Michael R Zalutsky
Jonathan Spicehandler, M.D. Professor of Neuro Oncology, in the School of Medicine
The overall objective of our laboratory is the development of novel radioactive compounds for improving the diagnosis and treatment of cancer. This work primarily involves radiohalo-genation of biomolecules via site-specific approaches, generally via demetallation reactions. Radionuclides utilized for imaging include I-123, I-124 and F-18, the later two being of particular interest because they can be used for the quantification of biochemical and physiological processes in the living human through positron emission tomography. For therapy, astatine-211 decays by the emission of alpha-particles, a type of radiation considerably more cytotoxic that the beta-particles used in conventional endoradiotherapy. The range of At-211 alpha particles is only a few cell diameters, offering the possibility of extremely focal irradiation of malignant cells while leaving neighboring cells intact. Highlights of recent work include: a)
development of reagents for protein and peptide radioiodination that decrease deiodination in vivo by up to 100-fold, b) demonstration that At-211 labeled monoclonal antibodies are effective in the treatment of a rat model of neoplastic meningitis, c) synthesis of a thymidine analogue labeled with At-211 and the demonstration that this molecule is taken up in cellular DNA with highly cytotoxicity even at levels of only one atom bound per cell and d) development of
radiohalobenzylguanidines which are specifically cytotoxic for human neuroblastoma cells.
Appointments and Affiliations
- Jonathan Spicehandler, M.D. Professor of Neuro Oncology, in the School of Medicine
- Professor of Radiology
- Professor of Radiation Oncology
- Professor in Pathology
- Member of the Duke Cancer Institute
- Office Location: 311 Research Drive, 161H Bryan Res Bldg, Durham, NC 27710
- Office Phone: (919) 684-7708
- Email Address: firstname.lastname@example.org
- Ph.D. Washington University, 1974
- M.A. Washington University, 1972
The development of novel radioactive compounds for improving the diagnosis and treatment of cancer.
Awards, Honors, and Distinctions
- MERIT Award. National Institutes of Health. 2005
- PATHOL 293: Research Independent Study
- PATHOL 793: Research Independent Study
- Zhou, Z; McDougald, D; Devoogdt, N; Zalutsky, MR; Vaidyanathan, G, Labeling Single Domain Antibody Fragments with Fluorine-18 Using 2,3,5,6-Tetrafluorophenyl 6-[18F]Fluoronicotinate Resulting in High Tumor-to-Kidney Ratios., Molecular Pharmaceutics (2018) [10.1021/acs.molpharmaceut.8b00951] [abs].
- Zhou, Z; Devoogdt, N; Zalutsky, MR; Vaidyanathan, G, An Efficient Method for Labeling Single Domain Antibody Fragments with 18F Using Tetrazine- Trans-Cyclooctene Ligation and a Renal Brush Border Enzyme-Cleavable Linker., Bioconjugate Chemistry (2018) [10.1021/acs.bioconjchem.8b00699] [abs].
- Chitneni, SK; Yan, H; Zalutsky, MR, Synthesis and Evaluation of a 18F-Labeled Triazinediamine Analogue for Imaging Mutant IDH1 Expression in Gliomas by PET., Acs Medicinal Chemistry Letters, vol 9 no. 7 (2018), pp. 606-611 [10.1021/acsmedchemlett.7b00478] [abs].
- Vaidyanathan, G; Kang, CM; McDougald, D; Minn, I; Brummet, M; Pomper, MG; Zalutsky, MR, Brush border enzyme-cleavable linkers: Evaluation for reducing renal uptake of radiolabeled prostate-specific membrane antigen inhibitors., Nuclear Medicine and Biology, vol 62-63 (2018), pp. 18-30 [10.1016/j.nucmedbio.2018.05.002] [abs].
- Pruszynski, M; Kang, CM; Koumarianou, E; Vaidyanathan, G; Zalutsky, MR, d-Amino Acid Peptide Residualizing Agents for Protein Radioiodination: Effect of Aspartate for Glutamate Substitution., Molecules (Basel, Switzerland), vol 23 no. 5 (2018) [10.3390/molecules23051223] [abs].