Small-Molecule Inhibition of UBE2T/FANCL-Mediated Ubiquitylation in the Fanconi Anemia Pathway | Zendy

Matthew Cornwell | Zendy; Graeme Thomson | Zendy; Julia Coates | Zendy; Rimma Belotserkovskaya | Zendy; Ian D. Waddell | Zendy; Stephen P. Jackson | Zendy; Yaron Galanty | Zendy

AI Assistant Blog Pricing

Home ZAIA Blog

Open Access

Small-Molecule Inhibition of UBE2T/FANCL-Mediated Ubiquitylation in the Fanconi Anemia Pathway

Author(s) -

Matthew Cornwell,

Graeme Thomson,

Julia Coates,

Rimma Belotserkovskaya,

Ian D. Waddell,

Stephen P. Jackson,

Yaron Galanty

Publication year - 2019

Publication title -

acs chemical biology

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.899

H-Index - 111

eISSN - 1554-8937

pISSN - 1554-8929

DOI - 10.1021/acschembio.9b00570

Subject(s) - fancd2 , fanconi anemia , ubiquitin , cancer research , microbiology and biotechnology , dna repair , ubiquitin conjugating enzyme , biology , chemistry , dna , ubiquitin ligase , genetics , gene

The Fanconi anemia pathway orchestrates the repair of DNA interstrand cross-links and stalled replication forks. A key step in this pathway is UBE2T and FANCL-dependent monoubiquitylation of the FANCD2-FANCI complex. The Fanconi anemia pathway represents an attractive therapeutic target, because activation of this pathway has been linked to chemotherapy resistance in several cancers. However, to date, very few selective inhibitors of ubiquitin conjugation pathways are known. By using a high-throughput screen-compatible assay, we have identified a small-molecule inhibitor of UBE2T/FANCL-mediated FANCD2 monoubiquitylation that sensitizes cells to the DNA cross-linking agent, carboplatin.

The content you want is available to Zendy users.

Already have an account? Click here to sign in.

Having issues? You can contact us here

Accelerating Research