The disulfide bond possesses unique chemical and biophysical properties which
distinguish it as one of the key structural elements of bioactive proteins and peptides, important
drugs and other materials. The chemo-selective synthesis of these structures and
the exploration of their function have been of longstanding interest to the chemistry community.
The past decades have witnessed significant progress in both areas. This review
will summarize the historically established and recently developed chemical methods in
disulfide bond formation. The discussion will also be extended to the use of the disulfide
linkers in small molecules, and peptide- and protein-drug conjugates. It is hoped that the
combined overview of the fundamental chemistries and applications to drug discovery
will inspire creative thinking and stimulate future novel uses of these versatile chemistries.
Keywords: Sulfur-sulfur bond, disulfide, chemical synthesis, targeted drug discovery, small molecule-drug conjugate, peptide-drug conjugate,
protein-drug conjugate and antibody-drug conjugate.
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