(A). Abridged biosynthesis of nocardicin A. The pentamodular NRPS comprised of NocA and NocB performs amino acid activation, peptide elongation, epimerization, and beta-lactam formation to produce a terminal thioesterase (NocTE) bound intermediate. NocTE catalyzes C-terminal L→D epimerization prior to hydrolytic release of pro-nocardicin G (1). Production of nocardicin G (2) by post-NRPS trimming of pro-nocardicin G, followed by late-stage tailoring steps, results in nocardicin A (3). (B). Proposed DPP and FP NocTE substrate analogue inhibitors. Electrophilic warheads highlighted in red.