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LY249543
- Development stage
- Preclinical
- Lead developer
- Eli Lilly
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
01
Overview
LY249543 is a small molecule experimental drug that acts as the S-isomer of lometrexol, a folate analog antimetabolite. It functions primarily as an inhibitor of methylenetetrahydrofolate dehydrogenase/cyclohydrolase (MTHFD), an enzyme involved in one-carbon metabolism and crucial for nucleotide and amino acid biosynthesis. By inhibiting this enzyme, LY249543 disrupts folate-dependent metabolic pathways essential for DNA synthesis and cell proliferation, making it of interest in cancer research. The compound has been studied structurally in complex with its target enzyme but has not advanced to clinical approval[1][2][3][5].
- Other names
- lometrexol S-isomer
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