The National Institute of General Medical Sciences (NIGMS) awarded Albert Einstein College of Medicine a Project Grant (CFDA 93.859 - Biomedical Research and Research Training) to expand the methodologies for chemical probe development toward underexplored biological targets and accelerate drug discovery. The $420,000 award, spanning 2024-2029, will enable two complementary research efforts:
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Improving the throughput of medicinal chemistry by expanding a high-throughput medicinal chemistry (HTMC) platform based on sulfur(VI) fluoride exchange (SuFEx) click-chemistry reactions. This will enable targeting of underexplored proteins, including those lacking distinct binding sites, by combining the HTMC platform with a covalent ligand approach.
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Developing strategies for the synthesis and evaluation of subcellular location-selective chemical probes. This includes establishing methods for extracellular-selective probe synthesis, demonstrating approaches to assess organelle-selective target engagement, and exploring the potential of modulating organelle selectivity to improve cellular potency.
The proposed research aims to fundamentally advance the fields of chemical biology and medicinal chemistry by accelerating and expanding the scope of chemical probe development in a proteome-wide and spatio-defined manner.
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