TfR-T12 TFA is a BBB-penetrated transferrin receptor (TfR) binding peptide, displaying a binding affinity in the nM range[1][2].
TfR-T12 binds to the TfR and is subsequently internalized into TfR-expressing cells[1].TfR-T12 is a synthetic peptide obtained by phage display, and is able to bind a different site on TfRs compared with transferrin. TfR-T12 can be chemically conjugated with a pegylated lipid derivative, 3-(N-succinimidyloxyglutaryl)aminopropyl- polyethyleneglycol(2000)- carbamyl distearoyl phosphatidylethanolamine (NHS-PEG2000-DSPE), and used as a functional material to construct the multifunctional lipid vesicles[2].
[1]. Carmen WÄngler, et al. In Vitro and Initial in Vivo Evaluation of (68)Ga-labeled Transferrin Receptor (TfR) Binding Peptides as Potential Carriers for Enhanced Drug Transport Into TfR Expressing Cells. Mol Imaging Biol. 2011 Apr;13(2):332-41. [2]. Li-Min Mu, et al. Lipid Vesicles Containing Transferrin Receptor Binding Peptide TfR-T 12 and Octa-Arginine Conjugate stearyl-R 8 Efficiently Treat Brain Glioma Along With Glioma Stem Cells. Sci Rep. 2017 Jun 14;7(1):3487.