Self-Assembling ER Stress Inhibitor for Denatured Protein Removal
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing chemical chaperones are ineffective in removing denatured proteins and only inhibit the denaturation of normal proteins, lacking the ability to target and self-assemble with denatured proteins.
Innovation Solution
Development of a novel compound with self-assembly activity, represented by a specific chemical formula, which can co-assemble with denatured proteins and inhibit endoplasmic reticulum stress.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing chemical chaperones are used to inhibit endoplasmic reticulum stress, then the denaturation of normal proteins is inhibited, but the ability to remove already denatured proteins is lost
Solution Approach 1:
The patent modifies the chemical structure of existing chemical chaperones by introducing self-assembly capable groups (such as beta-sheet forming peptides or amyloid-like structures) to create new compounds that can both inhibit denaturation and bind to/remove already denatured proteins. This structural parameter change enables dual functionality.
Solution Approach 2:
The invention creates composite molecular structures combining traditional chemical chaperone moieties with self-assembly domains. These composite molecules exhibit both the protective effects of conventional chaperones and the targeted removal capability through self-assembly into fibrillar structures that sequester denatured proteins.
2Stability of the object's composition
If chemical chaperones are designed to inhibit protein denaturation, then normal protein stability is improved, but effectiveness against accumulated denatured proteins is reduced
Solution Approach 1:
The patent converts the harmful accumulation of denatured proteins into a beneficial process by designing compounds that self-assemble into fibrillar structures capable of binding and sequestering denatured proteins. The self-assembly property, which could be considered a deviation from normal protein behavior, is harnessed to create a therapeutic mechanism for removing toxic aggregates.
Solution Approach 2:
The self-assembling compound acts as an intermediary between denatured proteins and the cellular degradation machinery. By forming structured assemblies with denatured proteins, these compounds facilitate their recognition and removal by autophagy or proteasomal systems, thereby eliminating cytotoxicity.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The novel compound effectively reduces cytotoxicity and cell death caused by denatured proteins, providing a therapeutic approach for neurodegenerative and ophthalmic diseases by targeting and inhibiting endoplasmic reticulum stress.
Implementation Method 1
A novel compound having self-assembly activity, if provided, can provide, for example, a new technique that targets a denatured protein, which is also prone to self-assemble.
Implementation Method 2
The present inventors have now surprisingly found that self-assembling chemicals that co-assemble with a denatured protein directly inhibit its activity (toxicity).
Data Source
AI summary
A novel compound having self-assembly activity is provided. Provided is a compound, a tautomer or stereoisomer of the compound, or a salt of the compound or of the tautomer or stereoisomer of the compound, the compound being represented by the following formula:whereinR1 is a hydrogen atom or a substituent represented by —SO2—R1, wherein R11 is a hydrogen atom or any substituent,R2 and R3 each represent a hydrogen atom, a halogen, a nitro group, a linear or branched alkyl group, a linear or branched alkoxy group, or a cyano group, wherein at least one hydrogen atom of the alkyl group or of the alkoxy group is optionally further substituted with a substituent, R1 and R3 may be joined together to form a cyclic structure with the benzene ring to which they are attached, Xs independently represent a hydrogen atom or any substituent, and may be the same or different, and Z is a hydrogen atom or any substituent.