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Article Abstract
Orthosteric inhibitors of the human heterodimeric DNA mismatch repair complex MutSβ 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 resulted in our obtaining the first reported X-ray and cryo-EM structures of small molecule inhibitors of MutSβ occupying the ATP-binding site of MSH3.
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| http://dx.doi.org/10.1016/j.bmcl.2025.130326 | DOI Listing |
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