OCTN: A transporter with relevance to human pathophysiology, drug discovery & diagnostics

January 29, 2019

In the February 2019 issue of SLAS Discovery, a review by researchers from the University of Calabria (Italy) explores OCTNs, a small but intriguing group of transporters that are opening new frontiers in drug design research for improving drug delivery and predicting drug-drug interactions.

OCTNs mediate the flux of physiological organic cations through the plasma membrane of cells. Among the three members of the sub-family, OCTN1 and 2 are present in humans, while OCTN3 was lost during evolution. OCTN2 has a well-established role in maintaining the homeostasis of carnitine, an essential cofactor for producing energy from fatty acid metabolism. Some inherited defects of OCTN2 cause the primary carnitine deficiency, a severe muscle pathology that can be alleviated by administering carnitine as a drug. Noteworthy deficiencies mimicking the disease features can be caused as side effects by some drugs interfering with the carnitine absorption or by a strict vegetarian diet during pregnancy or infancy.

The pathophysiological role of OCTN2 is also confirmed by its presence in exosomes, nanovesicles released in the extracellular environment involved in cell to cell communication. Interestingly, the OCTN1 function remains relatively obscure. In fact, ablation of its gene apparently does not cause any problems in animals. However, some mutations of OCTN1 in humans are associated with inflammatory diseases such as the Crohn's disease.

Studies with the most up to date methodological approaches highlight a link of OCTN1 with inflammation, suggesting that molecules with anti-inflammatory or antioxidant properties might be OCTN1 ligands. In this frame, ergothioneine, a mushroom metabolite and acetylcholine have been proposed. The latter is a well-known neurotransmitter that also plays a role in inflammation via a non-neuronal cholinergic system. Both OCTN1 and OCTN2 show a side function in interaction with cationic drugs. These novel findings open new frontiers in drug design research for improving drug delivery and predicting drug-drug interactions.
-end-
"OCTN: A Small Transporter Subfamily with Great Relevance to Human Pathophysiology, Drug Discovery and Diagnostics" can be accessed for free for limited time at https://journals.sagepub.com/doi/full/10.1177/2472555218812821. For more information about SLAS and its journals, visit http://www.slas.org/journals.

About our Society and Journals

SLAS (Society for Laboratory Automation and Screening) is an international community of nearly 20,000 professionals and students dedicated to life sciences discovery and technology. The SLAS mission is to bring together researchers in academia, industry and government to advance life sciences discovery and technology via education, knowledge exchange and global community building.

SLAS DISCOVERY: 2016 Impact Factor 2.355. Editor-in-Chief Robert M. Campbell, Ph.D., Eli Lilly and Company, Indianapolis, IN (USA). SLAS Discovery (Advancing Life Sciences R&D) was previously published (1996-2016) as the Journal of Biomolecular Screening (JBS).

SLAS TECHNOLOGY: 2016 Impact Factor 2.632. Editor-in-Chief Edward Kai-Hua Chow, Ph.D., National University of Singapore (Singapore). SLAS Technology (Translating Life Sciences Innovation) was previously published (1996-2016) as the Journal of Laboratory Automation (JALA).

Follow SLAS on Twitter at @SLAS_Org.

Follow SLAS on Facebook at SocietyforLaboratoryAutomationandScreening.

Follow SLAS on YouTube at SLASvideo.

Follow SLAS Americas on LinkedIn at Society for Laboratory Automation and Screening (SLAS Americas).

Follow SLAS Europe on LinkedIn at Society for Laboratory Automation and Screening Europe (SLAS Europe).

SLAS (Society for Laboratory Automation and Screening)

Related Inflammation Articles from Brightsurf:

3D printed stents that treat inflammation
POSTECH Professor Dong-Woo Cho's research team develops bioink-loaded esophageal stents for treating radiation esophagitis.

New cause of inflammation in people with HIV identified
A new study led by researchers at Boston Medical Center examined what factors could be contributing to this inflammation, and they identified the inability to control HIV RNA production from existing HIV DNA as a potential key driver of inflammation.

Maltreatment tied to higher inflammation in girls
New research by a University of Georgia scientist reveals that girls who are maltreated show higher levels of inflammation at an early age than boys who are maltreated or children who have not experienced abuse.

A protein that controls inflammation
A study by the research team of Prof. Geert van Loo (VIB-UGent Center for Inflammation Research) has unraveled a critical molecular mechanism behind autoimmune and inflammatory diseases such as rheumatoid arthritis, Crohn's disease, and psoriasis.

Inflammation in the brain linked to several forms of dementia
Inflammation in the brain may be more widely implicated in dementias than was previously thought, suggests new research from the University of Cambridge.

Social isolation could cause physical inflammation
Social isolation could be associated with increased inflammation in the body new research from the University of Surrey and Brunel University London has found.

Hydrogels control inflammation to help healing
Researchers test a sampling of synthetic, biocompatible hydrogels to see how tuning them influences the body's inflammatory response.

Why beta-blockers cause skin inflammation
Beta-blockers are often used to treat high blood pressure and other cardiovascular diseases.

The 'inflammation' of opioid use
New research correlates inflammation in the brain and gut to negative emotional state during opioid withdrawal.

Using a common anticonvulsant to counteract inflammation
The interaction between a chromosomal protein called HMGB1 and a cellular receptor called RAGE is known to trigger inflammation.

Read More: Inflammation News and Inflammation Current Events
Brightsurf.com is a participant in the Amazon Services LLC Associates Program, an affiliate advertising program designed to provide a means for sites to earn advertising fees by advertising and linking to Amazon.com.