Site-Selective, Chemical Modification of Protein at Aromatic Side Chain and Their Emergent Applications

Author(s): Arnab Chowdhury, Saurav Chatterjee, Akumlong Pongen, Dhanjit Sarania, Nitesh Mani Tripathi, Anupam Bandyopadhyay*

Journal Name: Protein & Peptide Letters

Volume 28 , Issue 7 , 2021

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Graphical Abstract:


Site-selective chemical modification of protein side chain has probed enormous opportunities in the fundamental understanding of cellular biology and therapeutic applications. Primarily, in the field of biopharmaceuticals, the formulation of bioconjugates has been found to have more potential than an individual constituent. In this regard, Lysine and Cysteine are the most widely used endogenous amino acid for these purposes. Recently, the aromatic side chain residues (Trp, Tyr, and His) that are low abundant in protein have gained more attention in therapeutic applications due to their advantages of chemical reactivity and specificity. This review discusses the site-selective bioconjugation methods for aromatic side chains (Trp, Tyr and His) and highlights the developed strategies in the last three years, along with their applications. Also, the review highlights the prevalent methods published earlier. We have examined that metal-catalyzed and photocatalytic reactions are gaining more attention for bioconjugation, though their practical operation is under development. The review has been summarized with the future perspective of protein and peptide conjugations contemplating therapeutic applications and challenges.

Keywords: Bioconjugation, site-selective modification, aromatic amino acids, peptide conjugation, protein therapeutics, antibody- drug conjugate.

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Article Details

Year: 2021
Published on: 29 January, 2021
Page: [788 - 808]
Pages: 21
DOI: 10.2174/0929866528666210129152535
Price: $65

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