Work

Chemo-selective modification of cysteine residue: synthesis and application in the discovery of potential drug candidates

Year: 2024

Type: article

Abstract: Chemo-select modification of peptides, targeting a handful of the most reactive proteinogenic amino acids (AAs), is gradually utilized to address the medical needs of peptide drugs and biopharmaceuticals. Cysteine (Cys), one of the less abundant AAs in many biological proteins, plays a vital role in the catalysis, signal transduction, and redox regulation of gene expression. In natural AAs (α-AAs) residues, Cys exhibits high nucleophilicity and low redox-active potential, making it a primary target for site-selective conjugation. This review summarizes several representative Cys-peptide/protein conjugation strategies developed in recent years, including polar reactions, radical coupling reactions, and stapling techniques.

Source: Exploration of Drug Science

DOI: 10.37349/eds.2024.00060

Authors: Yanyan Liao, Xuefeng Jiang

Institutions: East China Normal University, Henan Normal University

Language: English

Topic: Chemical Synthesis and Analysis

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

Open Access status: diamond

Funders: National Natural Science Foundation of China, Science and Technology Commission of Shanghai Municipality, Fundamental Research Funds for the Central Universities

Awards: G1351254609, G2490294893