Discovery of novel cardiac troponin activators using fluorescence polarization-based high throughput screening assays.

ABSTRACT: The large unmet demand for new heart failure therapeutics is widely acknowledged. Over the last decades the contractile myofilaments themselves have emerged as an attractive target for the development of new therapeutics for both systolic and diastolic heart failure. However, the clinical use of myofilament-directed drugs has been limited, and further progress has been hampered by incomplete understanding of myofilament function on the molecular level and screening technologies for small molecules that accurately reproduce this function in vitro. In this study we have designed, validated and characterized new high throughput screening platforms for small molecule effectors targeting the interactions between the troponin C and troponin I subunits of the cardiac troponin complex. Fluorescenc

SUBMITTER: Parijat P 

PROVIDER: S-EPMC10063609 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature