Mujeeb A. Wakeel

Lipidation of macrocyclic peptides is a pharmaceutically relevant chemical transformation. (1) Illustratively, lipidation enhances the antibiotic activity of teicoplanin and daptomycin. (2,3) Lipidation alters the peptide transport properties across biological membranes, an observation that has been exploited for chemical biology as well as therapeutic applications.

Lipidation of macrocyclic peptides is a pharmaceutically relevant chemical transformation. (1) Illustratively, lipidation enhances the antibiotic activity of teicoplanin and daptomycin. (2,3) Lipidation alters the peptide transport properties across biological membranes, an observation that has been exploited for chemical biology as well as therapeutic applications.

Post-translational modification of proteins during primary biological processes such as signaling and protein degradation relies on precise protein/protein interactions between modification enzymes and protein substrate(s). These interactions involve crosstalk between higher-order protein secondary and tertiary structural features that consist of amino acid residues that are spread across the entire protein sequence.