Biological Activity
Beprist at 1a is a selective reversible inhibitor of protein disulfide isomerase (PDI)an enzyme in the endoplasmic reticulum th at catalyzes disulfide bond breakage and reformation to catalyze protein folding. Unlike most PDI inhibitorsBeprist at 1a binds at the substrate-binding siterather than the catalytic site. It blocked PDI activity with an IC50 value of 700 nM. PDI is up-regulated in several cancershas been implicated in neurodegenerative processesand plays an important role in thrombus formation. Beprist at 1a potently inhibited platelet aggregation and thrombus formation in vivo.
