Expert Opinion on Therapeutic Patents, Journal Year: 2024, Volume and Issue: unknown, P. 1 - 10
Published: Sept. 11, 2024
EphA2 is a tyrosine kinase receptor and considered promising target in cancer. Different approaches are used to receptor, lot of preclinical data demonstrate the potential exploitation this clinical oncology for diagnosis cancer therapy, including immunotherapy.
Language: Английский
Chemical & Biomedical Imaging, Journal Year: 2025, Volume and Issue: unknown
Published: Jan. 30, 2025
Dextrorotary (d) peptides, composed of d-amino acids, are hyper-resistant to proteolytic hydrolysis, making them valuable ligands with excellent in vivo stability for radiopharmaceutical development. Multimerization is a well-established strategy enhancing the performance l-peptide-based radiopharmaceuticals. However, effect multimerization on fate d-peptide-based radiopharmaceuticals remains largely unexplored. Here, we synthesized d-peptide DPA, which targets PD-L1, along its dimer (DP2) and trimer (DP3). PET/CT imaging ex biodistribution studies were performed delineate pharmacokinetics target interactions [68Ga]DPA, [68Ga]DP2, [68Ga]DP3 both normal tumor-bearing mice. Our results revealed that tumor uptake kidney retention increased higher valency ([68Ga]DP3 > [68Ga]DP2 [68Ga]DPA). No significant differences observed liver, heart, lung, spleen, intestine, or bone among three radiotracers. Interestingly, reduction radioactivity bloodstream was detected [68Ga]DP3-treated group compared other two groups. Data analysis chiral configuration amino acids linking chemistry used dominant factors multimers. These findings indicate exerts distinct influence profiles l-peptide multimerization. This study deepens our understanding how mirror-imaged peptides/proteins interact living systems, paving way development harness d-peptides as targeting moieties.
Language: Английский
Citations
0
Expert Opinion on Therapeutic Patents, Journal Year: 2024, Volume and Issue: unknown, P. 1 - 10
Published: Sept. 11, 2024
EphA2 is a tyrosine kinase receptor and considered promising target in cancer. Different approaches are used to receptor, lot of preclinical data demonstrate the potential exploitation this clinical oncology for diagnosis cancer therapy, including immunotherapy.
Language: Английский
Citations
0