Journal
DALTON TRANSACTIONS
Volume 44, Issue 11, Pages 4859-4873Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c4dt03206c
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Funding
- CRUK [C5255/A8591]
- Siemens Molecular Imaging Ltd.
- Technology Strategy Board
- EU
- Cancer Research UK
- Siemens Molecular Imaging
- EU (FP7 Metoxia project)
- EU Commission via O2SENSE ERC Consolidator grant
- Royal Society
- STFC
- MRC
- FP7 MC ITN PROSENSE
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Carbonic anhydrase IX (CA IX) is currently generating great interest as a marker of tumour hypoxia and a potential chemotherapeutic target. In order to test the principle that a CA IX inhibitor could be used for targeting PET or SPECT metallic radioisotopes to tumours we have prepared a number of conjugates involving aryl-sulfonamides or an acetazolamide derivative linked to a range of copper, indium, rhenium, 99m-technetium and zinc complexes. Radiolabelled Cu-64 and Tc-99m analogues of the 'cold' Cu and some of the Re complexes were prepared in good radiochemical incorporation. Inhibition of various human carbonic anhydrase isoforms (I, II, IX and XII) was tested with the 'cold', non-radiolabelled complexes, and compared with an acetazolamide standard (AZA). The molecular structure of a new, tri-sulfonated porphyrin-labeled sulfonamide was determined using synchrotron X-ray crystallography.
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