FGF-2 Modulating Compounds for Stroke Recovery

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Solution Overview

Problem

Current treatments for stroke and other brain injuries lack effective methods for enhancing recovery and improving mobility in stroke survivors, with existing growth factors like FGF-2 being challenging to use due to their size and complexity.

Innovation Solution

Development of novel compounds that modulate FGF activity and enhance the binding between FGF-2 and its receptors, such as FGF-R1, to treat various diseases and injuries including stroke, traumatic brain injury, and other neurological conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If FGF-2 polypeptide is used as therapy, then FGF signaling activity is achieved, but the complexity and size of the polypeptide make it challenging to use

Engineering Contradiction:
ImproveFGF signaling activityVSAvoidpolypeptide complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent segments the FGF-2 polypeptide structure to identify and utilize only the critical functional domains (such as the N-terminal region containing the FGF box motif) required for receptor binding and signaling activity. This segmentation allows development of truncated or modified versions that retain biological activity while reducing overall molecular complexity and size.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent creates simplified copies or mimics of the FGF-2 polypeptide that replicate its key functional properties. These copies may be smaller peptides, peptidomimetics, or structurally simplified versions that maintain the essential binding interface with FGF receptors while eliminating unnecessary structural elements, thereby reducing complexity while preserving signaling activity.

Inventive Principle:
Principle #26Copying

2Reliability

If FGF-2 is administered to enhance recovery, then neuronal sprouting and synapse formation are improved, but the large molecular size complicates therapeutic delivery

Engineering Contradiction:
Improveneuronal recovery enhancementVSAvoidtherapeutic delivery
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent extracts the essential functional components of FGF-2 that are responsible for neuronal recovery enhancement, separating them from the full-length polypeptide structure. By isolating and utilizing only the critical active sites or motifs (such as specific amino acid sequences involved in receptor interaction), the therapy achieves the desired neuronal sprouting and synapse formation effects while using a much smaller, more deliverable molecular entity.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes key molecular parameters of the FGF-2 therapy, specifically reducing molecular weight and altering structural complexity. By modifying parameters such as peptide length, amino acid composition, or structural conformation while maintaining the essential binding affinity for FGF receptors, the therapy becomes easier to deliver administratively while preserving its ability to enhance neuronal recovery.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS20240174631A1Compounds, compositions, and methods for modulating FGF activity
Publication Date: 2024.05.30 RECOVERY THERAPEUTICS INC
  • US20240174631A1 patent drawing
  • US20240174631A1 patent drawing
  • US20240174631A1 patent drawing

AI summary

The invention features compounds which modulate FGF activity, e.g., by enhancing the binding between FGF-2 and its receptors, e.g., FGF-R1. Also featured is a pharmaceutical composition containing one or more of the compounds, a method of treating an injury or a disease e.g., stroke, congenital hypogonadotropic hypogonadism, and viral infection, and a method of increasing spermatogenesis using the pharmaceutical composition.