Results 131 to 140 of about 139,314 (301)

Corynoxine Inhibits Tumor Growth via Targeting NQO1 and Modulating the PTPA–NQO1/PP2A Switch to Activate PP2A

open access: yesAdvanced Science, EarlyView.
Corynoxine exerts potent broad‐spectrum anticancer activity by directly targeting NQO1. This interaction dissociates the oncogenic NQO1‐PTPA complex, releasing PTPA to robustly activate the tumor suppressor PP2A. Consequently, downstream Raf/MEK/ERK and PI3K/AKT signaling pathways are suppressed, downregulating c‐Myc and driving tumor regression ...
Guoqing Hou   +6 more
wiley   +1 more source

Macrophage RSAD2 Couples mtDNA Synthesis With a Self‐Amplifying Inflammatory Circuit to Orchestrate Tissue Repair

open access: yesAdvanced Science, EarlyView.
Macrophage RSAD2 dually regulates CMPK2—the rate‐limiting enzyme for mitochondrial DNA synthesis—by suppressing its ubiquitination and promoting its phosphorylation via Csnk2a2 recruitment. This amplifies mtDNA production, which simultaneously activates a cGAS‐STING‐IRF3‐RSAD2 feedforward loop and the NLRP3 inflammasome, driving a self‐sustaining ...
Haomiao Yuan   +16 more
wiley   +1 more source

DyProL: Dynamic Ensemble Representation Learning for Protein–Nucleic Acid Binding Site Prediction

open access: yesAdvanced Science, EarlyView.
Protein function is represented as a dynamic conformational ensemble rather than a single static structure. A multi‐conformation geometric attention framework aligns, clusters, and learns representative states to capture residue‐ and ensemble‐level signals. Integrating structural dynamics improves interpretable protein‐NA binding prediction and reveals
Pengpai Li   +3 more
wiley   +1 more source

Structural basis for positive allosteric regulation of CB2 receptor

open access: yesNature Communications
The synthetic positive allosteric modulator (PAM) of cannabinoid receptor CB2, Ec21a, exhibits better subtype selectivity and receptor specificity over orthosteric ligands, which holds promise for treating neuropathic pain and seizure without causing ...
Xuehui Wang   +7 more
doaj   +1 more source

Reversible, Chemically Gated FRET via Ligand‐Activated Acceptors

open access: yesAdvanced Science, EarlyView.
Fluorogen binding turns the compact FAST tag into a tunable FRET acceptor, with ligand chemistry programming spectral overlap and excited‐state lifetimes. Fluorescence‐lifetime imaging reads out energy transfer through the shortened donor lifetime, while simply adding or washing out the dye switches FRET on and off, reversibly mapping the supramodular ...
Nivedita Singh   +7 more
wiley   +1 more source

Allosteric ensembles elucidate mechanisms of inhibition in the human soluble epoxide hydrolase

open access: yesCommunications Biology
Human soluble epoxide hydrolase (sEH) is an important modulator of cardiovascular, brain and renal health, and a promising therapeutical target for several pathologies.
Qiongju Qiu   +4 more
doaj   +1 more source

Sulfur–Oxygen Competitive Coordination Allosteric Hydrogel for Triboelectric Nanogenerator‐Based Intelligent Tactile Recognition

open access: yesAdvanced Science, EarlyView.
A dynamic Ag+─S coordinated hydrogel with a sulfur–oxygen competitive coordination allosteric switch enables reversible tuning between soft–adhesive and stiff–robust states. Integrated with a lightweight 1DCNN classifier, the smart glove system achieves 99.70% laboratory and 93.35% real‐wear material recognition accuracy, offering a paradigm for self ...
Shixia Lan   +4 more
wiley   +1 more source

Structural Basis of Lymphangiogenic Receptor VEGFR‐3 Activation Mediated by Distinctive Clustering of the Ligand–Receptor Complex

open access: yesAdvanced Science, EarlyView.
VEGF‐C and its receptor VEGFR‐3 are critical for lymphangiogenesis. Cryo‐EM structures of the VEGFR‐3/VEGF‐C ectodomain complex reveal a canonical 2:2 ligand–receptor hetero‐tetramer that further assembles into higher‐order clusters beyond simple receptor dimerization.
Ryeongeun Cho   +6 more
wiley   +1 more source

Direct activation of M1 muscarinic receptors by the positive allosteric modulator, BQCA

open access: yes, 2014
BQCA (Benzyl quinolone carboxylic acid) was recently identified as a positive allosteric modulator of the M1 muscarinic receptor. We studied the nature of this effect on muscarinic signaling at the single cell level in Chinese Hamster Ovary (CHO) cells ...
Brinker, Katherine
core   +1 more source

An Extracellular Pore‑Targeting Peptide Defines a Designable Allosteric Site in TRPV2

open access: yesAdvanced Science, EarlyView.
Structure‐guided peptide engineering yields Depiv2, a highly potent and subtype‐selective TRPV2 inhibitor that binds to the extracellular pore and remodels it into a closed, non‐conductive state. Depiv2 suppresses pathological cardiac hypertrophy, establishing the TRPV2 outer pore as a designable interface for selective peptide modulation.
Aiqin Zhu   +7 more
wiley   +1 more source

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