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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).

References associated with 2.B.65 family:

Biswas, O., N. Akhtar, Y. Vashi, A. Saha, V. Kumar, S. Pal, S. Kumar, and D. Manna. (2020). Chloride Ion Transport by PITENINs across the Phospholipid Bilayers of Vesicles and Cells. ACS Appl Bio Mater 3: 935-944. 35019295