Prevention of Protease-Induced Degradation of Desmoplakin via Small Molecule Binding
Laboratory studyOther animals
- Design
- Laboratory study
- Subjects
- In vitro protein assays; about 2,500 small molecules screened
- Dose used in the study
- Not stated in the abstract
- Duration
- Not stated in the abstract
- What was measured
- Whether small molecules protect desmoplakin protein from trypsin and calpain digestion in vitro, plus computational docking and molecular dynamics
What the authors reported
Several molecules, including sodium dodecyl sulfate, palmitoylethanolamide, GW0742, salirasib, eprosartan mesylate and GSK1838705A, prevented degradation of wild-type and disease-variant desmoplakin by trypsin and calpain without changing protease activity. Computational screening did not predict which molecules would work. Simulations suggest long hydrophobic molecules can sit in a groove beside the cleavage site.
Limits of this study
A test-tube protein study; it cannot show effect in people or animals. PEA was one of many hits and no concentration is given in the abstract. The authors declare no conflict of interest and state funders had no role.
Source
PubMed 38392596 · doi:10.3390/jpm14020163
Entry checked against the abstract on PubMed on 2026-09-22. The dose shown is the dose the researchers used. It is not a recommendation. How to read this page.