Inspired by the potent GRPR antagonist, RC-3950-II ([D-Phe6, Leu13ψThz14]Bombesin(6-14)), reported by the Schally group [17,18], our group synthesized and evaluated a 68Ga-labeled DOTA-conjugated RC-3950-II derivative, [68Ga]Ga-TacsBOMB2 (Figure 1A), for imaging GRPR-expressing cancer with positron emission tomography (PET) [19]. The gene discussed is GRP; the disease is cancer.