Aureobasidins as new inhibitors of P-glycoprotein in multidrug resistant tumor cells.

Abstract

Cyclic depsipeptide antibiotic aureobasidin A (AbA) and its analogs were tested for the inhibitory activity of P-glycoprotein in multidrug resistant cancer cells as well as for the antifungal activity. Some analogs with lower antifungal activity than AbA showed higher inhibition of P-glycoproteins indicating difference of the structure-activity relationships between the two activities. Among AbA analogs tested, [D-beta-hydroxy-methylvalyl9]-AbA newly prepared by chemical synthesis, which had much lower antifungal activity than AbA, showed 10-fold higher inhibitory activity of P-glycoprotein than AbA.

• Authors: T Kurome, K Takesako, I Kato
• Journal: The Journal of antibiotics (J Antibiot (Tokyo)) Vol. 51 Issue 3 Pg. 353-8 (Mar 1998) ISSN: 0021-8820 [Print] England
• PMID: 9589072 (Publication Type: Journal Article)

Chemical References

• ATP Binding Cassette Transporter, Subfamily B, Member 1
• ATP-Binding Cassette Transporters
• Antifungal Agents
• Depsipeptides
• Multidrug Resistance-Associated Proteins
• Peptides, Cyclic
• aureobasidin A
• Vincristine

Topics

• ATP Binding Cassette Transporter, Subfamily B, Member 1 (antagonists & inhibitors)
• ATP-Binding Cassette Transporters (biosynthesis)
• Antifungal Agents (pharmacology)
• Depsipeptides
• Humans
• Multidrug Resistance-Associated Proteins
• Peptides, Cyclic (pharmacology)
• Structure-Activity Relationship
• Tumor Cells, Cultured
• Vincristine (pharmacokinetics)