Project ID BE-MI2025_02

ThemeBE-MI

Co Supervisor 1A Prof Tim Witney Faculty of Life Sciences & Medicine, School of Biomedical Engineering & Imaging Sciences, Department of Imaging Chemistry & BiologyEmail

Co Supervisor 1B Prof Gary Cook Faculty of Life Sciences & Medicine, School of Biomedical Engineering & Imaging Sciences, Department of Cancer ImagingEmail

2025 Project: Novel theranostics for the imaging and treatment of therapy-resistant breast cancer

Therapy resistance is one of the biggest problems currently facing clinical oncology, with most cancer deaths resulting from ineffective treatment of drug-resistant cancer. Through this project, we will develop an innovative preclinical programme of research to non-invasively image and treat drug resistant breast cancer through the creation of novel theranostic agents (Fig. 1). Theranostics describes the use of radioactive drugs or biomolecules for both treatment (thera-) and diagnosis (-nostics) of cancer. The tumour-targeting agent, in this case a small molecule, will be tagged with a radionuclide. By switching the radioisotope from a positron to an alpha/beta emitter we can use the same agent for imaging or treatment, respectively.

We will use these theranostics to target the very pathways that cause drug resistance. Drug-resistant tumours upregulate numerous antioxidant pathways that both counteract drug-induced oxidative stress and increase drug efflux. We will target aldehyde dehydrogenase 1A1, a cancer stem cell marker, which is upregulated many-fold in drug-resistant breast cancer. During your PhD you will develop an extensive range of experimental skills spanning in vitro mechanistic evaluation of drug-resistant cancer (flow cytometry, western blotting, biochemical assays, CRISPR/Cas9), to in vivo assessment in advanced animal models of breast cancer (orthotopic, PDX, isogenic). Our objectives over the course of your PhD will be to:

• Yr1: Select appropriate cell model, evaluate specificity, perform cell binding of theranostics, understand biochemical mechanism of cell-kill, perform genetic knockdown and over-expression of target
• Yr2: Perform imaging of lead theranostic to determine compound distribution, tumour binding and dosimetry
• Yr3: Undertake treatment studies in vivo, optimise dosing schedule, determine therapeutic index, publish results
• Yr4: Expand work to other cancer types, publish findings

Representative Publications

H.E. Greenwood, R.S. Edwards, W.E. Tyrrell, A.R. Barber, F. Baark, M. Tanc, E. Khalil, A. Falzone, N.P. Ward, J.M. DeBlasi, L. Torrente, D.R. Pearce, G. Firth, L.M. Smith, O. Vilhelmsson Timmermand, A. Huebner, M.E. George, C. Swanton, R.E. Hynds, G.M. DeNicola, T.H. Witney (2023). Imaging the master regulator of the antioxidant response in non-small cell lung cancer with positron emission tomography. bioRxiv. DOI: 10.1101/2023.12.16.572007

R. Pereira*, R.L. Flaherty*, R. Edwards*, H.E. Greenwood, A.J. Shuhendler & T.H. Witney (2022). A Prodrug Strategy for the In Vivo Imaging of Aldehyde Dehydrogenase Activity. RSC Chem Bio 3, pp.561-570. R. Pereira, T. Genderon, C. Sanghera, H.E. Greenwood, J. Newcombe, P.N. McCormick, K. Sander, M. Topf, E. Årstad, T.H. Witney (2019). Mapping aldehyde dehydrogenase 1A1 activity using an [18F]substrate-based approach. Chem Eur J 25, pp.2345-51.

Sharkey AR, Koglin N, Mittra ES, Han S, Cook GJR, Witney TH. Clinical [18F]FSPG Positron Emission Tomography Imaging Reveals Heterogeneity in Tumor-Associated System xc- Activity. Cancers (Basel). 2024 Apr 8;16(7):1437. Hughes DJ, Josephides E, O’Shea R, Manickavasagar T, Horst C, Hunter S, Tanière P, Nonaka D, Van Hemelrijck M, Spicer J, Goh V, Bille A, Karapanagiotou E, Cook GJR. Predicting programmed death-ligand 1 (PD-L1) expression with fluorine-18 fluorodeoxyglucose ([18F]FDG) positron emission tomography/computed tomography (PET/CT) metabolic parameters in resectable non-small cell lung cancer. Eur Radiol. 2024 Feb 22. doi: 10.1007/s00330-024-10651-5.

Cook GJR, Wong WL, Sanghera B, Mangar S, Challapalli A, Bahl A, Bassett P, Leaning D, Schmidkonz C. Eligibility for 177Lu-PSMA Therapy Depends on the Choice of Companion Diagnostic Tracer: A Comparison of 68Ga-PSMA-11 and 99mTc-MIP-1404 in Metastatic Castration-Resistant Prostate Cancer. J Nucl Med. 2023 Feb;64(2):227-231.