Accelerating antiviral drug discovery: lessons from COVID-19

A von Delft, MD Hall, AD Kwong, LA Purcell… - Nature Reviews Drug …, 2023 - nature.com
During the coronavirus disease 2019 (COVID-19) pandemic, a wave of rapid and
collaborative drug discovery efforts took place in academia and industry, culminating in …

Structure and function of SARS-CoV and SARS-CoV-2 main proteases and their inhibition: A comprehensive review

X Li, Y Song - European Journal of Medicinal Chemistry, 2023 - Elsevier
Severe acute respiratory syndrome-associated coronavirus (SARS-CoV) identified in 2003
infected∼ 8000 people in 26 countries with 800 deaths, which was soon contained and …

The rise of degrader drugs

M Teng, NS Gray - Cell Chemical Biology, 2023 - cell.com
The cancer genomics revolution has served up a plethora of promising and challenging
targets for the drug discovery community. The field of targeted protein degradation (TPD) …

Applications and prospects of cryo-EM in drug discovery

KF Zhu, C Yuan, YM Du, KL Sun, XK Zhang… - Military Medical …, 2023 - Springer
Drug discovery is a crucial part of human healthcare and has dramatically benefited human
lifespan and life quality in recent centuries, however, it is usually time-and effort-consuming …

Catalytic degraders effectively address kinase site mutations in EML4-ALK oncogenic fusions

Y Gao, B Jiang, H Kim, MJ Berberich… - Journal of Medicinal …, 2023 - ACS Publications
Heterobifunctional degraders, known as proteolysis targeting chimeras (PROTACs),
theoretically possess a catalytic mode-of-action, yet few studies have either confirmed or …

[HTML][HTML] Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders

YD Li, MW Ma, MM Hassan, M Hunkeler, M Teng… - BioRxiv, 2023 - ncbi.nlm.nih.gov
Small molecules that induce protein-protein interactions to exert proximity-driven
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …

[HTML][HTML] Antiviral PROTACs: Opportunity borne with challenge

J Liang, Y Wu, K Lan, C Dong, S Wu, S Li, HB Zhou - Cell Insight, 2023 - Elsevier
Proteolysis targeting chimera (PROTAC) degradation of pathogenic proteins by hijacking of
the ubiquitin-proteasome-system has become a promising strategy in drug design. The …

Ubiquitination and cell-autonomous immunity

J Mello-Vieira, T Bopp, I Dikic - Current opinion in immunology, 2023 - Elsevier
Highlights•Cell-autonomous immunity senses, signals, and eliminates intracellular
pathogens.•Ubiquitination is a post-translational modification that connects these pathways.• …

Targeted protein degradation in cancers: Orthodox PROTACs and beyond

J Li, X Chen, A Lu, C Liang - The Innovation, 2023 - cell.com
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology …

Structure-activity relationship study of RSL3-based GPX4 degraders and its potential noncovalent optimization

C Zheng, C Wang, D Sun, H Wang, B Li, G Liu… - European Journal of …, 2023 - Elsevier
Ferroptosis is an iron-dependent, non-apoptotic form of cell death involving in various
disease processes. Mechanistically, glutathione peroxidase 4 (GPX4) which belongs to the …