)

[0458] The properties of the synthetic peptides were measured by the following methods.

[0459] Lethal effect based on synthetic peptides using HepG2 cells derived from human liver cancer

[0460] Tested against the following test compounds; YS12, GT-11268, GT-11261, GT-11274, GT-11259, GT-11260, GT-11280, GT-11303, GT-11304, GT-11305, GT-11306 , GT-11307, GT-11308, and GT-11309.

[0461] HepG2 cells (ATCC, HB-8065) ​​were seeded on 8-well CHAMBER SLIDE (Nunc)), and the lethal effect was studied at 4 concentrations of the test compound.

[0462]Culture conditions: use D-MEM medium containing 10% fetal bovine serum (Fujifilm Wako Pure Chemical Industries, 045-30285), at 37°C, 5% CO 2 Cultured under -95% air condition.

[0463] Test concentration; 120 mu M, 60 mu M, 30 mu M and 15 mu M was the test compound, and PBS(-) was used as a control.

[0464] Cell number; 1.0~1.5×10 3 The num...

Embodiment 3

[0475] (Example 3: In vitro performance evaluation of human pancreatic cancer cells)

[0476] The in vitro performance of the synthetic peptides on human pancreatic cancer cells was evaluated by the following method.

[0477] AsPC-1 cells (ECACC, 96020930) from human pancreatic cancer were used in RPMI-1640 medium (Sigma , R8758-500ML), at 37°C, 5% CO 2 Subculture was carried out under -95% air condition (twice / week). Use 0.05% trypsin-0.02% EDTA solution (Sigma, T4174-100ML) to recover the AsPC-1 cells from the culture dish, suspend them in the above medium, and inoculate them in 96-well microplates (3×10 3 / 0.05mL / well). After culturing overnight, add test compounds (total 43 compounds, final concentration 150 mu M) medium (0.05 mL / well, 3 wells / test compound). After 72 hours, the cell proliferation ability of each well was measured by the WST method (Dojin Chemical Research Institute, Cell Counting Kit-8), and the inhibition rate of each test compound relative to the ...

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Abstract

The present invention provides an anti-EpoR peptide having the structure represented by formula (I): X1-SCH(A1)(A2)(A3)(A4)(A5)(A6)V(A7)(A8)-X2 (X1 is the amino terminal side of the peptide; X2 is the carboxy terminal side of the peptide; A1 is M or F, phenylglycine or phenethylglycine optionally substituted by a halogen atom or a hydroxyl group; A2 is A, d-alanine or G; A3 is P, homoproline or A; A4 is M, L, A or I; A5 is T or A; A6 is M or W, F, Y, beta-homotryptophan, alpha-naphthylalanine, beta-naphthylalanine, or quinolylalanine optionally substituted by methyl or a halogen atom; A7 is C, homocysteine, or penicillamine; and A8 is K, R or does not exist.).

Description

technical field [0001] The present invention relates to a novel anti-erythropoietin receptor (hereinafter also referred to as "EpoR") peptide, a composition comprising the peptide, and its use (application). Background technique [0002] Erythropoietin is involved in the differentiation and proliferation of red blood cells, and unlike other cytokines, is not produced in blood cells, but is produced in the kidney or liver and released into the blood. It is believed that erythropoietin acts on erythroid burst-forming unit (BFU-E, burst-forming unit-erythroid) and erythroid colony-forming unit (CFU-E, colony-forming unit-erythroid) in erythroid precursor cells, Promote their differentiation and proliferation, and induce the production of red blood cells (Krantz S. B. Blood, Vol. 77, pp. 419-434 (1991)). It is considered that when erythropoietin binds to the erythropoietin receptor present on the cell membrane of the precursor cell, the signal is transmitted to the nucleus, cau...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08A61K38/02A61K47/54A61P3/00A61P15/00A61P27/02A61P35/00A61P35/02
CPCA61P3/00A61P15/00A61P27/02A61P35/00A61P35/02C07K7/08C07K14/505A61K38/00
Inventor 小路弘行安田佳子加藤明良越智宏
Owner EPO MED INC
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