1.D.102.  The Monopeptide-based Artificial Anion Channel (MP-AAC) Family 

Chloride-selective transmembrane carriers or channels might be useful in treating channelopathies and/or cancers. Existing channels are limited by their large molecular weights, weak activities or low anion

selectivities. Ren et al. 2018 described a readily accessible and robust monopeptide-based scaffold
for the reliable construction of halogen bond-mediated artificial anion channels via directional
assembly of electron-deficient iodine atoms, which create a transmembrane pathway for facilitating
anion transport. The high intrinsic modularity of the backbone of the scaffold, which enables the
rapid and combinatorial optimization of the transport activity and selectivity of channels,
effectively allows synthesis of a highly active chloride channel A10. Such high activity in chloride transport
subsequently leads to an excellent IC50 value of 20 muM toward inhibiting the growth of human breast
cancer cells (BT-474), an anticancer activity that is even higher than that of the well-known
anticancer agent cisplatin.



Ren, C., X. Ding, A. Roy, J. Shen, S. Zhou, F. Chen, S.F. Yau Li, H. Ren, Y.Y. Yang, and H. Zeng. (2018). A halogen bond-mediated highly active artificial chloride channel with high anticancer activity. Chem Sci 9: 4044-4051.