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Synthesis of Azumamide Analogs

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Synthesis of Azumamide Analogs
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22
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BiosynthesisMeat analogueChemistryZigarettenschachtelGemstoneChemical structureThermoformingAageSteam distillationEnzymeCancerChain (unit)Chemical compoundActive siteFunctional groupChemical reactionCell (biology)ProteinSide chainEnzyme inhibitorDoppelbindungMethylgruppeHistone deacetylaseHistoneDNS-SyntheseAcetylationTube (container)ChromatinGeneGene expressionMeat analogueGenregulationLecture/Conference
Transcript: English(auto-generated)
The chromatin is a structure composed of DNA and histone proteins. How tightly packed this structure is depends on the acetylation of the histones. Histone as a tube transferase catalyzes the acetylation of the histones, which will result in a more loose form of the structure.
Histone deacetylase catalyzes the reverse reaction, thereby making a more tightly packed structure. Inhibitors of these histone deacetylases have shown potential in cancer treatment, and this can in part be explained by the histone deacetylase enzymes being upregulated in cancer cells.
The upregulation of the histone deacetylase enzymes will result in a tighter packed structure and thereby a reduced expression of poor apoptotic genes. Natural compounds exist that are inhibitors of these enzymes.
These include the episidin, azimimides, romidepsin, and lagazole. In my project, I have synthesized analogs of the azimimides, shown here, where the methyl group have been removed and the double bond have moved to a similar position as lagazole and romidepsin, and a transconfiguration as well.
Another interesting compound that we will synthesize is where we have attached the side chain similar to lagazole. These compounds will be tested in enzyme assays at our own laboratory.