Inhibitor for DNA Helicase Heliquinomycin

In 1976, Hoffmann-Berling et al.^{5, 6)}, Heidelberg University in Germany and Mackay and Linn ⁷⁾, UC Berkeley in the United States first reported that a protein untwisted double-stranded DNA in an ATP-dependent manner. In 1978, the term "Helicase," referring to ATP-dependent double-stranded DNA unwinding enzyme, was proposed by Hoffmann-Berling ⁸⁾.
DNA helicases move across DNA using energy from ATP hydrolysis and generate single-stranded DNA breaking hydrogen bonds between nucleotide base pairs in DNA double helix. DNA helicases play important roles in maintaining genomic integrity and cellular homeostasis, such as DNA replication, transcription and DNA repair. The importance is evident from the fact that mutations in helicase genes are associated with genetic disorders such as Werner syndrome, Bloom syndrome and RRAPADILINO syndrome as well as various types of cancer ⁹⁾.

Selective inhibitors of helicase activity are useful in elucidating helicase functions in cell proliferation and expected as lead compounds for development of selective antitumor agents. Compounds that inhibit DNA helicases, such as Heliquinomycin ⁴⁾, have been reported, and compounds that inhibit viral helicase-primase complex are being developed as antiviral agents.