Actinonin

Actinonin is a peptidomimetic antibiotic produced by Actinomyces that inhibits aminopeptidases. It inhibits the following matrix metalloproteinases (MMPs): MMP-1 (K_i = 300 nM), MMP-3 (K_i = 1,700 nM), MMP-8 (K_i = 130 nM), and MMP-9 (K_i = 330 nM).¹} Actinonin acts as an herbicide by targeting plastid peptide deformylase, an enzyme required for N-terminal processing of plastid-encoded proteins.² Actinonin has also been identified as an effective inhibitor of human meprin α (K_i = 20 nM), a zinc endopeptidase that cleaves matrix proteins.³ More recently actinonin has been shown to inhibit tumor cell invasion and matrix degradation and to induce apoptosis in animal models by targeting human mitochondrial peptide deformylase.⁴

WARNING This product is not for human or veterinary use.

1. Wahl, R.C., Pulvino, T.A., Mathiowetz, A.M., et al. Hydroxamate inhibitors of human gelatinase B (92 kDa). Bioorg. Med. Chem. Lett. 5(4), 349-352 (1995).

2. Duke, S.O., and Dayan, F.E. Modes of action of microbially-produced phytotoxins. Toxins (Basel) 3(8), 1038-1064 (2011).

3. Kruse, M.N., Becker, C., Lottaz, D., et al. Human meprin α and β homo-oligomers: Cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem. J. 378(1), 383-389 (2004).

4. Lee, M.D., She, Y., Soskis, M.J., et al. Human mitochondrial peptide deformylase, a new anticancer target of actinonin-based antibiotics. J. Clin. Invest. 114(8), 1107-1116 (2004).