ABSTRACT Cancer cells rewire their metabolism to sustain a high proliferation rate. Sensing external cues is essential to match the metabolic fluxes of the cells to the external stimuli. As part of the glucose metabolism, the hexosamine biosynthesis pathway (HBP) is considered a nutrient‐sensing pathway. The HBP produces UDP‐GlcNAc, a key precursor for
Pegah Rahimizadeh +4 more
wiley +1 more source
ABSTRACT Small extracellular vesicles (sEVs) are promising vehicles for targeted therapeutic delivery, but strategies for their surface functionalization remain limited. Here, we present a reliable and simple genetic approach that enables customized modification of sEV surfaces and supports enhanced sEV uptake by recipient cells. This strategy is based
Lukas Hyka +7 more
wiley +1 more source
Harnessing the SPOP E3 Ubiquitin Ligase via a Bridged Proteolysis Targeting Chimera (PROTAC) Strategy for Targeted Protein Degradation. [PDF]
Deng Z +9 more
europepmc +1 more source
Small Molecule Inhibition of Mononegavirales RNA Polymerases
ABSTRACT The order Mononegavirales includes several non‐segmented negative‐sense RNA viruses that are significant human pathogens, whose transcription and replication depend on multifunctional RNA‐dependent RNA polymerase (L protein). Recent discoveries in cryo‐electron microscopy (cryo‐EM) have elucidated the structures of these polymerases and their ...
Claire R. Cao +3 more
wiley +1 more source
Structure-guided design of a methyltransferase-like 3 (METTL3) proteolysis targeting chimera (PROTAC) incorporating an indole-nicotinamide chemotype. [PDF]
Weldert AC +6 more
europepmc +1 more source
Liver Fibrosis: Molecular Pathogenesis and Therapeutic Interventions
We systematically summarized the etiologies, diagnostic approaches, and pathogenic mechanisms of liver fibrosis. Also, the therapeutic interventions for liver fibrosis were systematically classified into two main categories: etiological treatment and mechanism‐based antifibrotic therapies.
Jiaorong Qu +8 more
wiley +1 more source
Discovery of the First Potent DYRK2 Proteolysis Targeting Chimera Degraders. [PDF]
Chen J +5 more
europepmc +1 more source
A protein knockdown strategy to study the function of β-catenin in tumorigenesis [PDF]
core +1 more source
Fusion Molecules Between the STAT5b Inhibitor Stafib‐2‐CR and a Cereblon Ligand
The design and synthesis of fusion molecules between the selective STAT5b inhibitor Stafib‐2‐CR and a ligand of the E3 ubiquitin ligase cereblon is reported. Activity analysis in fluorescence polarization assays and isothermal titration calorimetry indicated that the chosen attachment point for the linker is well‐suited to retain activity of the fusion
Theresa Münzel +4 more
wiley +1 more source
Chemoproteomics-Enabled <i>De Novo</i> Proteolysis Targeting Chimera Discovery Platform Identifies a Metallothionein Degrader to Probe Its Role in Cancer. [PDF]
Racioppo B +6 more
europepmc +1 more source

