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Abstract
Orthosteric inhibitors of the human heterodimeric DNA mismatch repair complex MutSbeta were identified by high-throughput screening. Following extensive hit confirmation to remove false positives, two series were found to give consistent activity free of likely artefactual effects. Extensive hit profiling confirmed an ATP-competitive mode of action, and X-ray crystallography showed the inhibitors occupying the ATP-binding site of MSH3.
Supplementary materials
Title
Identification of orthosteric inhibitors of MutSβ ATPase function - supporting information
Description
Supporting information including chemistry experimental information, compound profiles, and X-ray Crystallography and Cryo-EM Protocols.
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