Results 61 to 70 of about 57,293 (304)

Allosteric Modulation of Pathological Ataxin‐3 Aggregation: A Path to Spinocerebellar Ataxia Type‐3 Therapies

Advanced Science, EarlyView.
This study uncovers a new allosteric site in the Josephin domain of ataxin‐3 targeted by the molecular tweezer CLR01, which modulates protein aggregation, improves synaptic function in neuronal cells, and delays motor dysfunction in animal models.
Alexandra Silva, Sara Duarte‐Silva, Pedro M. Martins, Beatriz Rodrigues, Débora Serrenho, Daniela Vilasboas‐Campos, Andreia Teixeira‐Castro, Julio Vieyto‐Nuñez, Joel Mieres‐Perez, Francisco Figueiredo, Martyna Podlasiak, Tatiana Van‐der‐Kellen, Joana Fraga, James Noble, Carter Lantz, Niki Sepanj, Daniela Monteiro‐Fernandes, Sara Guerreiro, Andreia Neves‐Carvalho, Joana Pereira‐Sousa, Frank‐Gerrit Klärner, Thomas Schrader, Joseph A. Loo, Annalisa Pastore, Elsa Sanchez‐Garcia, Gal Bitan, Ana Luísa Carvalho, Patrícia Maciel, Sandra Macedo‐Ribeiro   +28 more
wiley   +1 more source

Stabilized Ion Selectivity Corrects Activation Drift in Kalium Channelrhodopsins

Advanced Science, EarlyView.
As newly emerged optogenetic tools, potassium channelrhodopsins (KCRs) can drift from inhibition to activation during illumination as K⁺ selectivity declines. It is shown that both the absolute K⁺/Na⁺ permeability ratio and its stability over time govern this drift, identify KCR1‐C29D as a reliably inhibitory variant, and outline design principles for ...
Xiao Duan, Chong Zhang, Stanislav Ott, Zhiyi Zhang, Christiane Ruse, Sven Dannhäuser, Robert Jacobi, Nadine Ehmann, Divya Sachidanandan, Georg Nagel, Manfred Heckmann, Robert J. Kittel, Alexander Gottschalk, Adam Claridge‐Chang, Shiqiang Gao   +14 more
wiley   +1 more source

Identification of new allosteric sites and modulators of AChE through computational and experimental tools

Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Allosteric sites on proteins are targeted for designing more selective inhibitors of enzyme activity and to discover new functions. Acetylcholinesterase (AChE), which is most widely known for the hydrolysis of the neurotransmitter acetylcholine, has a ...
Carlos Roca, Carlos Requena, Víctor Sebastián-Pérez, Sony Malhotra, Chris Radoux, Concepción Pérez, Ana Martinez, Juan Antonio Páez, Tom L. Blundell, Nuria E. Campillo   +9 more
doaj   +1 more source

Cinnamic‐Hydroxamic‐Acid Derivatives Exhibit Antibiotic, Anti‐Biofilm, and Supercoiling Relaxation Properties by Targeting Bacterial Nucleoid‐Associated Protein HU

Advanced Science, EarlyView.
Cinnamic‐hydroxamic‐acid derivatives (CHADs) are identified as novel inhibitors of the bacterial nucleoid‐associated protein HU, exhibiting potent antibacterial, anti‐biofilm (both inhibition and eradication), and DNA relaxation (anti‐supercoiling) activities. Moreover, CHADs demonstrate strong synergistic effects with multiple antibiotics.
Huan Chen, Yingqi Xu, Zhaoping Xiong, Hongliang Wang, Xin Wang, Yue Kang, Zhonglin Wang, Xiaoyan Zeng, Yahui Liu, Yehuan Zheng, Wei Chen, Mengzhe Li, Zhenyue Hu, Chi Xu, Yue Wu, Yawen Wang, Zuyi Yuan, Shuai Yuan, Huadong Liu, Steve Matthews, Nan Qiao, Yan Li, Bing Liu   +22 more
wiley   +1 more source

allosteric enzymes

, 2008
Citation: 'allosteric enzymes' in the IUPAC Compendium of Chemical Terminology, 3rd ed.; International Union of Pure and Applied Chemistry; 2006. Online version 3.0.1, 2019. 10.1351/goldbook.A00240 • 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

Precise Regulation of Membrane Proteins: From Physical Technology to Biomolecular Strategy

Advanced Science, EarlyView.
This review summarizes the emerging strategies for the precise regulation of membrane proteins using physical stimuli and biomolecule‐based tools. These methods provide new insights into cell regulation and offer promising directions for future disease treatment.
Xiu Zhao, Qingqing Zhou, Mengli Li, Wen Zou, Zhenzhong Zhang, Jinjin Shi, Junjie Liu   +6 more
wiley   +1 more source

Understanding allosteric and cooperative interactions in enzymes [PDF]

The FEBS Journal, 2013
The paper that introduced biochemists to the idea of allosteric feedback inhibition [Monod J, Changeux J‐P & Jacob F (1963) J Mol Biol 6, 306–329] is now 50 years old, and the two papers on models for enzyme cooperativity that followed it [Monod J, Wyman J & Changeux J‐P (1965) J Mol Biol 12, 88–118; Koshland DE, Némethy G & Filmer D (1966)
openaire   +3 more sources

Precision Editing of NLRS Improves Effector Recognition for Enhanced Disease Resistance

Advanced Science, EarlyView.
Precision engineering of plant NLR immune receptors enables rational design of enhanced pathogen resistance through mismatched pairing, domain swapping, and targeted mutagenesis. These approaches achieve multi‐fold expansion in recognition breadth while minimizing autoimmunity risks and fitness penalties.
Vinit Kumar, Vishwa I. P. W. A. Kumara, Pradeepa C. G. Bandaranayake, Dong Yawen, Yang‐Yang Gao, Junfeng Liu, Ge‐Fei Hao, Xiu‐Fang Xin   +7 more
wiley   +1 more source

A fast, miniaturised in-vitro assay developed for quantification of lipase enzyme activity

Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
The discovery of allosteric modulators is a multi-disciplinary approach, which is time- and cost-intensive. High-throughput screening combined with novel computational tools can reduce these factors. Thus, we developed an enzyme activity assay, which can
Ariane Menden, Davane Hall, Daniel Paris, Venkatarian Mathura, Fiona Crawford, Michael Mullan, Stefan Crynen, Ghania Ait-Ghezala   +7 more
doaj   +1 more source

Dipiperazine‐Phenyl Derivatives Based on Convergent Molecular Platforms Can Reverse Multidrug Resistance in Gram‐Negative Bacteria by Inhibiting Efflux and Permeabilizing Cell Membranes

Advanced Science, EarlyView.
By integrating a convergent molecular platform strategy, this study designed a novel dual‐target C5 to combat multidrug‐resistant Gram‐negative bacteria. C5 synergistically enhances antibiotic efficacy by inhibiting efflux pumps and increasing bacterial membrane permeability.
Jiale Dong, Ting Guo, Yi Huang, Yangchun Ma, Weijin Chen, Jie Xue, Jun Jiang, Enhui Dong, Yue Kong, Hang Ding, Wenlong Zhang, Shutao Ma   +11 more
wiley   +1 more source