Results 91 to 100 of about 4,452,404 (339)

Allosteric mechanism for site-specific ubiquitination of FANCD2 [PDF]

Nature Chemical Biology, 2019
DNA-damage repair is implemented by proteins that are coordinated by specialized molecular signals. One such signal in the Fanconi anemia (FA) pathway for the repair of DNA interstrand crosslinks is the site-specific monoubiquitination of FANCD2 and FANCI.
Viduth K. Chaugule, Connor Arkinson, Martin L. Rennie, Outi Kämäräinen, Rachel Toth, Helen Walden   +5 more
openaire   +4 more sources

Lithium‐Charged Gold Nanoparticles: A New Powerful Tool for Lithium Delivery and Modulation of Glycogen Synthase Kinase 3 Activity

Advanced Materials, EarlyView.
This study introduces glutathione‐stabilized gold nanoparticles for targeted lithium delivery (LiG‐AuNPs), enabling the controlled modulation of Glycogen Synthase Kinase‐3 (GSK‐3β). These non‐toxic, 2‐nm particles release lithium intracellularly, effectively inhibiting GSK‐3β in the brain without significant plasma lithium alterations.
Antonio Buonerba, Giulia Puliatti, Domenica Donatella Li Puma, Bruno Bandiera, Beatrice Cannata, Maria Elena Marcocci, Nicolina Castagno, Irene Contento, Salvatore Impemba, Mariarosa Scognamiglio, Rocco Di Girolamo, Vincenzo Naddeo, Patrizia Canton, Carmine Capacchione, Laura Sposito, Martina Albini, Francesco Pastore, Silvia Baroni, Alfonso Grassi, Claudio Grassi, Roberto Piacentini   +20 more
wiley   +1 more source

Fluorescent ligands targeting the intracellular allosteric binding site of the chemokine receptor CCR2 [PDF]

, 2022
Lara Toy, Max E. Huber, Maximilian F. Schmidt, Dorothée Weikert, Matthias Schiedel   +4 more
openalex   +1 more source

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

Studying early structural changes in SOS1 mediated KRAS activation mechanism

Current Research in Structural Biology
KRAS activation is known to be modulated by a guanine nucleotide exchange factor (GEF), namely, Son of Sevenless1 (SOS1). SOS1 facilitates the exchange of GDP to GTP thereby leading to activation of KRAS.
Kirti Bhadhadhara, Vinod Jani, Shruti Koulgi, Uddhavesh Sonavane, Rajendra Joshi   +4 more
doaj   +1 more source

Identification of an allosteric binding site for RORγt inhibition [PDF]

Nature Communications, 2015
AbstractRORγt is critical for the differentiation and proliferation of Th17 cells associated with several chronic autoimmune diseases. We report the discovery of a novel allosteric binding site on the nuclear receptor RORγt. Co-crystallization of the ligand binding domain (LBD) of RORγt with a series of small-molecule antagonists demonstrates occupancy
Scheepstra, M., Leysen, S., Almen, G.C. van, Miller, J.R., Piesvaux, J., Kutilek, V., Eenennaam, H. van, Zhang, H., Barr, K., Nagpal, S., Soisson, S.M., Kornienko, M., Wiley, K., Elsen, N., Sharma, S., Correll, C.C., Trotter, B.W., Stelt, M. van der, Oubrie, A., Ottmann, C., Parthasarathy, G., Brunsveld, L.   +21 more
openaire   +3 more sources

TSHR‐Targeting Nucleic Acid Aptamer Treats Graves' Ophthalmopathy via Novel Allosteric Inhibition

Advanced Science, EarlyView.
This study presents YC3, a novel inhibitory TSHR‐targeting aptamer, as a promising therapeutic for Graves' ophthalmopathy (GO). YC3 suppresses pathological phenotypes in human orbital fibroblasts and improves outcomes in GO mice by binding to a previously unidentified allosteric site on TSHR, demonstrating the potential of aptamers in advancing ...
Yanchen Zhang, Ende Wu, Weibin Liu, Ling Zeng, Neng Ling, Hongmei Wang, Zhixing Li, Shuang Yao, Tonghe Pan, Xuanwen Li, Yate Huang, Xiaojing Li, Yunhai Tu, Wentao Yan, Jianzhang Wu, Mao Ye, Wencan Wu   +16 more
wiley   +1 more source

Activity modulation in anaerobic ribonucleotide reductases: nucleotide binding to the ATP-cone allosterically mediates substrate binding to the active site [PDF]

, 2023
Ornella Bimaï, Ipsita A. Banerjee, Inna Rozman Grinberg, Ping Huang, Lucas Hultgren, Simon Ekström, Daniel Lundin, Britt‐Marie Sjöberg, Derek T. Logan   +8 more
openalex   +1 more source

Oral Exposure to Food‐Grade Nanoparticles Poses a Risk of Alzheimer's Disease‐Like Symptoms by Triggering Autophagy Defects in Neurons

Advanced Science, EarlyView.
Three food‐grade nanomaterials induce dysregulated RyR‐Ca2+ signaling through epigenetic modifications. This dysregulation impairs the autophagic clearance process, ultimately leading to abnormal Aβ deposition and increase phosphorylated tau levels.
Jiaxin Shang, Jun Yan, He Lou, Xuanxi Jiang, Ziyue Wang, Yue Gao, Xiaohui Fan, Xiaoyan Lu   +7 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