Projects per year
Interest in nuclear imaging of poly(ADP-ribose) polymerase-1 (PARP-1) has grown in recent years due to the ability of PARP-1 to act as a biomarker for glioblastoma and increased clinical use of PARP-1 inhibitors. This study reports the identification of a lead iodinated analog 5 of the clinical PARP-1 inhibitor olaparib as a potential single-photon emission computed tomography (SPECT) imaging agent. Compound 5 was shown to be a potent PARP-1 inhibitor in cell-free and cellular assays, and it exhibited mouse plasma stability but approximately 3-fold greater intrinsic clearance when compared to olaparib. An (123)I-labeled version of 5 was generated using solid state halogen exchange methodology. Ex vivo biodistribution studies of [(123)I]-5 in mice bearing subcutaneous glioblastoma xenografts revealed that the tracer had the ability to be retained in tumour tissue and bind to PARP-1 with specificity. These findings support further investigations of [(123)I]-5 as a non-invasive PARP-1 SPECT imaging agent.
- nuclear imaging
- radioiodinated tracer
- single-photon emission computed tomography
Targeted Cancer therapy combining radionuclides, gene transfer and cytotoxic drugs: from laboratory to clinic
1/05/09 → 30/04/11
Gamma irradiation and targeted radionuclides enhance the expression of the noradrenaline transporter transgene controlled by the radio-inducible p21WAF1/CIP1 promoterMcCluskey, A. G., Mairs, R. J., Sorensen, A., Robson, T., McCarthy, H. O., Pimlott, S. L., Babich, J. W., Champion, S. & Boyd, M., Mar 2013, In: Radiation Research . 179, 3, p. 282-292 11 p.
Research output: Contribution to journal › Article › peer-review
Efficacy in vivo of a cancer therapy strategy combining HSV1716 mediated oncolysis with gene transfer and targeted radiotherapySorensen, A., Mairs, R. J., Braidwood, L., Joyce, C., Conner, J., Pimlott, S., Brown, S. M. & Boyd, M., 2012, In: Mutagenesis. 27, 1, p. 134-135 2 p.
Research output: Contribution to journal › Conference Contribution › peer-review