Radiolabelled Amino Acids and Peptides for PET Imaging of Cancer

We are collaborating with Dr Peter Roselt and Prof Rod Hicks at the Peter MacCallum Cancer Centre on the preparation of radiolabelled peptides for cancer imaging. We have developed a one-step method for preparation of the radiolabelled synthon, p-nitrophenyl 2-[18]F-fluoropropionate, and incorporated this into the synthesis of gold-standard radiotracers using a fully automated, 2-stage radiochemistry module.

Recent Publications

M. B. Haskali, P. D. Roselt, T. J. O’Brien, C. A. Hutton, I. Ali, L. Vivash, B. Jupp, “Effective Preparation of [¹⁸F]Flumazenil Using Copper-Mediated Late-Stage Radiofluorination of a Stannyl Precursor”, Molecules 2022, 27, 5931.

N.U.H. Khan, A. Corlett, C. A. Hutton, M. B. Haskali, “Investigation of Fluorine-18 Labelled Peptides for Binding to Cholecystokinin-2 Receptors with High Affinity”, Int. J. Pept. Res.Therapeut. 2022, 28:6.

A. Corlett, M.-A. Sani, J. Van Zuylekom, C.-S. Ang, E. von Guggenberg, C. Cullinane, B. Blyth, R. Hicks, P. Roselt, P. Thompson, C. A. Hutton, M. B. Haskali, “A New Turn in Peptide-Based Imaging Agents: Foldamers Afford Improved Theranostics Targeting Cholecystokinin-2 Receptor Positive Cancer,” J. Med. Chem. 2021, 64,

M. B. Haskali, A. L. Farnsworth, P. D. Roselt, C. A. Hutton, “4-Nitrophenyl activated esters are superior synthons for indirect radiofluorination of biomolecules,” RSC Med. Chem., 2020, 11, 919–922.

M. B. Haskali, D. Denoyer, P. D. Roselt, R. J. Hicks, C. A. Hutton, “Radiosynthesis and preliminary in vivo evaluation of 18F-labelled glycosylated duramycin peptides for imaging of phosphatidylethanolamine during apoptosis,” Med. Chem. Commun., 2019, 10, 1930–1934.

M. B. Haskali, A. Hetsron, P. D. Roselt, D. Binns, C. A. Hutton R. J. Hicks “Automated preparation of clinical grade [⁶⁸Ga]Ga-DOTA-CP04, a cholecystokinin-2 receptor agonist, using a prototype synthesis platform (iPHASE MultiSyn),” Eur. J. Nucl. Med. Mol. Imaging, 2019, 4, 23.

M. B. Haskali, P. D. Roselt, R. J. Hicks, C. A. Hutton, “Automated Preparation of 2-[¹⁸F]Fluoropropionate Labelled Peptides using a Flexible, Multi-stage Synthesis Platform (iPHASE Flexlab),” J. Labelled Comp. Radiopharm., 2018, 61, 61­–67.

M. B. Haskali, D. Denoyer, W. Noonan, C. Culinane, C. Rangger, N. Pouliot, R. Haubner, P. D. Roselt, R. J. Hicks, C. A. Hutton, “Sulfonation of Tyrosine as a Method to Improve Biodistribution of Peptide-Based Radiotracers: Novel ¹⁸F-Labelled Cyclic RGD Analogues,” Mol. Pharmaceutics, 2017, 14, 1169–1180.

C. L. Charron, A. L. Farnsworth, P.D. Roselt, R. J. Hicks, C. A. Hutton, “Recent Developments in Radiolabelled Peptides for PET Imaging of Cancer,” Tetrahedron Lett., 2016, 57, 4119–4127.

 

M. B. Haskali, P. D. Roselt, J. A. Karas, W. Noonan, C. W. Wichmann, A. Katsifis, R. J. Hicks, C. A. Hutton, “One-step radiosynthesis of 4-nitrophenyl 2-[¹⁸F]fluoro-propionate ([¹⁸F]NFP); improved preparation of radiolabeled peptides for PET imaging,” J. Labelled Comp. Radiopharm., 2013, 56, 726­–730.