SRSF6-Targeting Small Molecule Inhibiting Colorectal Tumor Growth
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Solution Overview
Problem
Current treatments for colorectal cancer do not effectively target the aberrant alternative splicing events promoted by overexpressed SRSF6 protein, which are common in the development and progression of the disease.
Innovation Solution
A small molecule compound specifically designed to inhibit SRSF6 protein, selectively targeting cells with high SRSF6 expression, thereby reducing abnormal alternative splicing and inhibiting tumor growth, particularly in colorectal cancer, through a synthesis process involving bromination, stereoselective reduction, and intramolecular cyclization.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional treatments are used for colorectal cancer, then general tumor growth may be controlled, but they cannot effectively target aberrant alternative splicing events promoted by overexpressed SRSF6 protein
Solution Approach 1:
The patent introduces a small molecule compound as an intermediary that specifically binds to SRSF6 protein, thereby mediating the inhibition of SRSF6-mediated alternative splicing events. This intermediary approach allows selective targeting of SRSF6 overexpressing cells without affecting cells with normal SRSF6 expression levels, resolving the contradiction between general tumor control and specific targeting effectiveness.
Solution Approach 2:
The invention applies local quality by designing a compound with specific molecular structure features that enable selective interaction with SRSF6 protein only in cells where SRSF6 is overexpressed. The compound's chemical structure (Formula I) is optimized to bind specifically to SRSF6, creating a localized therapeutic effect precisely where the pathological splicing events occur, thus achieving both reliability and adaptability.
2Manufacturing precision
If a small molecule compound specifically targeting SRSF6 is developed, then selective inhibition of abnormal splicing events can be achieved, but the synthesis process becomes complex involving multiple steps
Solution Approach 1:
The synthesis process is segmented into distinct modular steps (bromination, stereoselective reduction, intramolecular cyclization), where each step produces a specific intermediate with well-defined structural features. This segmentation allows for precise control at each stage, ensuring the final compound achieves the required manufacturing precision for selective SRSF6 inhibition while making the overall complex synthesis manageable through systematic breakdown.
Solution Approach 2:
The invention employs parameter changes during synthesis, particularly in the stereoselective reduction step where chiral parameters are controlled to produce the desired enantiomer. By carefully adjusting reaction parameters (temperature, catalyst selection, solvent conditions) at critical steps, the synthesis achieves high selectivity and precision in producing the active compound form, thereby maintaining manufacturing precision despite process complexity.
3Object-generated harmful factors
If the compound selectively inhibits cells with high SRSF6 expression, then abnormal alternative splicing events are reduced, but the mechanism of action requires precise molecular recognition
Solution Approach 1:
The small molecule compound essentially creates a structural copy or mimic of the natural ligand or substrate that SRSF6 normally interacts with during splicing regulation. By replicating key structural features of the endogenous molecule, the compound can bind to SRSF6 with high precision, enabling selective inhibition of SRSF6-mediated splicing events in overexpressing cells while maintaining accurate molecular recognition through structural fidelity.
Data Source
AI summary
The invention discloses small molecular compounds targeting SRSF6 protein, its preparation method and applications. The compound is shown in formula (I). This molecule can selectively inhibit abnormal cells with high expression of SRSF6, thereby reducing the occurrence of abnormal alternative splicing events and inhibiting the occurrence and development of tumors, especially colorectal tumors. It can be used as a candidate new drug for anti-colorectal cancer.