Structure‐Based Gene Targeting Discovery of Sphaerimicin, a Bacterial Translocase I Inhibitor

Infectious and parasitic disease is estimated to be the second leading cause of death worldwide and is becoming increasingly problematic due to the steady rise in drug resistant pathogens.[1] The increase in resistance has also coincided with decreasing numbers of antibiotics brought to the market for the past few decades.[2] Naturally, it is paramount to global human health that new antibiotics are developed, particularly those with novel modes of action and/or unique chemical structures. Herein we present the discovery of sphaerimicin A, a sulfated hybrid polyketide-nucleoside that can be considered to fit both of these descriptors.