A fungal metabolite with antimuscarinic and anticancer activities
Migrastatin is a bacterial metabolite that has been found in Streptomyces with antimuscarinic and anticancer activities.1,2 It binds to M1-5 muscarinic acetylcholine receptors (Kis = >200, 200, 31, 43, and >200 µM, respectively) and inhibits calcium mobilization induced by carbamoylcholine in SK-N-SH cells (IC50 = 28 µM), as well as in primary rat bladder smooth muscle cells.1 Migrastatin inhibits the migration of EC17 esophageal cancer cells in a wound healing assay (IC50 = 10 µg/ml) and 4T1 mouse mammary carcinoma cells in a chamber cell migration assay (IC50 = 29 µM).2 It enhances cytotoxicity induced by vinblastine in vincristine-resistant P388/VCR cells.3
1.Nakae, K., Nishimura, Y., Ohba, S., et al.Migrastatin acts as a muscarinic acetylcholine receptor antagonistJ. Antibiot. (Tokyo)59(11)685-692(2006) 2.Reymond, S., and Cossy, J.Migrastatin and analogues: New anti-metastatic agentsC. R. Chim.11(11-12)1447-1462(2008) 3.Takemoto, Y., Tashiro, E., and Imoto, M.Suppression of multidrug resistance by migrastatinJ. Antibiot. (Tokyo)59(7)435-438(2006)
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