In Vitro and Initial In Vivo Evaluation of 68Ga-Labeled Transferrin Receptor (TfR) Binding Peptides as Potential Carriers for Enhanced Drug Transport into TfR Expressing Cells

Wängler, Carmen; Nada, Dina; Höfner, Georg; Maschauer, Simone; Wängler, Björn; Schneider, Stephan; Schirrmacher, Esther; Wanner, Klaus T.; Schirrmacher, Ralf; Prante, Olaf

doi:10.1007/s11307-010-0329-6

Cited by 24 publications

(16 citation statements)

References 34 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Transferrin receptor binding peptide TfR-T 12 , which consists of 12 amino acids (THRPPMWSPVWP), is a synthetic peptide obtained by phage display, and is able to bind a different site on TfRs compared with transferrin 15, 16 . In this study, TfR-T 12 was chemically conjugated with a pegylated lipid derivative, 3-(N-succinimidyloxyglutaryl)aminopropyl- polyethyleneglycol(2000)- carbamyl distearoyl phosphatidylethanolamine (NHS-PEG 2000 -DSPE), and used as a functional material to construct the multifunctional lipid vesicles.…”

Section: Introductionmentioning

confidence: 99%

Lipid vesicles containing transferrin receptor binding peptide TfR-T12 and octa-arginine conjugate stearyl-R8 efficiently treat brain glioma along with glioma stem cells

Liu

et al. 2017

Sci Rep

View full text Add to dashboard Cite

Surgery and radiotherapy cannot fully remove brain glioma; thus, chemotherapy continues to play an important role in treatment of this illness. However, because of the restriction of the blood-brain barrier (BBB) and the regeneration of glioma stem cells, post-chemotherapy relapse usually occurs. Here, we report a potential solution to these issues that involves a type of novel multifunctional vinblastine liposomes equipped with transferrin receptor binding peptide TfR-T12 and octa-arginine conjugate stearyl-R8. Studies were performed on brain glioma and glioma stem cells in vitro and were verified in brain glioma-bearing mice. The liposomes were transported across the BBB, killing brain glioma and glioma stem cells via the induction of necrosis, apoptosis and autophagy. Furthermore, we reveal the molecular mechanisms for treating brain glioma and glioma stem cells via functionalized drug lipid vesicles.

show abstract

Section: Introductionmentioning

confidence: 99%

Lipid vesicles containing transferrin receptor binding peptide TfR-T12 and octa-arginine conjugate stearyl-R8 efficiently treat brain glioma along with glioma stem cells

Liu

et al. 2017

Sci Rep

View full text Add to dashboard Cite

show abstract

“…D 1 and D 2 dopamine receptor membrane preparations : HEK293 cells stably expressing dopamine D 1 or D 2 receptors, respectively, were isolated from dishes (145 cm 2 ) with a confluence >85 %, washed two times with PBS (137 m m NaCl, 2.7 m m KCl, 8 m m Na 2 HPO 4 , 1.75 m m KH 2 PO 4 , pH 7.4) and homogenized in 0.32 m sucrose using a Polytron PT A7 (Kinematica Polytron, Littau‐Luzern, Switzerland). Aliquots of this suspension, corresponding to ∼5 mg protein, determined after dissolution in 100 m m NaOH for 1 h according to Bradford using bovine serum albumin standards for calibration, were stored at −80 °C.…”

Section: Methodsmentioning

confidence: 99%

Simultaneous Multiple MS Binding Assays Addressing D₁ and D₂ Dopamine Receptors

2017

Self Cite

View full text Add to dashboard Cite

MS Binding Assays are a label-free alternative to radioligand binding assays. They provide basically the same capabilities as the latter, but use a non-labeled reporter ligand instead of a radioligand. In contrast to radioligand binding assays, MS Binding Assays offer-owing to the selectivity of mass spectrometric detection-the opportunity to monitor the binding of different reporter ligands at different targets simultaneously. The present study shows a proof of concept for this strategy as exemplified for MS Binding Assays selectively addressing D and D dopamine receptors in a single binding experiment. A highly sensitive, rapid and robust LC-ESI-MS/MS quantification method capable of quantifying both SCH23390 and raclopride, selectively addressing D and D receptors, respectively, was established and validated for this purpose. Based thereon, simultaneous saturation and competition experiments with SCH23390 and raclopride in the presence of both D and D receptors were performed and analyzed by LC-MS/MS within a single chromatographic cycle. The present study thus demonstrates the feasibility of this strategy and the high versatility of MS Binding Assays that appears to surpass that common for conventional radioligand binding assays.

