An overview of PROTACs: a promising drug discovery paradigm

Z Liu, M Hu, Y Yang, C Du, H Zhou, C Liu, Y Chen… - Molecular …, 2022 - Springer
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …

[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 …

Screening of potential inhibitors targeting the main protease structure of SARS-CoV-2 via molecular docking, and approach with molecular dynamics, RMSD, RMSF, H …

AM da Fonseca, BJ Caluaco, JMC Madureira… - Molecular …, 2024 - Springer
Abstract Severe Acute Respiratory Syndrome caused by a coronavirus is a recent viral
infection. There is no scientific evidence or clinical trials to indicate that possible therapies …

Lenalidomide derivatives and proteolysis-targeting chimeras for controlling neosubstrate degradation

S Yamanaka, H Furihata, Y Yanagihara, A Taya… - Nature …, 2023 - nature.com
Lenalidomide, an immunomodulatory drug (IMiD), is commonly used as a first-line therapy in
many haematological cancers, such as multiple myeloma (MM) and 5q myelodysplastic …

Co-opting the E3 ligase KLHDC2 for targeted protein degradation by small molecules

CM Hickey, KM Digianantonio… - Nature Structural & …, 2024 - nature.com
Targeted protein degradation (TPD) by PROTAC (proteolysis-targeting chimera) and
molecular glue small molecules is an emerging therapeutic strategy. To expand the roster of …

Drug discovery targeting nuclear receptor binding SET domain protein 2 (NSD2)

Z Ma, AA Bolinger, H Chen, J Zhou - Journal of medicinal …, 2023 - ACS Publications
Nuclear receptor binding SET domain proteins (NSDs) catalyze the mono-or dimethylation
of histone 3 lysine 36 (H3K36me1 and H3K36me2), using S-adenosyl-l-methionine (SAM) …

Proteolysis-Targeting Chimera (PROTAC) Delivery into the Brain across the Blood-Brain Barrier

T Tashima - Antibodies, 2023 - mdpi.com
Drug development for neurodegenerative diseases such as Alzheimer's disease,
Parkinson's disease, and Huntington's disease has challenging difficulties due to the …

Journey of von hippel-lindau (VHL) E3 ligase in PROTACs design: From VHL ligands to VHL-based degraders

N Setia, HTA Almuqdadi, M Abid - European Journal of Medicinal Chemistry, 2023 - Elsevier
The scientific community has shown considerable interest in proteolysis-targeting chimeras
(PROTACs) in the last decade, indicating their remarkable potential as a means of achieving …

Recent Advances and Future Directions on Small Molecule VEGFR Inhibitors in Oncological Conditions

A Thakur, M Rana, A Mishra, C Kaur, CH Pan… - European Journal of …, 2024 - Elsevier
ABSTRACT “A journey of mixed emotions” is a quote that best describes the progress chart
of vascular endothelial growth factor receptor (VEGFR) inhibitors as cancer therapeutics in …

VHL-Modified PROteolysis TArgeting Chimeras (PROTACs) as a Strategy to Evade Metabolic Degradation in In Vitro Applications

B Castellani, M Eleuteri, S Di Bona… - Journal of Medicinal …, 2023 - ACS Publications
PROteolysis TArgeting Chimeras (PROTACs) are tripartite molecules consisting of a linker
connecting a ligand for a protein of interest to an E3 ligase recruiter, whose rationale relies …