Stauprimide
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Stauprimide is a
semi-synthetic Semisynthesis, or partial chemical synthesis, is a type of chemical synthesis that uses chemical compounds isolated from natural sources (such as microbial cell cultures or plant material) as the starting materials to produce novel compounds with ...
analog Analog or analogue may refer to: Computing and electronics * Analog signal, in which information is encoded in a continuous variable ** Analog device, an apparatus that operates on analog signals *** Analog electronics, circuits which use analog ...
of the
staurosporine Staurosporine (antibiotic AM-2282 or STS) is a natural product originally isolated in 1977 from the bacterium '' Streptomyces staurosporeus''. It was the first of over 50 alkaloids to be isolated with this type of bis-indole chemical structure. Th ...
family of
indolocarbazole Indolocarbazoles (ICZs) are a class of compounds that are under current study due to their potential as anti-cancer drugs and the prospective number of derivatives and uses found from the basic backbone alone. First isolated in 1977, a wide range o ...
s. Stauprimide was first published in 1994 as part of an extensive structure-activity investigation to improve the selective inhibition of
protein kinase C In cell biology, Protein kinase C, commonly abbreviated to PKC (EC 2.7.11.13), is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and t ...
as a potential antitumor agent. More recently, stauprimide has been shown to increase the efficiency of the directed differentiation of mouse and human embryonic stem cells in synergy with defined extracellular signaling cues. Stauprimide interacts with
NME2 Nucleoside diphosphate kinase B is an enzyme that in humans is encoded by the ''NME2'' gene. Function Nucleoside diphosphate kinase (NDK) exists as a hexamer composed of 'A' (encoded by NME1) and 'B' (encoded by this gene) isoforms. Multiple a ...
(PUF) transcription factor to down-regulate
c-Myc ''Myc'' is a family of regulator genes and proto-oncogenes that code for transcription factors. The ''Myc'' family consists of three related human genes: ''c-myc'' (MYC), ''l-myc'' (MYCL), and ''n-myc'' (MYCN). ''c-myc'' (also sometimes referre ...
expression, leading to differentiation of stem cells.


See also

*
Staurosporine Staurosporine (antibiotic AM-2282 or STS) is a natural product originally isolated in 1977 from the bacterium '' Streptomyces staurosporeus''. It was the first of over 50 alkaloids to be isolated with this type of bis-indole chemical structure. Th ...
*
Rebeccamycin Rebeccamycin (NSC 655649) is a weak topoisomerase I inhibitor isolated from ''Nocardia sp.'' It is structurally similar to staurosporine, but does not show any inhibitory activity against protein kinases. It shows significant antitumor properties ...
*
K252a K252a is an alkaloid isolated from '' Nocardiopsis'' bacteria. This staurosporine analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50 = 1.8 and 1.7 nmol/ L, respectively). At higher concentrations it ...
*
Midostaurin Midostaurin, sold under the brand name Rydapt & Tauritmo both by Novartis, is a multi-targeted protein kinase inhibitor that has been investigated for the treatment of acute myeloid leukemia (AML), myelodysplastic syndrome (MDS) and advanced sys ...


References

{{reflist Indolocarbazoles Protein kinase inhibitors