ArticleACS medicinal chemistry letters2026
High-Throughput Cardiac Hypertrophy Phenotyping Supports Lead Optimization of GRK5 Inhibitors.
Article in ACS medicinal chemistry letters, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Cardiac hypertrophy poses a clinical challenge in heart failure progression with limited therapeutic options to reverse the process of pathological remodeling. We present a high-throughput phenotypic screening assay designed to support lead optimization from novel approaches. A mixed cell culture from neonatal rat hearts was established, allowing simultaneous assessment of cardiomyocytes and noncardiomyocytes within a shared physiologically relevant microenvironment. Customized CellProfiler-based image analysis extracted multiparametric morphological data that was merged in a "Hypertrophy Score" metric for quantitative analyses. The assay was applied to investigate G protein-coupled receptor kinase 5 (GRK5) as a promising target in cardiac hypertrophy. Structure-activity and -property relationships from a focused GRK5 inhibitor collection revealed a negative influence on cellular efficacy by lipophilic and covalently reactive compounds. Correlating biochemical with cellular data eliminated GRK6 as a common off-target concern and underlined the value of potent GRK5 versus GRK2 inhibition. Diastereomers
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