193629-39-9, Name is N-Boc-3-(bromomethyl)piperidine, belongs to piperidines compound, is a common compound. 193629-39-9. In an article, authors is Actis, Marcelo L., once mentioned the new application about 193629-39-9.
Identification of the first small-molecule inhibitor of the REV7 DNA repair protein interaction
DNA interstrand crosslink (ICL) repair (ICLR) has been implicated in the resistance of cancer cells to ICL-inducing chemotherapeutic agents. Despite the clinical significance of ICL-inducing chemotherapy, few studies have focused on developing small-molecule inhibitors for ICLR. The mammalian DNA polymerase zeta, which comprises the catalytic subunit REV3L and the non-catalytic subunit REV7, is essential for ICLR. To identify small-molecule compounds that are mechanistically capable of inhibiting ICLR by targeting REV7, high-throughput screening and structure?activity relationship (SAR) analysis were performed. Compound 1 was identified as an inhibitor of the interaction of REV7 with the REV7-binding sequence of REV3L. Compound 7 (an optimized analog of compound 1) bound directly to REV7 in nuclear magnetic resonance analyses, and inhibited the reactivation of a reporter plasmid containing an ICL in between the promoter and reporter regions. The normalized clonogenic survival of HeLa cells treated with cisplatin and compound 7 was lower than that for cells treated with cisplatin only. These findings indicate that a small-molecule inhibitor of the REV7/REV3L interaction can chemosensitize cells by inhibiting ICLR.
Do you like my blog? If you like, you can also browse other articles about this kind. Thanks for taking the time to read the blog about 193629-39-9
Reference£º
Piperidine – Wikipedia,
Piperidine | C5H22593N – PubChem