Drug
conjugates are chemotherapeutic or cytotoxic agents covalently
linked to targeting ligands such as an antibody or a peptide via a
linker. While antibody–drug conjugates (ADCs) are now clinically
established for cancer therapy, peptide–drug conjugates (PDCs)
are gaining recognition as a new modality for targeted drug delivery
with improved efficacy and reduced side effects for cancer treatment.
The linker in a drug conjugate plays a key role in the circulation
time of the conjugate and release of the drug for full activity at
the target site. Herein, we highlight the main linker chemistries
utilized in the design of PDCs and discuss representative examples
of PDCs with different linker chemistries with the related outcome
in cell and animal studies.
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