Description
Novobiocin is an aminocoumarin antibiotic that inhibits the ATPase activity of the B subunit of bacterial DNA gyrase. Novobiocin is most often used in the treatment of methicillin-resistant Staphylococcus aureus (MRSA) infections. In addition to its antibacterial activity, novobiocin also displays anticancer chemotherapeutic and anti-angiogenic properties. Novoboicin inhibits HIF-1α binding to transcriptional coactivator p300/CBP in tumor models and analogs of this compound are in development as HSP90 inhibitors.
References
Gunaherath GM, Marron MT, Wijeratne EM, et al. Synthesis and biological evaluation of novobiocin analogues as potential heat shock protein 90 inhibitors. Bioorg Med Chem. 2013 Sep 1;21(17):5118-29. PMID: 23859777.
Wu D, Zhang R, Zhao R, et al. A novel function of novobiocin: disrupting the interaction of HIF 1α and p300/CBP through direct binding to the HIF1α C-terminal activation domain. PLoS One. 2013 May 6;8(5):e62014. PMID: 23671581.
Walsh TJ, Standiford HC, Reboli AC, et al. Randomized Double-Blinded Trial of Rifampin with Either Novobiocin or Trimethoprim-Sulfamethoxazole against Methicillin-Resistant Staphylococcus aureus Colonization: Prevention of Antimicrobial Resistance and Effect of Host Factors on Outcome. Antimicrobial agents and chemotherapy 1993 Jun;37(6):1334–42. PMID: 8328783.
Maxwell A. The interaction between coumarin drugs and DNA gyrase. Mol Microbiol 1993;9(4):681–6. PMID: 8231802.
