About
Contact & Profiles
A5001725729
Research Areas
- Cancer therapeutics and mechanisms
- DNA and Nucleic Acid Chemistry
- DNA Repair Mechanisms
DNA polymerase theta (Polθ) is an attractive synthetic lethal target for drug discovery, predicted to be efficacious against breast and ovarian cancers harboring BRCA-mutant alleles. Here, we describe our hit-to-lead efforts in search of a selective inhibitor human Polθ (encoded by POLQ). A high-throughput screening campaign 350,000 compounds identified 11 micromolar hit, giving rise the N2-substituted fused pyrazolo series, which was validated biophysical methods. Structure-based design...
10.1021/acs.jmedchem.2c00998
article
EN
Journal of Medicinal Chemistry
2022-09-20
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