Targeted protein degradation: advances in drug discovery and clinical practice

G Zhong, X Chang, W Xie, X Zhou - Signal Transduction and Targeted …, 2024 - nature.com
Targeted protein degradation (TPD) represents a revolutionary therapeutic strategy in
disease management, providing a stark contrast to traditional therapeutic approaches like …

Covalent Proximity Inducers

N London - Chemical Reviews, 2024 - ACS Publications
Molecules that are able to induce proximity between two proteins are finding ever increasing
applications in chemical biology and drug discovery. The ability to introduce an electrophile …

Development of novel antivrial agents that induce the degradation of the main protease of human-infecting coronaviruses

S Cheng, Y Feng, W Li, T Liu, X Lv, X Tong, G Xi… - European journal of …, 2024 - Elsevier
The family of human-infecting coronaviruses (HCoVs) poses a serious threat to global health
and includes several highly pathogenic strains that cause severe respiratory illnesses. It is …

Expedited SARS‐CoV‐2 Main Protease Inhibitor Discovery Through Modular 'Direct‐To‐Biology'Screening

H Wilders, G Biggs, SM Rowe… - Angewandte Chemie …, 2024 - Wiley Online Library
Reactive fragment (RF) screening has emerged as an efficient method for ligand discovery
across the proteome, irrespective of a target's perceived tractability. To date, however, the …

[HTML][HTML] PROTAC unleashed: Unveiling the synthetic approaches and potential therapeutic applications

N Pravin, K Jozwiak - European Journal of Medicinal Chemistry, 2024 - Elsevier
ABSTRACT Proteolysis-Targeting Chimeras (PROTACs) are a novel class of bifunctional
small molecules that alter protein levels by targeted degradation. This innovative approach …

Discovery of Potent Degraders of the Dengue Virus Envelope Protein

Z Li, HY Liu, Z He, A Chakravarty, RP Golden… - Advanced …, 2024 - Wiley Online Library
Targeted protein degradation has been widely adopted as a new approach to eliminate both
established and previously recalcitrant therapeutic targets. Here, it is reported that the …

Novel Acyl Thiourea-Based Hydrophobic Tagging Degraders Exert Potent Anti-Influenza Activity through Two Distinct Endonuclease Polymerase Acidic-Targeted …

X Ma, X Wang, F Chen, W Zou, J Ren… - Journal of Medicinal …, 2024 - ACS Publications
The spread of the influenza virus has caused devastating pandemics and huge economic
losses worldwide. Antiviral drugs with diverse action modes are urgently required to …

Recent Advances on Targeting Proteases for Antiviral Development

PHO Borges, SB Ferreira, FP Silva Jr - Viruses, 2024 - mdpi.com
Viral proteases are an important target for drug development, since they can modulate vital
pathways in viral replication, maturation, assembly and cell entry. With the (re) appearance …

Human E3 ubiquitin ligases: accelerators and brakes for SARS-CoV-2 infection

J Pellman, A Goldstein, M Słabicki - Biochemical Society …, 2024 - portlandpress.com
E3 ubiquitin ligases regulate the composition of the proteome. These enzymes mono-or poly-
ubiquitinate their substrates, directly altering protein function or targeting proteins for …

Lessons learnt from broad-spectrum coronavirus antiviral drug discovery

AA Bolinger, J Li, X Xie, H Li, J Zhou - Expert Opinion on Drug …, 2024 - Taylor & Francis
ABSTRACT Introduction Highly pathogenic coronaviruses (CoVs), such as severe acute
respiratory syndrome CoV (SARS-CoV), Middle East respiratory syndrome CoV (MERS …