A VersaTile-driven platform for rapid hit-to-lead development of engineered lysins.

Gerstmans, H; Grimon, D; Gutiérrez, D; Lood, C; Rodríguez, A; van Noort, V; Lammertyn, J; Lavigne, R et al. · Sci Adv · 2020

basic_science · Level V

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Abstract

Health care authorities are calling for new antibacterial therapies to cope with the global emergence of antibiotic-resistant bacteria. Bacteriophage-encoded lysins are a unique class of antibacterials with promising (pre)clinical progress. Custom engineering of lysins allows for the creation of variants against potentially any bacterial pathogen. We here present a high-throughput hit-to-lead development platform for engineered lysins. The platform is driven by VersaTile, a new DNA assembly method for the rapid construction of combinatorial libraries of engineered lysins. We constructed approximately 10,000 lysin variants. Using an iterative screening procedure, we identified a lead variant with high antibacterial activity against <i>Acinetobacter baumannii</i> in human serum and an ex vivo pig burn wound model. This generic platform could offer new opportunities to populate the preclinical pipeline with engineered lysins for diverse (therapeutic) applications.