Proteasome Inhibition Measurements: Clinical Application

Proteasome inhibition measurements: clinical application.

BACKGROUND PS-341, a selective inhibitor of the proteasome, currently is under evaluation as an anticancer agent in multiple phase I clinical trials. In animal-model studies, PS-341 was rapidly removed from the vascular compartment and distributed widely, quickly approaching the limits of detection. An accurate pharmacodynamic assay has been developed as an alternative or complement to pharmaco...

Lp ( a ) Measurements for Clinical Application

Proteasome inhibition in hypertrophied myocardium.

CARDIAC REMODELING has been described as both an adaptive and a maladaptive process. The adaptive component enables the heart to maintain function in response to pressure overload and has the effect of decreasing ventricular wall stress and compensates for the increased workload preserving cardiac function. Along with the changes in ventricular mechanics, the development of hypertrophy is accom...

Proteasome Inhibition in Lymphoproliferative Disorder

Proteasomes are multi-subunit protein complexes, which present numerous targets for therapeutic interference. The most commonly used proteasome is 26S proteasome, which contains one 20S proteolytic core subunit and two 19S regulatory cap subunits. There are three different types of active sites of 20S proteolytic core and both, natural and synthetic proteasome inhibitors have been developed for...

Proteasome inhibition during myocardial infarction.

The ubiquitin-proteasome system (UPS) plays a central role in protein degradation and regulates a variety of critical cellular processes. During recent years, the cardiac UPS has become increasingly recognized as a key regulator of cardiac function under both physiological and pathological conditions. Numerous studies have demonstrated that altered UPS function is involved in the pathogenesis o...