Results 141 to 150 of about 149,452 (339)

CD147/Basigin: From Integrative Molecular Hub to Translational Therapeutic Target

Advanced Science, EarlyView.
This review conceptualizes CD147 as a fundamental “Energy‐Structure Coupler,” physically bridging metabolic flux (via MCTs) with morphogenetic plasticity (via integrins/MMPs) to drive cancer, infection, and autoimmunity. Addressing the “specificity paradox” that limits current translation, the authors chart a strategic roadmap—spanning logic‐gated ...
Xiang‐Min Yang, Huijie Bian, Zhi‐Nan Chen   +2 more
wiley   +1 more source

Discovery of a First‐in‐Class Covalent Allosteric SHP1 Inhibitor with Immunotherapeutic Activity

Angewandte Chemie, EarlyView.
A covalent allosteric inhibitor M029 was discovered for SHP1, a novel target for immunotherapy. M029 binds to a cryptic Cys remote from the active site, exhibits robust target engagement, and blocks tumor progression by stimulating antitumor immune response.
Zihan Qu, Frederick Nguele Meke, Zheng Zhang, Aaron D. Krabill, Christine S. Muli, Brenson A. Jassim, Jiajun Dong, Quyen D. Nguyen, Yunpeng Bai, Jinyue Li, Yiming Miao, Bardia Asadi, Levi M. Johnson, Jinmin Miao, Darci J. Trader, W. Andy Tao, Zhong‐Yin Zhang   +16 more
wiley   +2 more sources

A potential allosteric inhibitor of SARS-CoV-2 main protease (Mpro) identified through metastable state analysis

Frontiers in Molecular Biosciences
Anti-COVID19 drugs, such as nirmatrelvir, have been developed targeting the SARS-CoV-2 main protease, Mpro, based on the critical requirement of its proteolytic processing of the viral polyproteins into functional proteins essential for viral replication.
Asma Fatima, Anupriya M. Geethakumari, Wesam S. Ahmed, Kabir H. Biswas   +3 more
doaj   +1 more source

Analysis of Allosteric Effector Binding Sites of Potato ADP-glucose Pyrophosphorylase through Reverse Genetics [PDF]

, 2001
İbrahim Halil Kavaklı, Jong-Sug Park, Casey J. Slattery, Peter R. Salamone, Jennifer Frohlick, Thomas W. Okita   +5 more
openalex   +1 more source

Ligand‐Induced Electronic Response Enables Predictive QM/MM Simulations

Advanced Science, EarlyView.
Quantum mechanics/molecular mechanics (QM/MM) simulations are powerful tools for modeling complex molecular systems; however, their predictability has been constrained by the ambiguous definition of the QM region. An electronically informed protocol is introduced that defines QM regions by quantifying guest‐induced orbital shifts and charge ...
Nichika Ozawa, Nahoko Kuroki, Hirotoshi Mori   +2 more
wiley   +1 more source

allosteric site

Citation: 'allosteric site' in the IUPAC Compendium of Chemical Terminology, 5th ed.; International Union of Pure and Applied Chemistry; 2025. Online version 5.0.0, 2025. 10.1351/goldbook.14107 • License: The IUPAC Gold Book is licensed under Creative Commons Attribution-ShareAlike CC BY-SA 4.0 International for individual terms.
openaire   +1 more source

NADH‐Reductive Stress Induced by Dihydrolipoamide Dehydrogenase Activation Contributes to Cuproptosis

Advanced Science, EarlyView.
This study demonstrates a cuproptosis mechanism involving nicotinamide adenine dinucleotide (NADH)‐reductive stress in neural cells. Copper activates dihydrolipoamide dehydrogenase under mitochondrial pH, accumulating NADH. Copper also induces mitochondrial permeability transition pore opening, facilitating NADH translocation to the cytosol and ...
Si‐Yi Zhang, Xing‐Hua Ren, Cheng‐Hong Zhang, Zhan‐You Wang   +3 more
wiley   +1 more source

Allosteric Agonism of α7 Nicotinic Acetylcholine Receptors: Receptor Modulation Outside the Orthosteric Site [PDF]

, 2019
Alican Gulsevin, Roger L. Papke, Clare Stokes, Sumanta Garai, Ganesh A. Thakur, Marta Quadri, Nicole A. Horenstein   +6 more
openalex   +1 more source

Targeted Degradation of eEF2K by a Structure‐Guided PROTAC Strategy for the Treatment of Triple‐Negative Breast Cancer

Advanced Science, EarlyView.
This study developed an eEF2K‐targeting PROTAC, A6, that efficiently degrades eEF2K in TNBC cells, inhibiting tumor growth in vitro and in vivo. To enhance tumor‐specific delivery, we engineered A6@ZIF‐8, a pH‐sensitive nanocarrier, which improved drug accumulation at tumor sites, offering a promising therapeutic strategy for TNBC through targeted ...
Shijun Cao, Changxin Zhong, Shilong Jiang, Yungui Li, Yang Xi, Mingxuan Xiao, Ting Jiang, Xiaoya Wan, Zonglin Chen, Xiaohui Yu, Yan Cheng   +10 more
wiley   +1 more source

TRIM40 Drives Pathological Cardiac Hypertrophy and Heart Failure via Ubiquitination of PKN2

Advanced Science, EarlyView.
This study identifies the E3 ligase TRIM40 as a key driver of pathological cardiac hypertrophy. TRIM40 binds PKN2 via its B‐box domain and, through its C29‐dependent catalytic activity, mediates K63‐linked ubiquitination of PKN2. This modification enhances PKN2 phosphorylation at Ser815, thereby driving hypertrophy.
Risheng Zhao, Xiaoli Cui, Huizhu Du, Zhuoqun Wang, Chang Liu, Linxin Zhang, Jianing Qi, Di Yang, Hui Yu, Shuang Yan, Wei Liu, Haiming Sun, Mengyang Wang   +12 more
wiley   +1 more source