show abstract

“…All substances were evaluated in 3 independent competition experiments in six concentrations (each in triplicate). The K i -values were calculated from the IC 50 -values according to Cheng-Prusoff [ 22 ] as described in detail in [ 23 ].…”

Section: Methodsmentioning

confidence: 99%

t-Bu2SiF-Derivatized D2-Receptor Ligands: The First SiFA-Containing Small Molecule Radiotracers for Target-Specific PET-Imaging

et al. 2011

Self Cite

View full text Add to dashboard Cite

The synthesis, radiolabeling and in vitro evaluation of new silicon-fluoride acceptor (SiFA) derivatized D2-receptor ligands is reported. The SiFA-technology simplifies the introduction of fluorine-18 into target specific biomolecules for Positron-Emission-Tomography (PET). However, one of the remaining challenges, especially for small molecules such as receptor-ligands, is the bulkiness of the SiFA-moiety. We therefore synthesized four Fallypride SiFA-conjugates derivatized either directly at the benzoic acid ring system (SiFA-DMFP, SiFA-FP, SiFA-DDMFP) or at the butyl-side chain (SiFA-M-FP) and tested their receptor affinities. We found D2-receptor affinities for all compounds in the nanomolar range (Ki(SiFA-DMFP) = 13.6 nM, Ki(SiFA-FP) = 33.0 nM, Ki(SiFA-DDMFP) = 62.7 nM and Ki(SiFA-M-FP) = 4.21 nM). The radiofluorination showed highest yields when 10 nmol of the precursors were reacted with [18F]fluoride/TBAHCO3 in acetonitrile. After a reversed phased cartridge purification the desired products could be isolated as an injectable solution after only 10 min synthesis time with radiochemical yields (RCY) of more than 40% in the case of SiFA-DMFP resulting in specific activities >41 GBq/µmol (>1,100 Ci/mmol). Furthermore, the radiolabeled products were shown to be stable in the injectable solutions, as well as in human plasma, for at least 90 min.

show abstract

In Vitro and Initial In Vivo Evaluation of 68Ga-Labeled Transferrin Receptor (TfR) Binding Peptides as Potential Carriers for Enhanced Drug Transport into TfR Expressing Cells

Cited by 24 publications

References 34 publications

Lipid vesicles containing transferrin receptor binding peptide TfR-T12 and octa-arginine conjugate stearyl-R8 efficiently treat brain glioma along with glioma stem cells

Lipid vesicles containing transferrin receptor binding peptide TfR-T12 and octa-arginine conjugate stearyl-R8 efficiently treat brain glioma along with glioma stem cells

Simultaneous Multiple MS Binding Assays Addressing D₁ and D₂ Dopamine Receptors

t-Bu2SiF-Derivatized D2-Receptor Ligands: The First SiFA-Containing Small Molecule Radiotracers for Target-Specific PET-Imaging

Contact Info

Product

Resources

About

In Vitro and Initial In Vivo Evaluation of 68Ga-Labeled Transferrin Receptor (TfR) Binding Peptides as Potential Carriers for Enhanced Drug Transport into TfR Expressing Cells

Cited by 24 publications

References 34 publications

Lipid vesicles containing transferrin receptor binding peptide TfR-T12 and octa-arginine conjugate stearyl-R8 efficiently treat brain glioma along with glioma stem cells

Lipid vesicles containing transferrin receptor binding peptide TfR-T12 and octa-arginine conjugate stearyl-R8 efficiently treat brain glioma along with glioma stem cells

Simultaneous Multiple MS Binding Assays Addressing D1 and D2 Dopamine Receptors

t-Bu2SiF-Derivatized D2-Receptor Ligands: The First SiFA-Containing Small Molecule Radiotracers for Target-Specific PET-Imaging

Contact Info

Product

Resources

About

Simultaneous Multiple MS Binding Assays Addressing D₁ and D₂ Dopamine Receptors