CONTEXT

Peptide deformylase (PDF) is an essential enzyme found in all Gram-positive and Gram-negative bacteria and the natural target of actinonin, a natural antibiotic substance produced by a Streptomyces sp. For the past decade, PDF has been selected as a target of choice for the selection of new antibiotics using state-of-the-art drug discovery methods. As a consequence, numerous PDF inhibitors (PDFI) mimicking actinonin have therefore been discovered. However, it has also been shown that one type of PDF has also been discovered in human mitochondria leading to an issue as for the action of such PDFI. Even if mitochondrial membranes are generally considered as impermeable, great caution has to be taken.