Abstract
Peptidic receptor targeting in nuclear oncology has been significantly improved the last 20 years. A better in-depth knowledge of peptidic receptor has permitted more extensive research and development of new radioligands. The different published studies showed the interest of radiolabelled peptide development but also the difficulties to obtain a radiopharmaceutical with pharmacologic and pharmacokinetic properties adapted to clinical applications in diagnosis and internal radiotherapy. Based on the literature, the most applied methodology is to modify the structure of the endogenous ligand iteratively and to synthesize various derivatives radiolabelled peptide tested one by one. We chose to address the issue of optimization of radiolabelled peptide analogues from a different recent method via molecular modelling and for our purpose more specifically the targeting of the peptide receptor cholecystokinin/gastrin.
Published Version
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