OCTN Cation Transporters in Health and Disease Role as Drug Targets and Assay Development

摘要: The three members of the organic cation transporter novel subfamily are known to be involved in interactions with xenobiotic compounds. These proteins characterized by 12 transmembrane segments connected nine short loops and two large hydrophilic loops. It has been recently pointed out that acetylcholine is a physiological substrate OCTN1. Its transport could nonneuronal cholinergic functions. OCTN2 maintains carnitine homeostasis, resulting from intestinal absorption, distribution tissues, renal excretion/reabsorption. OCTN3, identified only mouse, mediates also transport. OCTN1 associated several pathologies, such as inflammatory bowel disease, primary deficiency, diabetes, neurological disorders, cancer, thus representing useful pharmacological targets. function interaction drugs OCTNs have studied intact cell systems proteoliposomes. latter experimental model enables reduced interference other transporters or enzyme pathways. Using proteoliposomes, molecular bases toxicity some revealed. Therefore, proteoliposomes represent promising tool suitable for large-scale screening chemicals regarding human health.