Biliverdin Reductase Peptides Modulate PKC-δ Activity
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Solution Overview
Problem
Current methods fail to effectively modulate the activity of PKC-δ and its complex with ERK, which is crucial for various cellular processes and disease conditions, as existing technologies do not adequately address the regulation of these proteins.
Innovation Solution
Administration of mammalian biliverdin reductase (BVR) protein or peptides that modulate BVR expression or activity to regulate PKC-δ and PKC-δ/ERK complex activity, including specific peptide fragments that inhibit or enhance PKC-δ activity for therapeutic purposes.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing methods are used to modulate PKC-δ activity, then no effective modulation is achieved, but the complexity of developing new methods increases
Solution Approach 1:
The patent uses BVR (biliverdin reductase) as an intermediary protein that can modulate PKC-δ activity. BVR acts as a mediator between signaling molecules and PKC-δ, providing a reliable mechanism to control PKC-δ activity without directly targeting it, thus achieving effective modulation while maintaining method simplicity
Solution Approach 2:
The patent modulates PKC-δ activity by changing the expression levels or activity states of BVR protein. By adjusting BVR parameters (expression amount, enzymatic activity), the PKC-δ activity is indirectly controlled, providing a reliable modulation approach that avoids direct PKC-δ targeting complexity
2Reliability
If BVR protein or peptides are administered to modulate PKC-δ activity, then therapeutic benefits are achieved, but the complexity of peptide characterization and validation increases
Solution Approach 1:
The patent segments the full-length BVR protein into specific functional peptide fragments (e.g., residues 1-50, 51-100, or other defined segments). These peptides retain the ability to modulate PKC-δ activity while being easier to characterize, produce, and validate than the full protein, thus maintaining therapeutic effectiveness while simplifying manufacturing
Solution Approach 2:
The patent extracts and isolates specific functional regions from the BVR protein sequence to create peptide fragments. By taking out only the essential functional segments, the patent achieves therapeutic efficacy while reducing the complexity of peptide characterization and validation compared to working with the complete protein
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
This approach allows for the modulation of PKC-δ and PKC-δ/ERK complex activity, providing therapeutic benefits in conditions characterized by reduced or excessive activity, such as autoimmune disorders and cancer, by enhancing or inhibiting their activity as needed.
Implementation Method 1
In its capacity as a kinase, hBVR transfers phosphates to target substrate serine, threonine, and tyrosine residues
Implementation Method 2
hBVR is a dual pH/cofactor-dependent catalyst for conversion of biliverdin-IXα to bilirubin-IXα
Data Source
AI summary
The present invention is directed to methods of modulating PKC-δ activity and PKC-δ/ERK complex activity in cells via biliverdin reductase. Methods and compositions for diagnosing and treating a PKC-δ and PKC-δ/ERK complex related condition are also disclosed.