Ontology highlight
ABSTRACT:
SUBMITTER: Malik FI
PROVIDER: S-EPMC4090309 | biostudies-literature | 2011 Mar
REPOSITORIES: biostudies-literature
Science (New York, N.Y.) 20110301 6023
Decreased cardiac contractility is a central feature of systolic heart failure. Existing drugs increase cardiac contractility indirectly through signaling cascades but are limited by their mechanism-related adverse effects. To avoid these limitations, we previously developed omecamtiv mecarbil, a small-molecule, direct activator of cardiac myosin. Here, we show that it binds to the myosin catalytic domain and operates by an allosteric mechanism to increase the transition rate of myosin into the ...[more]