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Allosteric regulation of DNA binding and target residence time drive the cytotoxicity of phthalazinone-based PARP-1 inhibitors

Moriah R. Arnold, Marie-France Langelier, Jessica Gartrell, Ilsa T. Kirby, Daniel J. Sanderson, Daniel S. Bejan, Justina Šileikytė, Sunil K. Sundalam, Shanthi Nagarajan, Parthiban Marimuthu, Anna K. Duell, Anang A. Shelat, John M. Pascal, Michael S. Cohen

2022Cell chemical biology11 citationsDOI

Topics & Concepts

Allosteric regulationCytotoxicityPoly ADP ribose polymeraseNAD+ kinasePARP inhibitorDNAChemistryDNA replicationBinding siteBiochemistryBiologyCell biologyStereochemistryIn vitroEnzymePolymerasePARP inhibition in cancer therapyIntegrated Circuits and Semiconductor Failure AnalysisDNA Repair Mechanisms
Allosteric regulation of DNA binding and target residence time drive the cytotoxicity of phthalazinone-based PARP-1 inhibitors | Litcius