Specificity of the ergothioneine transporter natively expressed in HeLa cells
Open accessAbstract
Ergothioneine is a biologically important compound that has been shown to be transported by the organic cation transporter novel type 1 (OCTN1). Following this discovery, a variety of alternate functions for OCTN1 have been suggested including an integral function in the extra-neuronal cholinergic system. The present study reaffirms the primacy of ergothioneine over these alternate substrates using natively expressed OCTN1 in HeLa cells. Besides the general transport inhibitors, quinidine, verapamil and pyrilamine no other putative substrate inhibited ergothioneine transport significantly, with only a slight inhibition demonstrated by carnitine. Even compounds structurally similar to ergothioneine failed to inhibit ergothioneine uptake, suggesting high selectivity of OCTN1. Ergothioneine was found to be avidly accumulated even at low concentrations (300 nM) by HeLa cells.
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SLC22A4 and its homologues have significant specificity for ERG and weak activity for various drugs.
“Subsequent work(87,169–172) has confirmed and reinforced this view of SLC22A4 and its homologues(173) as having significant specificity for ERG, and weak activity for various drugs(174–177).”
From The biology of ergothioneine, an antioxidant nutraceutical (2020) · cites this paper as [87]
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- Authors
- Tucker, R. A. J., Cheah, I. K., & Halliwell, B.
- Affiliations
- National University of Singapore (SG)
- Corresponding author
- Halliwell, Barry
- Venue
- Biochemical and Biophysical Research Communications
- Publisher
- Elsevier BV
- Published
- 2019-05
- Volume
- 513
- Issue
- 1
- Pages
- 22-27
- ISSN
- 0006-291X (ISSN-L)
- OpenAlex
- W2931654306
- Cited by
- 38
- References
- 39
- Citations by year
- 2026: 5 · 2025: 6 · 2024: 4 · 2023: 2 · 2022: 5 · 2021: 8 · 2020: 7 · 2019: 1
- FWCI
- 2.21
- Type
- journal article
- Language
- en
- Open access
- Licence
- Locations
- Biochemical and Biophysical Research Communications (publishedVersion)
- PubMed (publishedVersion)
- National University of Singapore (submittedVersion, cc-by-nc-nd)
- Funders
- National Medical Research Council (NMRC/1264/2010/082/12)
- Topics
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Sulfur Compounds in Biology
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Amino Acid Enzymes and Metabolism
- Keywords
- ergothioneine, OCTN1, organic cation transporters, substrate specificity, HeLa cells, L-carnitine, quinidine, verapamil, mepyramine, cholinergic system, amino acid transport
- MeSH terms
- Antioxidants, Ergothioneine, HeLa Cells, Humans, Substrate Specificity, Organic Cation Transport Proteins, Symporters
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