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Article ; Online: Therapeutic disruption of RAD52-ssDNA complexation via novel drug-like inhibitors.

Bhat, Divya S / Malacaria, Eva / Biagi, Ludovica Di / Razzaghi, Mortezaali / Honda, Masayoshi / Hobbs, Kathryn F / Hengel, Sarah R / Pichierri, Pietro / Spies, M Ashley / Spies, Maria

NAR cancer

2023  Volume 5, Issue 2, Page(s) zcad018

Abstract: RAD52 protein is a coveted target for anticancer drug discovery. Similar to poly-ADP-ribose polymerase (PARP) inhibitors, pharmacological inhibition of RAD52 is synthetically lethal with defects in genome caretakers BRCA1 and BRCA2 (∼25% of breast and ... ...

Abstract RAD52 protein is a coveted target for anticancer drug discovery. Similar to poly-ADP-ribose polymerase (PARP) inhibitors, pharmacological inhibition of RAD52 is synthetically lethal with defects in genome caretakers BRCA1 and BRCA2 (∼25% of breast and ovarian cancers). Emerging structure activity relationships for RAD52 are complex, making it challenging to transform previously identified disruptors of the RAD52-ssDNA interaction into drug-like leads using traditional medicinal chemistry approaches. Using pharmacophoric informatics on the RAD52 complexation by epigallocatechin (EGC), and the Enamine
Language English
Publishing date 2023-05-01
Publishing country England
Document type Journal Article
ISSN 2632-8674
ISSN (online) 2632-8674
DOI 10.1093/narcan/zcad018
Database MEDical Literature Analysis and Retrieval System OnLINE

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