Peptide–Targeting Ligand Conjugates

Bio-Synthesis provides peptide–targeting ligand conjugation services and builds chemically defined peptide–targeting ligand conjugates by attaching non-drug small-molecule ligands to a chosen peptide site (N-/C-terminus, single-Cys, or handle-enabled chemistry; project-dependent) to support research-stage and preclinical workflows.

Peptide–targeting ligand conjugates are non-drug peptide conjugates in which a peptide is covalently linked to a small-molecule targeting ligand that enhances binding to a specific receptor, transporter, or tissue-associated target. The ligand is used for recognition and localization—not for pharmacological payload delivery. ^{[1], [2]}

In a typical design, the peptide may provide binding motifs, transport elements, or a structural scaffold, while the small-molecule ligand provides target specificity (e.g., receptor engagement) or uptake bias in a defined biological context. Spacer selection (e.g., PEG) and site-defined attachment help preserve peptide function and ligand recognition while reducing heterogeneity. ^[2]

This category differs from peptide–drug conjugates (PDCs), where the payload is a therapeutic drug. Here, the conjugated small molecule is typically a non-drug ligand (e.g., folate, GalNAc, sugars/glycans, or other receptor-binding motifs) used for research and early development evaluation. ^{[3], [4]}

Explore related pages: Non-drug peptide–small molecule/ligand conjugates · Peptide–GalNAc conjugates · Peptide–folate conjugates · Peptide–imaging conjugates