With the serious problem of multiple drug resistance to antibiotics among pathogenic bacteria spreading
across the world over the past 30 years, it is crucial to search for novel inhibitors with distinct modes of action
from diverse chemical classes. NAD+-dependent DNA ligases (LigAs) are essential enzymes in bacteria, vital for
DNA replication and repair. Additionally, LigAs exclusively exist in eubacteria and some viruses and are not
found in humans. Those enzymes have therefore been identified as attractive antibacterial drug targets. In this
review we explore the discovered inhibitors of LigA through high-throughput screening or virtual screening respectively
and their further structure optimization.
Keywords: DNA ligases, LigAs, inhibitors, antibacterial, HTS, VS.
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