R.; Lober, S.; Hubner, H.; Gmeiner, P., Click chemistry on solid phase: parallel synthesis of -benzyltriazole carboxamides as super-potent G-protein coupled receptor ligands.
Bombesin receptor ligand analogues have been used in clinical studies however the high potency of agonists brings up challenges requiring synthesis with high specific radioactivity in order to exclude pharmacological effects. Antagonists even though they do not internalize have shown improved imaging capabilities. Given recent achievements in the design of antagonists and experience with SST analogues demonstrating advantages of antagonists, the future development will most likely move in the direction of bombesin antagonists.
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