Ligand engineering for theranostic applications

Area of Science:

• Oncology
• Biotechnology
• Radiopharmaceutical Science

Background:

• Targeted cancer therapy presents a promising alternative to traditional chemotherapy and radiotherapy.
• Advancements in biotechnology enhance the development of novel radiopharmaceuticals for precise imaging and therapy of epithelial tumors.

Purpose of the Study:

• To identify and validate novel radiopharmaceuticals for targeted cancer therapy.
• To develop fibroblast activation protein inhibitors (FAPI) and alpha-v-beta-6 integrin-binding peptides for diagnostic imaging and endoradiotherapy.

Main Methods:

• Rational design of quinoline-based fibroblast activation protein inhibitors (FAPI).
• High-throughput screening of a sunflower trypsin inhibitor 1-based peptide library.
• Identification of a novel alpha-v-beta-6 integrin-binding peptide (SFITGv6).

Main Results:

• Several FAPI derivatives were identified.
• A novel alpha-v-beta-6 integrin-binding peptide, SFITGv6, was discovered.
• FAPI and SFITGv6 show potential as radiopharmaceuticals.

Conclusions:

• FAPI and SFITGv6 are effective radiopharmaceuticals for targeting FAP- and alpha-v-beta-6 integrin-expressing epithelial tumors, respectively.
• These agents hold promise for improved diagnostic imaging and endoradiotherapy in oncology.