Bax Inhibitor Compounds With Higher Binding Affinity at Lower Doses
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Solution Overview
Problem
Existing Bax inhibitors are inefficient at low concentrations and fail to effectively inhibit Bax-induced cell death, which contributes to various degenerative diseases.
Innovation Solution
Development of novel Bax inhibiting compounds with improved binding affinity (Kd ranging from 1 nM to 1000 nM) that suppress Bax-mediated cell death, formulated as specific chemical structures to target and inhibit Bax activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing Bax inhibitors are used, then Bax-induced cell death can be inhibited, but the inhibitors require high concentrations (at least 200 nM) to achieve effective inhibition
Solution Approach 1:
The patent modifies the chemical structure of Bax inhibitors by changing molecular parameters (introducing specific functional groups, modifying binding moieties) to enhance binding affinity. This allows the inhibitors to achieve effective Bax-induced cell death inhibition at lower concentrations (1 nM-1000 nM range), directly resolving the contradiction between inhibition effectiveness and required concentration.
2Reliability
If previous Bax inhibitors are used, then some level of cell death inhibition is achieved, but the binding affinity is insufficient (Kd > 200 nM)
Solution Approach 1:
The patent optimizes binding affinity parameters by modifying the chemical structure to achieve Kd values ranging from 1 nM to 1000 nM. This structural optimization enables the inhibitors to bind more effectively to Bax, improving both binding affinity measurement and resulting cell death suppression reliability.
Data Source
AI summary
A compound having formula (I) or (II) for use inhibiting Bax mediated cell death and/or apoptosis.