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Cp2c-targeting peptide-based anticancer agent

A technology targeting peptides and C-terminals, which is applied in the direction of peptides, antineoplastic drugs, peptide/protein components, etc., and can solve the problems of stability, safety and drug resistance that have not yet been developed.

Pending Publication Date: 2021-12-31
IUCF HYU (IND UNIV COOP FOUND HANYANG UNIV) +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Likewise, despite competing efforts worldwide to develop anticancer drugs, anticancer drugs that have no problems in in vivo stability, safety, and drug resistance have not yet been developed

Method used

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  • Cp2c-targeting peptide-based anticancer agent
  • Cp2c-targeting peptide-based anticancer agent
  • Cp2c-targeting peptide-based anticancer agent

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0077] [Preparation Example 1] Preparation of CP2c targeting peptide conjugated to cell penetrating peptide

[0078] The transcription factor CP2c is known to be overexpressed in various cancers. According to a study by an American research group, it was reported that inhibition of CP2c expression in liver cancer cell lines suppressed cell growth, while overexpression of CP2c led to cancer progression and metastasis [Grant et al., Antiproliferative small-molecule inhibitors of transcription factor LSF reveal oncogene addiction to LSF in hepatocellular carcinoma, Proc. Nail. Acad. Sci. 2012; 109(12): 4503-4508].

[0079] The present inventors identified peptides that bind to transcription factor CP2c (also known as Tfcp2, LSF, LBP1, UBP1, etc.) by phage display method [Kang et al., Identification and characterization Of four novelpeptide motifs that recognize distinct regions of the transcription factor CP2 , FEBS Journal 2005; 272:1265-1277], a type of peptide (CP2c targeting...

Embodiment 1

[0080] [Example 1] Determination of the anticancer effect of ACP52C

[0081] The selected peptides bind to CP2c and inhibit the formation of CP2c-containing transcription factor complexes (CP2c homotetramer and CP2c / CP2b / PIAS1 heterohexamer), thereby indirectly interfering with CP2c DNA binding. As a result of analyzing the anticancer effect of synthetically targeted ACP52C in various cancers, it was confirmed that it exhibits cancer cell-specific growth-inhibiting and cell-death potency ( figure 1 ).

[0082] The growth inhibitory and cell death inducing potency of ACP52C was confirmed by FACS analysis by treating cells with ACP52C after cell cycle synchronization to G1 / S phase by double thymidine blockade. As a result, it was confirmed that polyploidy was formed when the cell cycle was arrested in the G2 / M phase. On the other hand, it was demonstrated that when ACP52C was applied to a cell line synchronized to G2 / M phase with thymidine / nocodazole treatment, the cell cycle...

preparation example 2

[0086] [Preparation Example 2] Synthesis of CP2c targeting peptide-fatty acid conjugate

[0087] Our data suggest that, although ACP52C shows promising anticancer activity, ACP52C may be unstable in vivo. As an effort to improve the in vivo stability of ACP52C, 4 types of albumin-affinity C were synthesized 16 Fatty acid (palmitoyl acid) conjugated peptide ( Figure 7 ). Each peptide was synthesized with N- and C-termini modified, followed by C 16 A fatty acid is conjugated to each peptide.

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Abstract

The present invention relates to a CP2c-targeting peptide-based anticancer agent. A CP2c-targeting peptide according to the present invention binds to transcription factor CP2c so as to inhibit the formation of transcription factor complexes (CP2c homotetramer and CP2c / CP2b / PIAS1 heterohexamer) comprising CP2c, thereby inducing cancer cell-specific cell death, and binds a fatty acid to the peptide so as to ensure stability enabling long-term sustenance in vivo.

Description

technical field [0001] The present invention relates to anticancer agents based on CP2c targeting peptides. Background technique [0002] Although many protein / peptide anticancer agents and anticancer agents based on low-molecular compounds have been developed and used, they do not selectively act only on cancer cells in vivo, but cause serious side effects on normal cells as well, and Its effect is sometimes insignificant due to the emergence of drug-resistant cancer cells. In addition, many protein / peptide anticancer agents under development have a short half-life in vivo, and therefore various studies are underway to overcome this problem. Also, despite competing efforts worldwide to develop anticancer drugs, anticancer drugs that have no problems in in vivo stability, safety, and drug resistance have not yet been developed. Therefore, the discovery of drugs that ensure long-term stability in vivo, selectively remove only various types of cancer cells, and act on drug-r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61K47/64A61K47/54A61P35/00
CPCA61K47/64A61P35/00A61K38/00C07K7/06A61K47/542C07K2319/035C07K2319/10A61K47/65
Inventor 金喆根金敏煐金灿吉孙胜汉金智淑崔成宇李卨医郑珉诚朴东宣李想远郑在民蔡东镐张起硕
Owner IUCF HYU (IND UNIV COOP FOUND HANYANG UNIV)
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