Results 121 to 130 of about 702,558 (291)

Allosteric modulators of metabotropic glutamate receptors: from virtual screening to experimental validation [PDF]

, 2007
The goal of this thesis was to gain further insight into the binding behavior of ligands in the heptahelical domain (HD) of group I metabotropic glutamate receptors (mGluRs).
Noeske, Tobias
core  

Targeting the PHB2–ACSL3 Lipid‐Remodeling Axis Overcomes Cisplatin Resistance by Restoring Ferroptosis in Gastric Cancer

Advanced Science, EarlyView.
ABSTRACT Platinum‐based chemotherapy resistance remains a major obstacle in gastric cancer (GC) treatment. Through integrated transcriptomic profiling of cisplatin‐resistant xenografts and pharmacogenomic interrogation of the NCI‐60 dataset, we identified Prohibitin‐2 (PHB2) as a previously unrecognized determinant of chemoresistance.
Liang Xu, Wanying Xiang, Xinyue Wang, Yue Pan, Jing Gao, Jiezhen Yang, Yufei Wang, Zhipu Zhu, Man Tong, Lei Jin, Yan Ye   +10 more
wiley   +1 more source

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

Advanced 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, Li Lin, Mengjie Xia, Ruohan Liang, Yueyue Zhang, Linna Du, Xuan Cao   +6 more
wiley   +1 more source

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

Advanced 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, Shukui Du, Chunfei Li, Xinjie Li, Shuyang Mu, Anran Qu, Hengxu Yan, Chongchong Xu, Jinnong Yang, Jingkai Sun, Yijun Wang, Jiayang Xiao, Fuyuan Zhang, Linlin Wang, Tiegang Li, Rui Zhao, Dawei Guan   +16 more
wiley   +1 more source

Activation and Allosteric Modulation of Human μ Opioid Receptor in Molecular Dynamics

, 2015
Allosteric protein modulation has gained increasing attention in drug design. Its application as a mechanism of action could bring forth safer and more effective medicines.
Dariusz Matosiuk (1478035), Damian Bartuzi (1478032), Agnieszka A. Kaczor (772893)   +2 more
core   +1 more source

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

Advanced 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, Yiman Liu, Liya Liang, Rongming Liu   +3 more
wiley   +1 more source

Reversible, Chemically Gated FRET via Ligand‐Activated Acceptors

Advanced 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, Smruti Ranjan Nayak, Sanjay Kumar Mohanty, Aishwarya Hanumantharaju, Amala Shaju, Mini Jose, Aravind Penmatsa, Deepak Nair   +7 more
wiley   +1 more source

Free fatty acid receptor 2 allosterism is defined by cellular context

Cell Communication and Signaling
Background Allosteric modulators offer a way to fine-tune GPCR signaling in the presence of endogenous ligands. The short-chain fatty acid receptor FFA2R (GPR43) recognizes propionate and allosteric ligands such as Cmp58 and AZ1729.
Simon Lind, Ayaan Abdi Ali, Sarah Al Hamoud Al Asswad, Volker M. Lauschke, Huamei Forsman, Claes Dahlgren, Linda C. Johansson   +6 more
doaj   +1 more source

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

Advanced 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, Lin Zhang, Yunyun Dong, Yongyun Mao, Wanbiao Hu   +4 more
wiley   +1 more source

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

Advanced 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, Jinsook Ahn, Jimin Yang, Dong Sun Lee, Gahi Hong, Sangkyu Lee, Ho Min Kim   +6 more
wiley   +1 more source