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The specific molecules of cellular and metabolic processes have the potential to become the targets of several diseases. The understanding of these molecular targets is crucial for the identification and development of targeting molecules. The specific sequences on targeted molecules that are responsible for the interaction with targeting molecules or ligands have been identified. These ligands are also suitable for delivering radionuclides for imaging and therapy (Auger, gamma, beta and alpha particles) to cancer cells. These ligands for molecular imaging and targeted radiation therapy are specifically designed to carry specific radionuclides to molecular targets expressed on cancer cells. Peptides and small molecules are the most preferred ligands. The purpose of using these molecules is to identify molecular targets for personalised disease management and, if needed, for targeted radiation therapy to minimise damage to healthy cells and reduce side effects which are commonly associated with non-targeted and conventional therapies. Several radiolabelled peptides and small molecules are currently in clinical use. Moreover, the scope for exploration and design of new targeted therapies is vast.

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