Results 101 to 110 of about 68,403 (252)

Mechanozyme: An Artificial Enzyme With a Mechanophore Framework

Advanced Science, EarlyView.
Mechanical destabilization of a G‐quadruplex mechanophore in a DNAzyme markedly boosts its catalytic activity, demonstrating “mechanozymes” as artificial enzymes whose functions are modulated by mechanical stress exerted by ultrasonication. This mechanozyme principle is broadly applicable to control biomolecular activities.
Jiahao Ji, Pravin Pokhrel, Sajan Shakya, Bishal Pokhrel, Grinsun Sharma, Pratiksha Chaudhary, Hao Shen, Hanbin Mao   +7 more
wiley   +1 more source

Discovery of a Potent Fluorescence Polarization Probe for Identifying USP1 Allosteric Inhibitors

Advanced Science, EarlyView.
This study presents the first ubiquitin‐specific protease 1 (USP1) allosteric fluoroprobe and fluorescence polarization assay, enabling the differentiation of allosteric and catalytic site inhibitors. Further, a novel class of tetrahydroisoquinoline‐based USP1 inhibitors is designed, with compound 14a (USP1 IC50 = 29.9 nM) showing strong selectivity ...
Jiawei Cheng, Peipei Wang, Pengfei Wang, Jiamin Wang, Baiyang Li, Daqing Fang, Jian He, Xiaobei Hu, Weijuan Kan, Yubo Zhou, Chunpu Li, Jia Li, Hong Liu   +12 more
wiley   +1 more source

Boosting Sensory Nerve‐to‐Bone Interactions Enhances Hedgehog Mediated Calvarial Bone Repair

Advanced Science, EarlyView.
Boosting sensory nerve activity via TrkA agonism strongly accelerates calvarial bone repair in adult mice. Furthermore, single‐cell RNA sequencing and neuron–bone interactome analyses identify these sensory neurons as a direct neural source of Hedgehog pathway ligands. Consequently, these ligands drive osteoblast differentiation of skeletal progenitors,
Zhao Li, Xin Xing, Beicheng Du, Myles Zhou, Austin Z. Chen, Mary Archer, Chunbao Rao, Manyu Zhu, Masnsen Cherief, Aaron W. James   +9 more
wiley   +1 more source

Revisiting Target‐Aware de novo Molecular Generation with TarPass: Between Rational Design and Texas Sharpshooter

Advanced Science, EarlyView.
TarPass provides a rigorous benchmark for target‐aware de novo molecular generation by jointly evaluating protein‐ligand interactions, molecular plausibility, and drug‐likeness on 18 well‐studied targets. Results show that current models often fail to consistently surpass random baseline in target‐specific enrichment, while post hoc multi‐tier virtual ...
Rui Qin, Zijie Chen, Yurong Li, Meijing Fang, Longji Shen, Yilong Su, Odin Zhang, Qinghan Wang, Qun Su, Jike Wang, Tingjun Hou, Yu Kang   +11 more
wiley   +1 more source

Allosteric DNAzyme‐Enabled Sensitive and Multiplex Detection of Biomarkers for Rapid Diagnosis of Urinary Tract Infections

Advanced Science, EarlyView.
A catalytic allosteric DNAzyme assay (SMART) is developed by engineering DNAzyme into a unimolecular biosensor, enabling highly sensitive and multiplex detection of small molecules and nucleic acids. SMART enables extraction‐free, one‐pot, one‐step, isothermal, and cost‐effective detection of biological markers, achieving >95% accuracy for rapid ...
Yanzhe Shen, Chenzhi Shi, Xiaowei Ma, Pengfei Hou, Haomin Zhang, Juanxiu Qin, Li Pan, Guilin Li, Lifei Gao, Qian Ma, Donglei Yang, Min Li, Pengfei Wang   +12 more
wiley   +1 more source

AI-Driven Design of Miniproteins as Potential Allosteric Modulators

Pharmaceuticals
Allosteric modulation has emerged as a powerful strategy for achieving superior selectivity and safety in drug discovery and protein function regulation.
Xin Liu, Yunxiang Sun, Yulong Xia, Huaqiong Li, Zhiqiang Yan   +4 more
doaj   +1 more source

T‐Cell Exhaustion in the Tumor Microenvironment: Subcellular Dysfunction, Pan‐Cancer Characteristics, and Therapeutic Interventions

Advanced Science, EarlyView.
This study elucidates the mechanisms of subcellular multidimensional collapse in exhausted T cells. By specifically targeting the nucleus, mitochondria, and endoplasmic reticulum, strategic interventions can effectively remodel the compromised organelle network. This integrated approach drives comprehensive T cell resuscitation, ultimately establishing
Mingxing Wang, Wanhui Dong, Jian Chen, Zhangjie Zhou, Shujuan Fu, Tingting Wu, Haiyan Jiang, Zhiying Wang, Zhixian Zhong, Yi Zhong   +9 more
wiley   +1 more source

Understanding the Catalytic Determinant role of Diaphorase‐Like Subunit in Formate Dehydrogenases via Redox Couples

Advanced Science, EarlyView.
A unique mechanism of catalytic bias regulated by diaphorase‐like subunit in formate dehydrogenase from Rhodobacter aestuarii is revealed. The diaphorase‐like subunit functions act as a biological “voltage rheostat” that controls the slow release of NADH to regulate redox balance, biasing the enzyme's catalytic preference toward CO2 reduction over ...
Kuncheng Zhang, Weisong Liu, Hao Su, Huijuan Cui, Yuanming Wang, Zhiguang Zhu, Chun You, Lingling Zhang   +7 more
wiley   +1 more source

A Non‐Canonical Core Transcriptional Regulatory Circuit Orchestrates Chromatin Reprogramming to Drive Osimertinib Resistance in Non‐Small Cell Lung Cancer

Advanced Science, EarlyView.
A non‐canonical core transcriptional regulatory circuit, composed of ID3, SMAD3, and NR2F2, drives Osimertinib resistance in non‐small cell lung cancer through super‐enhancer‐mediated activation of EPAS1, which couples neuroendocrine differentiation with ferroptosis evasion.
Aochu Liu, Zhenguo Liu, Lizhen Jiang, Andong Huang, Xinqing Lin, Xinyue Li, Bingyuan Liu, Shiwen Hu, Qiang Pan, Junjun Huang, Liyuan Yin, Liling Jiang, Wei Yi, Wenjun Mao, Yueyuan Zheng, Xianping Shi   +15 more
wiley   +1 more source

Allosteric Regulation of Photophysics and Binding in Oxazine‐macrocycle Complexes at Single‐molecule Resolution

Angewandte Chemie, EarlyView.
This work explores the interactions between the oxazine dye ATTO655 and two macrocyclic hosts using optical (single‑molecule) spectroscopy. Although ATTO655 forms a classical inclusion complex with cucurbit[8]uril (CB8), its interaction with p‑sulfonatocalix[4]arene (sCX4) leads to the formation of dim exclusion complexes.
Siyu Lu, Thomas‐Otavio Peulen, Hongbin Wu, Florian Lindemann, Despoina Kapiki, Rasmus Linser, Andreas Hennig, Thorben Cordes   +7 more
wiley   +2 more sources