Apicidin

Apicidin is a cyclic tetrapeptide that is derived from Fusarium species of fungi. It is a potent Histone deacetylase inhibitor with antiproliferative activity.

History

Apicidin was first isolated in 1996 from the fungus Fusarium pallidoroseum. It was discovered during a screening for new antiparasitic agents.

Structure and Synthesis

Apicidin is a cyclic tetrapeptide, composed of four amino acids: tryptophan, cysteine, dihydroxy-isovaleric acid, and phenylalanine. The synthesis of apicidin involves the formation of a peptide bond between these four amino acids, followed by cyclization to form the cyclic structure.

Mechanism of Action

Apicidin exerts its antiproliferative effects by inhibiting histone deacetylase, an enzyme that is involved in the regulation of gene expression. By inhibiting this enzyme, apicidin alters the acetylation state of histones, leading to changes in gene expression that can inhibit cell proliferation.

Clinical Use

Apicidin has shown promise in preclinical studies for the treatment of various types of cancer, including leukemia, breast cancer, and colorectal cancer. However, it is not currently approved for use in humans.

See Also

• Histone deacetylase inhibitor
• Antiproliferative
• Cyclic peptide

References

Apicidin Resources
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