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Staurosporine



Staurosporine
Systematic (IUPAC) name
(9S,10R,11R,13R)-2,3,10,11,12,13-Hexahydro-
10-methoxy-9-methyl-11-(methylamino)-9,13-epoxy-
1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]
benzodiazonin-1-one
Identifiers
CAS number 62996-74-1
ATC code  ?
PubChem 5280487
Chemical data
Formula C28H26N4O3 
Mol. mass 466.53 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
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Staurosporine (antibiotic AM-2282) is a natural product originally isolated in 1977 from bacterium Streptomyces staurosporeus. It was the first of over 50 alkaloids to be isolated with this type of bis-indole chemical structure. The chemical structure of staurosporine was elucidated by X-ray analysis of a single crystal and the absolute stereochemical configuration by the same method in 1994.

Staurosporine was discovered to have biological activities ranging from anti-fungal to anti-hypertensive.[1] The interest in these activities resulted in a large investigative effort in chemistry and biology and the discovery of the potential for anti-cancer treatment.

The main biological activity of staurosporine is the inhibition of protein kinases through the prevention of ATP binding to the kinase. This is achieved through the stronger affinity of staurosporine to the ATP-binding site on the kinase.


References

  1. ^ [1] Rüegg UT, Burgess GM. (1989) Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases. Trends in Pharmacological Science 29: 253-257.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Staurosporine". A list of authors is available in Wikipedia.
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