Quinoline Compounds Modulating SERCA to Reduce ER Stress
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Solution Overview
Problem
Current therapies lack effective solutions for reducing endoplasmic reticulum stress, which is linked to various diseases such as diabetes, neurodegenerative disorders, and cancer, and for modulating sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) activity.
Innovation Solution
Development of quinoline compounds that can be administered to treat, prevent, or ameliorate symptoms of endoplasmic reticulum stress-related diseases by reducing stress and modulating SERCA activity, thereby restoring cellular homeostasis.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current therapies are used, then treatment of various diseases can be provided, but effective reduction of endoplasmic reticulum stress and modulation of SERCA activity cannot be achieved
Solution Approach 1:
The patent employs parameter changes by developing a series of quinoline compounds with varying substituents (R1, R2, R3, R4, R5, R6, R7) to optimize the balance between reducing ER stress and modulating SERCA activity. Different substitution patterns on the quinoline core structure allow fine-tuning of the compound's pharmacological properties to achieve the desired therapeutic effect while maintaining reliability across multiple disease indications.
2Reliability
If quinoline compounds are developed to reduce ER stress and modulate SERCA activity, then therapeutic benefits for ER stress-related diseases can be achieved, but the complexity of the compound structure increases
Solution Approach 1:
The quinoline compounds described in the patent exhibit multi-functionality by simultaneously reducing endoplasmic reticulum stress and modulating SERCA activity. This dual mechanism of action allows a single compound to address multiple pathological aspects of ER stress-related diseases, thereby achieving therapeutic effectiveness without requiring complex combinations of multiple drugs, thus managing structural complexity while maintaining reliability.
Data Source
AI summary
Provided herein are quinolines, e.g., a compound of Formula I, pharmaceutical compositions thereof, and methods of their use for treating, preventing, or ameliorating one or more symptoms of an endoplasmic reticulum stress-caused disease. Also provided herein are methods of their use for reducing endoplasmic reticulum stress and modulating the activity of a sarcoplasmic/endoplasmic reticulum Ca2+ ATPase.