Aleplasinin

Aleplasinin
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
DrugBank
KEGG
UNII
  • InChI=1S/C28H27NO3/c1-18-6-5-7-20(14-18)21-10-13-25-23(15-21)24(26(30)27(31)32)17-29(25)16-19-8-11-22(12-9-19)28(2,3)4/h5-15,17H,16H2,1-4H3,(H,31,32)
    Key: HSXLMAFNWCSZGP-UHFFFAOYSA-N
  • CC1=CC(=CC=C1)C2=CC3=C(C=C2)N(C=C3C(=O)C(=O)O)CC4=CC=C(C=C4)C(C)(C)C
Properties
C28H27NO3
Molar mass 425.5 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

Aleplasinin is an experimental drug belonging to the class of plasminogen activator inhibitors (PAI-1 inhibitors). It is being developed by the U.S. pharmaceutical company Wyeth for potential use in the treatment of Alzheimer's disease.

Mechanism of action

In Alzheimer's disease, senile plaques composed of misfolded beta-amyloid peptides accumulate within neurons, together with neurofibrils. This accumulation leads to necrosis of the nerve cells.

The beta-amyloid peptide activates the tissue-specific plasminogen activator tPA (tissue plasminogen activator), which in turn activates plasminogen, thereby inducing the formation of plasmin. Plasmin promotes the degradation of beta-amyloid.

tPA, however, is inhibited by the plasminogen activator inhibitor PAI-1. In Alzheimer's disease, this inhibitor exhibits markedly increased activity. Aleplasinin selectively inhibits PAI-1, thereby preventing the enzyme inhibition of tPA. As a result, the degradation of the beta-amyloid peptide is enhanced, preventing its aggregation with neurofibrils in nerve cells. This process helps to prevent neuronal necrosis.

Literatur


References

This article is issued from Wikipedia. The text is available under Creative Commons Attribution-Share Alike 4.0 unless otherwise noted. Additional terms may apply for the media files.