Drug intelligence / Profile preview

myriocin

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal, Oral
01

Overview

Myriocin, also known as antibiotic ISP-1 or thermozymocidin, is a non-proteinogenic amino acid isolated from various fungi, including Isaria sinclairii and Mycelia sterilia. It functions as a potent and selective inhibitor of serine palmitoyltransferase (SPT), the rate-limiting enzyme in the biosynthesis of sphingolipids. This inhibition leads to a reduction in cellular ceramide and sphingolipid levels. Myriocin is widely utilized in biochemical research as a tool for studying sphingolipid metabolism and has demonstrated significant immunosuppressant activity, even surpassing ciclosporin in potency. Notably, the multiple sclerosis drug fingolimod (FTY720) was developed through structural modifications of myriocin. While myriocin itself has not progressed to clinical trials due to potential gastrointestinal toxicity, its mechanism of action has been explored in preclinical models for a range of conditions, including metabolic disorders, neurobehavioral dysfunction, and certain viral infections.

Other names
antibiotic ISP-1thermozymocidinISP-1ISP1ISP 1ISP-I(2S,3R,4R,6E)-2-Amino-3,4-dihydroxy-2-(hydroxymethyl)-14-oxoicos-6-enoic acid
02

Targets

SPT (Serine palmitoyltransferase)

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