Actinonin

Actinonin

Actinonin is a naturally occurring antibacterial agent that has been isolated from the actinomycete Actinomyces species. It is a hydroxamic acid that acts as a potent inhibitor of peptidyl deformylase, an enzyme involved in protein synthesis in bacteria.

History

Actinonin was first isolated in 1964 from the fermentation broth of Actinoplanes missouriensis. It was identified as a potent antibacterial agent, particularly against Gram-positive bacteria.

Structure and Properties

Actinonin is a small molecule with a molecular weight of 270.3 g/mol. It is composed of a hydroxamic acid group, which is responsible for its activity as a peptidyl deformylase inhibitor, and a tetrahydrofuran ring, which contributes to its stability and lipophilicity.

Mechanism of Action

Actinonin inhibits peptidyl deformylase, an enzyme that is essential for protein synthesis in bacteria. By binding to the active site of the enzyme, actinonin prevents the removal of the formyl group from the initiating methionine residue of nascent polypeptide chains, thereby blocking protein synthesis and inhibiting bacterial growth.

Clinical Use

While actinonin has potent antibacterial activity, its clinical use has been limited due to its poor solubility and bioavailability. However, recent research has focused on developing actinonin derivatives with improved pharmacokinetic properties, and some of these compounds are currently in preclinical development.

See Also

• Peptidyl deformylase
• Actinomyces
• Antibacterial agent

References

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