Hepatitis B Peptide Targeting Hypoxic Cells

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for diseases associated with hypoxia, such as age-related macular degeneration and cancer, face challenges due to off-target effects and poor delivery of therapeutic agents to hypoxic cells, with existing carrier peptides being large, expensive, and non-specific, leading to toxicity and reduced efficacy.

Innovation Solution

A novel method using a construct comprising a targeting carrier peptide derived from the Hepatitis B virus X-protein for delivering compounds to hypoxic cells, specifically interacting with connexin43, to enhance uptake and reduce off-target effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing carrier peptides are used to deliver therapeutic agents to hypoxic cells, then delivery is achieved, but the carrier peptides are large, expensive, and non-specific, leading to toxicity and reduced efficacy

Engineering Contradiction:
Improvedelivery efficacyVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the key parameter of carrier peptide size by using a small peptide (5-20 amino acids) instead of large existing carriers. This size reduction eliminates toxicity associated with large carriers while maintaining delivery capability to hypoxic cells through specific binding to hypoxia-induced receptors

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies local quality by designing a peptide with specific local properties - the peptide sequence is optimized to bind specifically to receptors upregulated in hypoxic regions. This allows selective delivery only to hypoxic cells while leaving normal cells unaffected, thereby reducing off-target toxicity

Inventive Principle:
Principle #3Local quality

2Reliability

If existing carrier peptides are used to deliver therapeutic agents, then delivery is achieved, but the carriers are non-specific, leading to off-target effects

Engineering Contradiction:
Improvedelivery efficacyVSAvoidoff-target effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The peptide is designed with specific local binding properties that recognize and bind only to receptors overexpressed in hypoxic tissues. This selective binding ensures the therapeutic agent is delivered only to the intended target (hypoxic cells) and not to healthy tissues, eliminating off-target effects

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The small peptide acts as a specific intermediary that mediates between the therapeutic agent and hypoxic cells. It binds to hypoxia-specific receptors with high affinity, serving as a selective bridge that directs the drug payload exclusively to hypoxic regions without interacting with normal cells

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If high concentrations of connexin channel blockers are used to achieve efficacy, then therapeutic effect is achieved, but undesirable side effects such as off-target effects or unsolicited immune response occur

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the concentration parameter by enabling effective delivery at low concentrations of the connexin channel blocker. The small targeted peptide carrier efficiently delivers the blocker to hypoxic cells, achieving therapeutic effect at concentrations that avoid immune response and off-target effects associated with high-dose administration

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS20230123615A1Methods of treatment and novel constructs
Publication Date: 2023.04.20 AUCKLAND UNISERVICES LTD
  • US20230123615A1 patent drawing
  • US20230123615A1 patent drawing
  • US20230123615A1 patent drawing

AI summary

The present invention provides novels method of targeting delivery of a compound to hypoxic cells, for example treatment of diseases and disorders associated with hypoxia, comprising administration of a construct comprising a targeting carrier peptide and a compound for delivery to a hypoxic cell. The invention also provides novel methods for the treatment of diseases or disorders of the eye by administration of a novel construct, a nucleic acid encoding a novel construct, and/or a nucleic acid vector comprising a nucleic acid encoding a novel construct. The invention further provides novel constructs, nucleic acids encoding such constructs, and/or nucleic acid vectors comprising nucleic acids encoding such constructs.