OCTN1: A Widely Studied but Still Enigmatic Organic Cation Transporter Linked to Human Pathology and Drug Interactions

• Published in: International journal of molecular sciences Vol. 23; no. 2; p. 914
• Main Authors: Pochini, Lorena, Galluccio, Michele, Scalise, Mariafrancesca, Console, Lara, Pappacoda, Gilda, Indiveri, Cesare
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 14.01.2022; MDPI
• Subjects: Acetylation; Animals; Binding Sites; Biological Transport; Biomarkers; Breastfeeding & lactation; Disease Susceptibility; Drug Interactions; Ergothioneine - metabolism; Gene Expression Regulation - drug effects; Gene Knockdown Techniques; Genes; Humans; Localization; Metabolism; Metabolites; Models, Molecular; Molecular Conformation; Nervous system; Organ Specificity; Organic Cation Transport Proteins - chemistry; Organic Cation Transport Proteins - genetics; Organic Cation Transport Proteins - metabolism; Oxidative stress; Pathology; Physiology; Protein Binding; Proteins; Review; Stem cells; Structure-Activity Relationship; Symporters - chemistry; Symporters - genetics; Symporters - metabolism; ergothioneine; inflammation; pharmacology; carnitine; health; cancer; acetylcholine; oxidative stress
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms23020914

The Novel Organic Cation Transporter, OCTN1, is the first member of the OCTN subfamily; it belongs to the wider Solute Carrier family SLC22, which counts many members including cation and anion organic transporters. The tertiary structure has not been resolved for any cation organic transporter. The functional role of OCNT1 is still not well assessed despite the many functional studies so far conducted. The lack of a definitive identification of OCTN1 function can be attributed to the different experimental systems and methodologies adopted for studying each of the proposed ligands. Apart from the contradictory data, the international scientific community agrees on a role of OCTN1 in protecting cells and tissues from oxidative and/or inflammatory damage. Moreover, the involvement of this transporter in drug interactions and delivery has been well clarified, even though the exact profile of the transported/interacting molecules is still somehow confusing. Therefore, OCTN1 continues to be a hot topic in terms of its functional role and structure. This review focuses on the most recent advances on OCTN1 in terms of functional aspects, physiological roles, substrate specificity, drug interactions, tissue expression, and relationships with pathology.