Drug intelligence / Profile preview

tunicamycin

Development stage
Phase 3
Lead developer
Streptomyces clavuligerus (natural producer)
Modality
Small Molecules
01

Overview

Tunicamycin is a mixture of homologous nucleoside antibiotics produced by Streptomyces species, including Streptomyces clavuligerus and Streptomyces lysosuperficus. It acts as a potent inhibitor of the UDP-HexNAc: polyprenol-P HexNAc-1-P family of enzymes, most notably GlcNAc phosphotransferase (GPT), which catalyzes the first step in N-linked glycoprotein synthesis. By blocking this enzyme, tunicamycin prevents the transfer of N-acetylglucosamine from UDP-N-acetylglucosamine to dolichol phosphate, thereby inhibiting N-linked glycosylation in eukaryotic cells. This leads to cell cycle arrest at the G1 phase and induces endoplasmic reticulum (ER) stress and unfolded protein response. Tunicamycin is widely used as an experimental tool in cell biology to study ER stress, autophagy induction, protein palmitoylation inhibition, and glycoprotein synthesis pathways[1][3][5]. It also exhibits antimicrobial activity against gram-positive bacteria, fungi, yeasts, and viruses[10].

Other names
tunicamycin Atunicamycin B2tunicamycin V(+)-tunicamycin V
02

Targets

GNPTAB (N-acetylglucosamine-1-phosphotransferase alpha/beta subunits)

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