Late-Stage Serine Modification Enables Noncanonical Peptide Synthesis.

ABSTRACT: Noncanonical amino acids play a critical role in enhancing drug efficacy, specificity, pharmacokinetics, and other key therapeutic properties. However, their incorporation into peptides or small molecules often presents significant synthetic challenges. Late-stage modification of natural residues, after the primary structural framework of a molecule is established, offers an efficient strategy for generating analogue libraries. Serine, one of the most abundant natural amino acids, remains underutilized due to the incompatibility of existing deoxygenative methods with complex peptides. Currently, no method is available for the late-stage modification of serine residues in peptides through carbon-carbon bond formation. Here, we address this gap by developing a site-selective, late-stage deox

SUBMITTER: Guo Z 

PROVIDER: S-EPMC12426918 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature