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

Perfluoroalkyl Editing of Fluoroalkynes: Chemo-, Regio-, and Stereoselective Synthesis of (E)-(2-Amino-fluoroalkenyl)pyrimidines DOI
M Kellis,

Ming-Yao Tang,

Tong Qian

et al.

Organic Letters, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 26, 2025

A chemo-, regio-, and stereoselective condensation reaction of perfluoroalkyl alkynes (PFAAs), (CH2O)n, (NH4)2CO3 through the cleavage five inert C(sp3)-F bonds at three distinct carbon sites, thereby establishing an unprecedented platform for synthesizing structurally unique (E)-(2-amino-fluoroalkenyl)pyrimidines, is first developed. Remarkably, this features mild conditions, good compatibility with various functional groups, excellent E-stereoselectivity, late-stage modification complex molecules, scalability, versatile synthetic transformations resulting heterocyclic compounds.

Language: Английский

Citations

1
General structure-activity relationship models for the inhibitors of Adenosine receptors: A machine learning approach DOI Creative Commons

Mona Janbozorgi,

Sara Kaveh, M. S. Neiband

et al.

Molecular Diversity, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 20, 2025

Language: Английский

Citations

0
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