Python Serum Proteins Induce Cancer Cell Apoptosis

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Solution Overview

Problem

Current antitumor drugs often lack selective pro-apoptotic action on cancer cells while sparing healthy cells, and there is a need for compounds that can effectively target cancer stem cells.

Innovation Solution

Proteins P3, P4, P5, and P6, with specific amino acid sequences and structures, form non-covalent hetero-tetrameric and hexameric complexes exhibiting pro-apoptotic and anti-telomerase activity, specifically designed to induce apoptosis in cancer cells and cancer stem cells.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional chemotherapeutics are used to inhibit cell cycle and block cell growth, then tumor growth is suppressed, but healthy cells are also affected and selective action on cancer cells is not achieved

Engineering Contradiction:
Improveselectivity of pro-apoptotic actionVSAvoiddamage to healthy cells
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing proteins with specific amino acid sequences (P3, P4, P5, P6) that confer selective recognition and binding to cancer cells. The proteins exhibit differential activity based on the local biochemical environment and cell type, enabling selective induction of apoptosis in cancer cells while sparing healthy cells through targeted molecular interactions

Inventive Principle:
Principle #3Local quality

2Reliability

If proteins with pro-apoptotic activity are used to induce apoptosis in cancer cells, then tumor growth inhibition is achieved, but effective targeting of cancer stem cells is not sufficient

Engineering Contradiction:
Improveeffectiveness against cancer stem cellsVSAvoidbroad spectrum anti-tumor activity
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies universality by designing a protein family (P3, P4, P5, P6) where each protein exhibits multi-functional activity. These proteins simultaneously induce apoptosis in differentiated cancer cells and target cancer stem cells, while also displaying anti-telomerase activity. This multi-functionality ensures broad-spectrum anti-tumor efficacy without requiring multiple different agents

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Reliability

If proteins P3 and P4 are isolated from python serum, then natural anti-tumor activity is obtained, but production quantity and scalability are limited

Engineering Contradiction:
Improvenatural anti-tumor activityVSAvoidproduction quantity
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent applies copying by determining the amino acid sequences of naturally occurring proteins P3 and P4 from python serum, then creating synthetic copies (P5 and P6) through molecular biology techniques. This allows replication of the natural proteins' anti-tumor activity while enabling scalable production through recombinant expression systems, overcoming the limitations of natural extraction

Inventive Principle:
Principle #26Copying

4Reliability

If proteins with significant sequence divergence of key amino acids are designed, then enhanced pro-apoptotic activity is achieved, but structural complexity increases

Engineering Contradiction:
Improvepro-apoptotic activityVSAvoidprotein structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by systematically modifying specific amino acid positions in the protein sequences (e.g., positions 94, 132, 134, 153 in P3 relative to P1). These targeted parameter changes in the primary structure result in enhanced pro-apoptotic and anti-telomerase activities while maintaining the fundamental hetero-tetrameric structural framework, thus improving function without proportionally increasing complexity

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP2739644B1Proteins with pro-apoptotic and antitelomerase activity on cancer cells, their preparation and use.
Publication Date: 2016.03.30 SQUEO MARIA
  • EP2739644B1 patent drawingFigure 1~2
  • EP2739644B1 patent drawingFigure 3
  • EP2739644B1 patent drawing

AI summary

Proteins are described which exhibit pro-apoptotic and anti-telomerase activity on cancer cells and are useful for preparation of pharmaceutical formulations capable of inducing apoptosis of cancer cells and cancer stem cells selectively; furthermore the processes for their purification and/or synthesis are described.