Current State of Targeted Radiometal-Based Constructs for the Detection and Treatment of Disease in the Brain.

  title={Current State of Targeted Radiometal-Based Constructs for the Detection and Treatment of Disease in the Brain.},
  author={Michael D. Phipps and Vanessa A Sanders and Melissa A Deri},
  journal={Bioconjugate chemistry},
The continual development of radiopharmaceutical agents for the field of nuclear medicine is integral to promoting the necessity of personalized medicine. One way to greatly expand the selection of radiopharmaceuticals available is to broaden the range of radionuclides employed in such agents. Widening the scope of development to include radiometals with their variety of physical decay characteristics and chemical properties opens up a myriad of possibilities for new actively targeted molecules… 
1 Citations

Detection of Dopamine Receptors Using Nanoscale Dendrimer for Potential Application in Targeted Delivery and Whole-Body Imaging: Synthesis and In Vivo Organ Distribution.

dendrimer-conjugated dopamine was utilized as a chelating agent for Technetium-99m to investigate the organ distribution of this compound in vivo using the single-photon emission computed tomography (SPECT) technique and revealed that dopamine D1 receptors exhibited the highest accumulation in the liver and the drug retained its specificity.



A Picture of Modern Tc-99m Radiopharmaceuticals: Production, Chemistry, and Applications in Molecular Imaging

In this review, the most efficient chemical methods, based on the modern concept of the 99mTc-metal fragment approach, applied to the development of technetium-99m radiopharmaceuticals for molecular imaging, are described.

Current advances in delivery of biotherapeutics across the blood-brain barrier.

Recent advances in biotherapeutic delivery mechanisms across the blood-brain barrier including transcranial brain drug delivery, focused ultrasound technology, nasal delivery, absorptive endocytosis, and receptor mediated endocyTosis are evaluated using an industrial perspective.

Noninvasive brain cancer imaging with a bispecific antibody fragment, generated via click chemistry

It is demonstrated that dual targeting of EGFR and CD105 provides a synergistic improvement on both affinity and specificity of 64Cu-NOTA-Bs-F(ab)2, and can be used in the construction of other disease-targeting bispecific antibody fragments for early detection and diagnosis of small malignant lesions.

A Proof-of-Concept Study on the Therapeutic Potential of Au Nanoparticles Radiolabeled with the Alpha-Emitter Actinium-225

It is shown that [225Ac]225Ac-Au@TADOTAGA resulted in the retardation of tumor growth after its intratumoral injection in U87MG tumor-bearing mice, even though very low activities were injected per mouse.

Strategy for effective brain drug delivery.

  • M. I. AlamS. Beg M. Akbar
  • Biology
    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
  • 2010

Peptide-based PET imaging of the tumor restricted IL13RA2 biomarker

It is demonstrated that [64Cu]Pep-1L selectively binds hIL13RA2-expressing tumors and validates Pep- 1L as an effective platform to deliver diagnostics and therapeutics to IL13ra2- expressing cancers.

Synthesis and Characterization of (89)Zr-Labeled Ultrasmall Nanoparticles.

Coupling AGuIX to a long-lived radioisotope would help to more completely measure the magnitude and duration of its retention within the tumor microenvironment, and developed (89)Zr-DFO-AGuIX.

Use of 99m-technetium-glucoheptonate as a tracer for brain tumor imaging: An overview of its strengths and pitfalls

The basics of 99mTc-GHA SPECT imaging in brain tumor along with the available literature are discussed, which shows promising results for differentiation of recurrent brain tumor from radiation necrosis.

Gadolinium-Based Nanoparticles and Radiation Therapy for Multiple Brain Melanoma Metastases: Proof of Concept before Phase I Trial

After intravenous injection into animals bearing B16F10 tumors, some nanoparticles remained inside the tumor cells for more than 24 hours, indicating that a single administration of nanoparticles might be sufficient for several irradiations.

Advancements in PARP1 Targeted Nuclear Imaging and Theranostic Probes

Nuclear medicine has now advanced towards conjugating theranostic radionuclides toPARP1 inhibitors, paving the way for a future of PARP1-targeted theranostics and personalized therapy.