99mTc-Tat-BN

99mTc-Tat-BN is a hybrid radiopharmaceutical imaging agent developed for the molecular imaging and potential targeted radiotherapy of tumors expressing the gastrin-releasing peptide receptor (GRPR). The molecule consists of the HIV-1 Tat(49-57) cell-penetrating peptide linked to a Lys3-bombesin peptide, labeled with the radioisotope technetium-99m (99mTc) via an N2S2 chelator. While 99mTc is primarily used for SPECT imaging, the incorporation of the Tat peptide facilitates the internalization of the complex into the cancer cell nucleus. This nuclear localization allows the Auger and internal conversion electrons emitted by 99mTc to be delivered in close proximity to DNA, potentially inducing cytotoxic effects. The agent has been evaluated in preclinical models of prostate cancer (PC-3) and breast cancer (MCF7, MDA-MB231), showing significant nuclear uptake and inhibition of cell proliferation.

Other names

Tc-Tat-BN99mTc-N2S2-Tat(49-57)-Lys3-BN99mTc-Tat-bombesin99mTc-N2S2-Tat(49-57)-Lys3-bombesin