Actin-binding compounds that affect the kinetics of the interaction of cardiac myosin with actin

Abstract

the effects of ten actin binding compounds on the interaction of cardiac myosin subfragment 1 (S1) with pyrene labeled F actin (PFA). These compounds, previously identified from a small-molecule high-throughput screen (HTS), perturb the microsecond structural dynamics of actin and the steady-state activity of actin-activated myosin ATPase. In the present study, we have further characterized their mechanisms of action by measuring their effects on PFA fluorescence, which is decreased specifically by the strong binding of myosin to actin, and is restored upon release of S1 by MgATP...