Related Experiment Video
Updated: Nov 9, 2025
MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent
Published on: September 3, 2013
Synthesis and evaluation of tumor-homing peptides for targeting prostate cancer
Ayca Ece Nezir1, Melek Parlak Khalily2,3, Sevgi Gulyuz4,5
1Department of Genetics and Bioengineering, Yeditepe University, 34755, Istanbul, Turkey.
Abstract:
High toxicity caused by chemotherapeutic drugs and the acquisition of drug resistance by cancer cells are the major drawbacks in cancer therapy. A promising approach to overcome the posed barriers is conjugating tumor-homing peptides to drugs or nanocarriers. Such high-affinity peptides can specifically target surface markers overexpressed by cancer cells, ensuring a rapid and cancer-specific uptake of the drugs. Since prostate-specific membrane antigen (PSMA) is overexpressed by aggressive prostate cancer cells, targeting this surface protein with peptide conjugates can lead to the development of effective strategies against prostate cancer. In this study, we aimed to determine which PSMA-binding peptide among peptides 563, 562 and 9-mer, show the highest selectivity towards PSMA using 22Rv1 prostate cancer cells, a cell line with moderate PSMA levels. Tumor-homing peptides were synthesized by fluorenylmethoxycarbonyl-based solid-phase peptide synthesis (Fmoc-SPPS) strategy, and evaluated for their prostate cancer cell-specific targeting efficiencies by flow cytometry. Our results showed that the PSMA-binding capacity of peptide 563 was superior to those of 562, 9-mer, and 5-mer; therefore, can be utilized as a potent-targeting agent not only in the treatment of high PSMA positive but also moderate PSMA positive prostate cancer tumors.
Insights
Peptide 563 demonstrates superior prostate-specific membrane antigen (PSMA) binding compared to other peptides. This finding supports its potential as a targeted therapy for both high and moderate PSMA-expressing prostate cancers.
Area of Science:
- Oncology
- Peptide Chemistry
- Drug Delivery
Background:
- Chemotherapy faces challenges from toxicity and drug resistance.
- Tumor-homing peptides offer targeted drug delivery to cancer cells.
- Prostate-specific membrane antigen (PSMA) is a key target in prostate cancer.
Purpose of the Study:
- To identify the most effective PSMA-binding peptide for prostate cancer targeting.
- To compare the selectivity of peptides 563, 562, and 9-mer for PSMA.
- To evaluate peptide targeting efficiency in a moderate PSMA-expressing cell line.
Main Methods:
- Synthesis of tumor-homing peptides using Fmoc-based solid-phase peptide synthesis (Fmoc-SPPS).
- Evaluation of prostate cancer cell-specific targeting using flow cytometry.
- Utilized 22Rv1 prostate cancer cells with moderate PSMA expression.
Main Results:
- Peptide 563 exhibited significantly higher PSMA-binding capacity than peptides 562, 9-mer, and 5-mer.
- Peptide 563 demonstrated superior selectivity for PSMA.
- The study confirmed peptide 563's potential as a targeting agent.
Conclusions:
- Peptide 563 is a potent PSMA-targeting agent.
- Peptide 563 can be used for both high and moderate PSMA-expressing prostate tumors.
- Targeted peptide conjugates represent a promising strategy to overcome chemotherapy limitations.
More Related Videos
07:25A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
11:58Initial Evaluation of Antibody-conjugates Modified with Viral-derived Peptides for Increasing Cellular Accumulation and Improving Tumor Targeting
Published on: March 8, 2018