Results 51 to 60 of about 7,774 (200)
Advanced Science, EarlyView.Targeted protein degradation is often limited by the scarcity of usable E3 ligases. Herein, we report the first small‐molecule GPX4 degraders that incorporate either electrophilic warheads or a minimal azide group as an E3 recruitment ligand. The azide‐based degrader DK‐5070 effectively drives potent GPX4 degradation; mechanistic studies reveal that ...
Zehong Lin +14 more
wiley +1 more source
Advanced Science, 2021 DNA‐binding proteins, including transcription factors (TFs), play essential roles in various cellular processes and pathogenesis of diseases, deeming to be potential therapeutic targets.
Jingwei Shao +9 more
doaj +1 more source
A Drug‐Gated, Modular STAb‐T Immunotherapy With External Control
Advanced Science, EarlyView.Engineered STAb‐TON cells act as programmable living factories that continuously secrete inactive antibody modules, which assemble extracellularly into a functional T cell engager only upon small‐molecule administration. This externally controlled platform enables reversible, on‐demand regulation of antitumor immunity, establishing a new paradigm for ...
Susana Luengo‐Arias +23 more
wiley +1 more source
PTGES3 proteolysis using the liposomal peptide-PROTAC approach
Biology DirectBackground Hepatocellular carcinoma (HCC) is the leading cause of cancer-related deaths worldwide, and the lack of effective biomarkers for early detection leads to poor therapeutic outcomes.
Shiwei Liu +6 more
doaj +1 more source
Supramolecular Degraders: An Emerging Paradigm in Targeted Protein Degradation
Advanced Science, EarlyView.Dynamic supramolecular assembly reshapes targeted protein degradation by coordinating modular degrader construction, delivery, functional integration, and intracellular assembly or activation across proteasomal, endosomal–lysosomal, and autophagy–lysosomal pathways.
Kongjun Liu +8 more
wiley +1 more source
Advanced Science, EarlyView.A mechanically activated SynNotch reporter platform enables detection of force transmission through receptors as they mediate immune cell interactions. Targeting CD40 on B cells and TCR on T cells records force‐induced reporter activation across 2D coculture, 3D organoid, and implanted in mice, which also reveal force‐amplification of immune receptor ...
Menglan Li +9 more
wiley +1 more source
Advanced Science, EarlyView.AI‑guided single‑cell transcriptomics identifies OGT as a key regulator enriched in rheumatoid arthritis fibroblast‑like synoviocytes (RA‐FLSs). Inflammatory stimuli activate the OGT–SAP130 axis, which modulates the H3K27ac/H3K27me3 balance and epigenetically silences BTG2, promoting aggressive transformation of RA‑FLSs.
Duoli Xie +14 more
wiley +1 more source
Advanced Science, EarlyView.To model a nutrient‐restricted tumor microenvironment, breast cancer cells were adapted to low glucose and glutamine levels. In the adapted cells, BRD4‐driven enhancer activation increases pro‐invasive EDN1 expression, facilitated by ATF3/c‐JUN and reinforced by enhancer RNA.
Poshan Yugal Bhattarai +4 more
wiley +1 more source
PROTACs in Oncology: Emerging Frontiers for Next-Generation Cancer Therapeutics
OncoPROTACs represent a cutting-edge approach to the discovery of innovative cancer therapies. By exploiting the cell’s ubiquitin–proteasome system, PROTACs induce the selective degradation of target proteins, providing a distinct advantage over conventional
Salahuddin +6 more
doaj +1 more source
Advanced Science, EarlyView.Here, we report a novel NIR fluorescent PROTAC platform that enables real‐time imaging and targeted degradation of Alzheimer's p‐Tau. Our lead compound effectively clears p‐Tau, reduces APP/Aβ, and alleviates cognitive deficits in AD mice. This work demonstrates a theranostic strategy for visualizing degradation and developing next‐generation AD ...
Ziwei Ren +11 more
wiley +1 more source