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Staurosporine analogues from microbial and synthetic sources and their biological activities

In 1977 an unknown natural product was isolated from Streptomyces staurosporeus by Omura et al. during a search for new alkaloids present in actinomycetes and was given the name AM-2282. Later, the structure of AM-2282 was elucidated by single crystal X-ray analysis and renamed as staurosporine. It has been published that staurosporine and its analogues display strong inhibitory effect against a variety of kinases and a number of biological properties such as antifungal, antibacterial, and immunosuppressive activities. Despite strong inhibitory activity of staurosporine, a very high level of cross-reactivity makes it impossible to use staurosporine as a therapeutic agent. In the course of searching for other staurosporine-related compounds, a number of staurosporine analogues have been isolated from different microorganisms. In addition, a number of staurosporine analogues have been synthesized to improve the poor selectivity and target specificity of staurosporine which limited its clinical effectiveness. The review addresses staurosporine analogues from both microbial and synthetic sources and their biological activities.

 

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Staurosporine and its analogues, isolated from Streptomyces staurosporeus and other microorganisms or synthesized, display strong inhibitory effect against a variety of kinases and have various biological properties such as antifungal, antibacterial, and immunosuppressive activities but poor selectivity and target specificity limit their clinical effectiveness.

Related Products

Cat.No. Product Name Information
S1421 Staurosporine (STS) Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.

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