KARS1 Inhibitor Compounds for Broad Cell Migration Suppression

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Solution Overview

Problem

Existing drugs designed to prevent specific cell migration have shown significant limitations and insufficient efficacy due to the diverse modes and characteristics of cell migration, particularly in immune cell migration-related diseases and cancer metastasis, where the signaling and mechanism characteristics are not fully elucidated.

Innovation Solution

Development of novel compounds represented by Formula 1 that inhibit the activity of lysyl-tRNA synthetase 1 (KARS1), suppressing immune cell migration and cancer cell migration, thereby treating related diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing drugs are designed to prevent specific cell migration, then cell migration prevention is attempted, but efficacy is insufficient due to diverse migration modes and mechanisms

Engineering Contradiction:
ImproveefficacyVSAvoiddiverse migration modes
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies universality by designing a compound that can inhibit multiple cell migration types (immune cells, cancer cells, fibroblasts) through a single mechanism - targeting KARS1 enzyme. This multi-functional approach allows one drug to address diverse migration modes across different cell types, resolving the contradiction between efficacy and adaptability to diverse migration characteristics

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

2Reliability

If cell migration is suppressed to treat diseases, then disease treatment is achieved, but understanding of signaling mechanisms is incomplete

Engineering Contradiction:
Improvedisease treatmentVSAvoidsignaling mechanism characteristics
Core Design Contradiction:
ReliabilityVSLoss of information

Solution Approach 1:

The patent uses KARS1 enzyme as an intermediary target to control cell migration. By identifying and targeting this specific enzyme that plays a crucial role in migration across multiple cell types, the patent achieves effective disease treatment while establishing a clear mechanistic pathway (CCL2-RhoA-KARS1 axis), thereby reducing information loss about signaling mechanisms

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentEP4656630A1Novel compound as lysyl-trna synthetase 1 inhibitor, and use thereof
Publication Date: 2025.12.03 ZYMEDI CO LTD
  • EP4656630A1 patent drawingFigure 1
  • EP4656630A1 patent drawingFigure 2~3
  • EP4656630A1 patent drawingFigure 4

AI summary

The present invention relates to a novel compound as a lysyl-tRNA synthetase 1 (KARS 1) inhibitor, and a use thereof, and, more specifically, to a novel compound as a lysyl-tRNA synthetase 1 inhibitor, and a use of preventing or treating immune cell migration-associated diseases and cancer metastasis.