Accelerating antiviral drug discovery: lessons from COVID-19
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 …
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
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 …
infected∼ 8000 people in 26 countries with 800 deaths, which was soon contained and …
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 …
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
Heterobifunctional degraders, known as proteolysis targeting chimeras (PROTACs),
theoretically possess a catalytic mode-of-action, yet few studies have either confirmed or …
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
Small molecules that induce protein-protein interactions to exert proximity-driven
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …
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 …
the ubiquitin-proteasome-system has become a promising strategy in drug design. The …
Ubiquitination and cell-autonomous immunity
Highlights•Cell-autonomous immunity senses, signals, and eliminates intracellular
pathogens.•Ubiquitination is a post-translational modification that connects these pathways.• …
pathogens.•Ubiquitination is a post-translational modification that connects these pathways.• …
Targeted protein degradation in cancers: Orthodox PROTACs and beyond
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology …
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 …
disease processes. Mechanistically, glutathione peroxidase 4 (GPX4) which belongs to the …