Results 91 to 100 of about 827,025 (271)
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
PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics
Oncogene, 2020 Using PROteolysis TArgeting Chimeras (PROTACs) to degrade proteins that are important for tumorigenesis has emerged as a potential therapeutic strategy for cancer. PROTACs are heterobifunctional molecules consisting of one ligand for binding to a protein of interest (POI) and another to an E3 ubiquitin (E3) ligase, connected via a linker.
Sajid Khan +7 more
openaire +3 more sources
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
CD36-mediated endocytosis of proteolysis-targeting chimeras
CellPassive diffusion does not explain why many drugs are too large and/or too polar for rule-breaking membrane penetration, such as proteolysis-targeting chimeras (PROTACs, generally of a molecular weight > 800 Da). Here, using biotinylated chemical-probe-based target fishing and genetic knockdown/knockin approaches, we discovered that the membrane ...
Zhengyu Wang +17 more
openaire +2 more sources
Advanced Science, EarlyView.A new class of lysosome‐directed molecular glue degraders selectively enhance CAPRIN1–APP interactions, driving APP degradation and reducing amyloid‐β production in human neurons and Alzheimer's disease mouse models. This CAPRIN1‐dependent targeted protein degradation strategy reveals a previously unrecognized therapeutic approach for disrupting the ...
Sunghan Jung +15 more
wiley +1 more source
Advanced Science, EarlyView.Targeted chimeric degraders engage extracellular or membrane proteins and endocytosable cell‐surface receptors, forming ternary complexes that induce receptor‐mediated internalization. Following endocytosis, post‐endocytic sorting—not internalization alone—determines target fate.
Ke Liu +6 more
wiley +1 more source
Acta Pharmaceutica Sinica BIn light of the burgeoning successes of cancer immunotherapy, glioblastoma (GBM) remains refractory due to an immunosuppressive microenvironment originating from its molecular heterogeneity.
Yeongji Jang +13 more
doaj +1 more source