Neuromedin B receptor antagonist suppresses tumor angiogenesis and tumor growth in vitro and in vivo

Neuromedin B (NMB), a member of the mammalian bombesin-like peptide family, and its receptor were aberrantly expressed in vascularized solid tumors. Here, the NMB receptor (NMB-R) antagonist PD168368 specifically inhibited both NMB-induced in vivo and in vitro angiogenesis. In addition, PD168368 showed growth inhibitory effects on MDA-MB-231 breast cancer cells by inducing cell cycle arrest and apoptosis. Furthermore, PD168368 effectively suppressed tumor growth in a xenograft model of breast tumor in vivo. Overall, NMB-R antagonist exhibited a significant antitumor activity by simultaneously inhibiting neovascularization and cancer cell growth, thereby suggesting that NMB-R could be a potential therapeutic target for cancer treatment.

► Neuromedin B (NMB) receptor antagonist PD168368 inhibits NMB-induced endothelial angiogenesis in vitro and in vivo. ► PD168368 reduces viability and xenograft tumor growth of human MDA-MB-231 breast cancer cells. ► PD168368 induces cell cycle arrest and apoptosis in MDA-MB-231 cells. ► PD168368 exerts antitumor activity through the inhibition of tumor growth and angiogenesis.