Amide-to-Triazole Switch vs. In Vivo NEP-Inhibition Approaches to Promote Radiopeptide Targeting of GRPR-Positive Tumors

Radiolabeled bombesin (BBN)-analogs have been proposed for diagnosis and therapy of gastrin-releasing peptide receptor (GRPR)-expressing tumors, such as prostate, breast and lung cancer. Metabolic stability represents a crucial factor for the success of this approach by ensuring sufficient delivery of circulating radioligand to tumor sites. The amide-to-triazole switch on the backbone of DOTA-PEG4-[Nle14]BBN(7 –14) (1) was reported to improve the in vitro stability of resulting 177Lu-radioligands.

Source: Nuclear Medicine and Biology - June 10, 2017 Category: Nuclear Medicine Authors: Theodosia Maina, Aikaterini Kaloudi, Ibai E. Valverde, Thomas L. Mindt, Berthold A. Nock Source Type: research