2.B.65. The Pitenin-mediated Chloride/Proton Transport (Pitenin) Family
The anticancer agents, PITENINs, have an efficient transmembrane Cl- ion transport activity, and each of them strongly binds a Cl- ion. In addition to their lipophilicity, the presence of both acylthiourea and phenolic OH moieties of the compounds plays a crucial role in the transport of Cl- ions. Among the tested compounds, PIT-1 and DM-PIT-1 showed higher Cl- ion selectivity and transport efficiency. Mechanistic studies demonstrated that the potent compounds follow the H+/Cl- transport pathway. Cellular activity studies showed that disruption of Cl- ion homeostasis by PIT-1 or DM-PIT-1 preferentially promotes apoptotic cell death (Biswas et al. 2020).