Caspase-Activated Anticancer Prodrug for Targeted Drug Release
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Solution Overview
Problem
Conventional chemotherapy and radiotherapy are toxic to normal cells, leading to severe side effects due to the non-specific targeting of anticancer drugs, which limits their therapeutic efficacy.
Innovation Solution
Development of an anticancer prodrug composed of a peptide with a caspase cleavage site linked to an anticancer drug, which remains non-toxic until activated by caspase in the presence of radiation or UV, allowing for targeted release of the drug specifically at the tumor site.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high doses of anticancer drugs are used to enhance therapeutic effect, then cancer cell inhibition is improved, but toxicity to normal cells increases causing severe side effects
Solution Approach 1:
The anticancer drug is segmented into a prodrug form that is inactive in normal cells but can be activated specifically in cancer cells through radiation-induced caspase activation, thereby separating the therapeutic effect from toxicity
Solution Approach 2:
The prodrug is designed to have different biological properties in different locations: it remains inactive in normal tissues but becomes activated in irradiated cancer cells, achieving local differentiation of drug activity
2Reliability
If conventional chemotherapy is used to treat cancer, then cancer cell growth inhibition is achieved, but damage to normal cells occurs due to non-specific targeting
Solution Approach 1:
Radiation acts as an intermediary that triggers caspase activation, which in turn activates the prodrug specifically in cancer cells, creating a mediated pathway that spares normal cells from direct drug exposure
Solution Approach 2:
The prodrug is administered in advance in an inactive form, and radiation is applied to cancer cells to activate caspase, which then converts the prodrug to its active form specifically at the tumor site
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 maximizes therapeutic effect with lower doses of anticancer drugs and radiation, minimizing damage to normal cells and reducing side effects, while providing a targeted therapy that enhances the efficacy of conventional treatments.
Implementation Method 1
the peptide is cleaved by active caspase to thereby topically release the active ingredient
Implementation Method 2
in vivo by radiation of radioactive ray or UV
Data Source
AI summary
The present invention relates to an anticancer prodrug consisting of peptide of acetyl-SEQ ID NO: 1-linker-anticancer drug. The anticancer prodrug effectively provides an anticancer drug unstable in acid or base, such as doxorubicin, in a form of prodrug. Thus, the anticancer prodrug exists as a non-toxic inactive form when administered into the body, but effectively releases the anticancer drug as an active ingredient in the target area in the presence of caspase activated by radiation or UV treatment after administered into the body. Accordingly, the anticancer drug exhibits selective anticancer effects on cancer cells, thereby maximizing the therapeutic effect and minimizing the side-effects of chemotherapy.