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Development of a Peptide-Based Nano-Sized Cathepsin B Inhibitor for Anticancer Therapy
So-Hyeon Park1, Jun-Hyuck Lee1, Seong-Bin Yang1
1Department of Applied Life Science, BK21 Program, Graduate School, Konkuk University, Chungju 27478, Republic of Korea.
Abstract:
Numerous cathepsin B inhibitors have been developed and are under investigation as potential cancer treatments. They have been evaluated for their ability to inhibit cathepsin B activity and reduce tumor growth. However, they have shown critical limitations, including low anticancer efficacy and high toxicity, due to their low selectivity and delivery problems. In this study, we developed a novel peptide and drug conjugate (PDC)-based cathepsin B inhibitor using cathepsin-B-specific peptide (RR) and bile acid (BA). Interestingly, this RR and BA conjugate (RR-BA) was able to self-assemble in an aqueous solution, and as a result, it formed stable nanoparticles. The nano-sized RR-BA conjugate showed significant cathepsin B inhibitory effects and anticancer effects against mouse colorectal cancer (CT26) cells. Its therapeutic effect and low toxicity were also confirmed in CT26 tumor-bearing mice after intravenous injection. Therefore, based on these results, the RR-BA conjugate could be developed as an effective anticancer drug candidate for inhibiting cathepsin B in anticancer therapy.
Insights
A novel peptide and drug conjugate (RR-BA) forms nanoparticles for targeted cancer therapy. This conjugate effectively inhibits cathepsin B, showing potent anticancer effects and low toxicity in preclinical models.
Area of Science:
- Biochemistry
- Nanotechnology
- Oncology
Background:
- Cathepsin B inhibitors are explored for cancer treatment but face challenges like low efficacy and high toxicity.
- Existing inhibitors often lack selectivity and efficient delivery systems, limiting their therapeutic potential.
Purpose of the Study:
- To develop a novel peptide and drug conjugate (PDC) based cathepsin B inhibitor.
- To create a self-assembling nanoparticle system for improved drug delivery and efficacy.
Main Methods:
- Synthesized a conjugate (RR-BA) combining a cathepsin-B-specific peptide (RR) and bile acid (BA).
- Investigated the self-assembly properties of RR-BA in aqueous solution to form nanoparticles.
- Evaluated the cathepsin B inhibitory and anticancer effects of RR-BA nanoparticles in vitro (CT26 cells) and in vivo (CT26 tumor-bearing mice).
Main Results:
- The RR-BA conjugate self-assembled into stable nanoparticles in aqueous solution.
- Nano-sized RR-BA demonstrated significant cathepsin B inhibition and anticancer activity against colorectal cancer cells.
- In vivo studies confirmed the therapeutic efficacy and low toxicity of RR-BA nanoparticles in tumor-bearing mice.
Conclusions:
- The developed RR-BA conjugate effectively self-assembles into nanoparticles, enhancing cathepsin B inhibition and anticancer efficacy.
- RR-BA nanoparticles show promising therapeutic potential with reduced toxicity for colorectal cancer treatment.
- This novel PDC represents a potential drug candidate for cathepsin B-targeted anticancer therapy.
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