In vitro studies revealed that for overexpressed GRP-rin PC-3 cells, 99mTc-AuNP-Lys3-bombesin exhibits higher specificity with 71% enhanced cellular uptake compared 99mTc-AuNPs, while in vivo SPECT/CT imaging of this novel multifunctional system displayed tumor uptake of 6.39 ± 0.83% IA/g at one h with significant uptake by spleen and liver. Here, GRP is linked to neoplasm.