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Imaging COX-2 expression in cancer using PET/SPECT radioligands: current status and future directions

Pacelli, A. ; Greenman, J. ; Cawthorne, C. ; Smith, G.

Journal of labelled compounds & radiopharmaceuticals, 2014-04, Vol.57 (4), p.317-322 [Periódico revisado por pares]

England: Blackwell Publishing Ltd

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  • Título:
    Imaging COX-2 expression in cancer using PET/SPECT radioligands: current status and future directions
  • Autor: Pacelli, A. ; Greenman, J. ; Cawthorne, C. ; Smith, G.
  • Assuntos: [11C]-methylation ; Animals ; cancer ; COX-2 ; coxib ; Cyclooxygenase 2 - metabolism ; Gene Expression Regulation, Neoplastic ; Humans ; imaging biomarker ; imidazole ; indole ; Ligands ; Medical imaging ; Neoplasms - diagnostic imaging ; Neoplasms - metabolism ; PET ; Positron-Emission Tomography - methods ; prostaglandin ; SPECT ; Tomography ; Tomography, Emission-Computed, Single-Photon - methods
  • É parte de: Journal of labelled compounds & radiopharmaceuticals, 2014-04, Vol.57 (4), p.317-322
  • Notas: This article is published in the Journal of Labelled Compounds and Radiopharmaceuticals as a special issue on 'Current Developments in PET and SPECT Imaging', edited by Jonathan R. Dilworth, University of Oxford and Sofia I. Pascu, University of Bath.
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  • Descrição: The role of cyclooxygenase (COX)‐2 as a driving force in early tumourigenesis and the current interest in the combination of COX‐2 inhibitors with standard therapy in clinical trials creates an urgent need to establish clinically relevant diagnostic tests for COX‐2 expression. Molecular imaging using small‐molecule probes radiolabelled for both positron emission tomography (PET) and single photon emission computed tomography (SPECT) offers the potential to meet this need, providing a minimally invasive readout for the whole disease burden. This review summarises current approaches to the radiolabelling of small‐molecule COX‐2 inhibitors and their analogues for PET and SPECT imaging, and gives an overview of their biological evaluation and likely success of clinical application. Radiolabelled cyclooxygenase‐2 probes have been the focus of considerable interest over the last few years, but progress to optimal imaging agents has been slow. This is in large part a result of the challenging nature of the target and the local tumour microenvironment. This review summarises the most recent developments in the area.
  • Editor: England: Blackwell Publishing Ltd
  • Idioma: Inglês;Francês;Alemão
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  • Realização: ABCD-USP USP   Logos de Redes Sociais: Freepik

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