Triflic Acid-Mediated Chemoselective Indole C2-Heteroarylation of Peptide Tryptophan Residues by Triazine DOI
Jian Li, Qi-Long Hu,

Jia-Shu Liu

et al.

Organic Letters, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 9, 2024

Peptide modification provides opportunities to afford peptides with designed functions. Among the proteogenic amino acids, tryptophan represents an ideal and attractive target for peptide because of exclusive chemical reactivity its unique indole structure. Herein, we reported C2 position-selective transition-metal-free approach derivatives tryptophan-containing by triazine via triflic acid activation that incorporated functional group could act as orthogonal handle further bioconjugation inverse electron demand Diels–Alder reaction.

Language: Английский

A patent review of anti-coronavirus agents targeting the spike-ACE2 interaction (2019–present) DOI
Xing Huang, Heng Gao, Jiwei Zhang

et al.

Expert Opinion on Therapeutic Patents, Journal Year: 2025, Volume and Issue: unknown

Published: April 22, 2025

The Angiotensin-converting enzyme 2 (ACE2) receptor, crucial for coronavirus recognition of host cells, is a key target therapeutic intervention against SARS-CoV-2 and related coronaviruses. Therefore, thoroughly investigating the interaction mechanism between ACE2 Spike protein (S protein), as well developing targeted inhibitors based on this mechanism, vital effectively controlling spread preventing potential future pandemics caused by other This article comprehensively reviews mechanisms underlying ACE2-S that facilitates entry into cells. It also analyzes patent landscape regarding targeting interface since 2019. In five years outbreak SARS-CoV-2, numerous methods design strategies have been employed to develop innovative therapeutics Among these approaches, both receptor S gained significant interest due their in blocking various Despite facing challenges similar protein-protein inhibitors, progress has made through virtual screening, covalent binding, peptide modification strategies. However, obstacles persist clinical translation, necessitating multidisciplinary strategy integrates state-of-the-art methodologies optimize S-ACE2 interface-targeted drug discovery.

Language: Английский

Citations

0

A Critical Review of Sensors for Detecting Per- and Polyfluoroalkyl Substances: Focusing on Diverse Molecular Probes DOI

Jiancheng Zha,

Muyuan Ma,

Yue Shen

et al.

Environmental Research, Journal Year: 2025, Volume and Issue: unknown, P. 121669 - 121669

Published: April 1, 2025

Language: Английский

Citations

0

Triflic Acid-Mediated Chemoselective Indole C2-Heteroarylation of Peptide Tryptophan Residues by Triazine DOI
Jian Li, Qi-Long Hu,

Jia-Shu Liu

et al.

Organic Letters, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 9, 2024

Peptide modification provides opportunities to afford peptides with designed functions. Among the proteogenic amino acids, tryptophan represents an ideal and attractive target for peptide because of exclusive chemical reactivity its unique indole structure. Herein, we reported C2 position-selective transition-metal-free approach derivatives tryptophan-containing by triazine via triflic acid activation that incorporated functional group could act as orthogonal handle further bioconjugation inverse electron demand Diels–Alder reaction.

Language: Английский

Citations

1