Results 51 to 60 of about 19,325 (262)

DNA‐Templated 2D Heterostructures as Phototriggered Dynamic Nanohybrids: From Releasing Molecular Loads to Controlling Enzyme Biocatalytic Function

Advanced Functional Materials, EarlyView.
DNA strands are employed both as dynamic linkers and nanoscale templates for the integration of Ag2S nanoparticles on MoS2, which in turn imparted photothermal responsiveness; this feature permits the selective cargo (fluorophore, quantum dots or an enzyme) release from the MoS2 surface in response to local heat induced by light irradiation.
Kai Chen, Haosen Miao, Weiying Hong, Matteo Palma   +3 more
wiley   +1 more source

Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor [PDF]

Proceedings of the National Academy of Sciences, 2013
μ-Opioid receptors are among the most studied G protein-coupled receptors because of the therapeutic value of agonists, such as morphine, that are used to treat chronic pain. However, these drugs have significant side effects, such as respiratory suppression, constipation, allodynia, tolerance, and dependence, as well as abuse potential.
Neil T, Burford, Mary J, Clark, Tom S, Wehrman, Samuel W, Gerritz, Martyn, Banks, Jonathan, O'Connell, John R, Traynor, Andrew, Alt   +7 more
openaire   +2 more sources

The Disordered Region of ASXL1 Acts as an Auto‐Regulator Through Condensation

Advanced Science, EarlyView.
ASXL1's long IDR encodes an electrostatic “basic platform + acidic brake” that autoregulates condensation. Truncation at a clinical hotspot lifts this brake, forming condensates that retarget BRD2, remodel local chromatin accessibility, and impair neutrophil maturation.
Xiao Fang, Qiwei Li, Wenqing Zhang
wiley   +1 more source

Q94 is not a selective modulator of proteinase-activated receptor 1 (PAR1) in platelets

Platelets, 2022
Thrombin is a potent platelet activator, acting through proteinase-activated receptors −1 and −4 (PAR1 and PAR4). Of these, PAR-1 is activated more rapidly and by lower thrombin concentrations.
Luc R. A. Francis, Sarah L. Millington-Burgess, Taufiq Rahman, Matthew T. Harper   +3 more
doaj   +1 more source

Allosteric Modulation of Metabotropic Glutamate Receptors [PDF]

, 2011
The development of receptor subtype-selective ligands by targeting allosteric sites of G protein-coupled receptors (GPCRs) has proven highly successful in recent years. One GPCR family that has greatly benefited from this approach is the metabotropic glutamate receptors (mGlus).
Douglas J, Sheffler, Karen J, Gregory, Jerri M, Rook, P Jeffrey, Conn   +3 more
openaire   +2 more sources

Fibrates Inhibit PLTP‐induced M2 Macrophage Infiltration and Increase the Sensitivity of Hepatocellular Carcinoma to ICIs

Advanced Science, EarlyView.
Phospholipid transfer protein(PLTP) plays a critical role in forming a complex with kinase A (AURKA) and P65. This interaction facilitates phosphorylation of P65 at Ser536, leading to the activation of the NF‐κB signaling pathway. Ultimately, this leads to the upregulation of downstream cytokines, including IL‐6, IL‐8, and CSF‐1, which promotes M2 ...
Xinyue Liang, Yaning Li, Jianxun Cai, Lisi Luo, Pengfei Yang, Yutong Chen, Jiancong Zhou, Yan Zeng, Jiaping Yu, Weiyu Zhang, Wenzheng Pang, Yufang Li, Chunhua Wen, Jian Li, Linjuan Zeng   +14 more
wiley   +1 more source

Ufmylation‐Deficient DDRGK1 Ameliorates Obesity by Inhibiting FASN‐Mediated Adipocyte Lipogenesis

Advanced Science, EarlyView.
DDRGK1 regulates de novo lipogenesis via stabilization of fatty acid synthase (FASN). DDRGK1‐mediated UFMylation of FASN prevents its ubiquitin–proteasomal degradation. Reduced DDRGK1 expression or mutation at the key UFMylation site enhances FASN degradation and suppresses fatty acid synthesis (FAS), resulting in smaller adipocytes and improved ...
Yin Li, Tangjun Zhou, Xiao Yang, Kewei Rong, Xiankun Cao, Lei Shi, Xin Wang, Hongjin Wan, Lei Cui, Kexin Liu, Tong Xing, Hang Zhang, Chen Zhao, Tingxian Guo, Peixiang Ma, Jie Zhao, An Qin   +16 more
wiley   +1 more source

The positive allosteric modulator of NMDA receptors, GNE‐9278, blocks the ethanol‐induced decrease of excitability in developing retrosplenial cortex neurons from mice

Neuropsychopharmacology Reports, 2023
Binge‐like exposure to ethanol during the brain growth spurt triggers apoptotic neurodegeneration in multiple brain regions, including the retrosplenial cortex, a brain region that is part of the hippocampal‐diencephalic‐cingulate memory network. This is
Clark W. Bird, Carlos F. Valenzuela
doaj   +1 more source

Metabolic Regulation of Dimethylsulfoniopropionate Cleavage and Dimethyl Sulfide Production in Halomonas sp. D47

Advanced Science, EarlyView.
Dimethylsulfoniopropionate (DMSP) is a major marine organosulfur compound central to climate‐relevant dimethyl sulfide (DMS) production. In Halomonas sp. D47, DMSP catabolism is revealed to be coordinated by two transcriptional regulators, AcuR and AcuZ, which control gene expression by sensing DMSP and its metabolites.
Li‐Yuan Zheng, Wen‐Xin Jiang, Xiao‐Meng Sun, Li Liu, Zhao‐Jie Teng, Hou‐Qi Wang, Wen‐Jing Zhu, Chang Ge, Qi‐Long Qin, Ning‐Hua Liu, Hai‐Yan Cao, Hui‐Hui Fu, Chun‐Yang Li, Jonathan D. Todd, Xiu‐Lan Chen, Yu‐Zhong Zhang, Peng Wang   +16 more
wiley   +1 more source

Mechanism of Allosteric Modulation of the Cys-loop Receptors

Pharmaceuticals, 2010
The cys-loop receptor family is a major family of neurotransmitter-operated ion channels. They play important roles in fast synaptic transmission, controlling neuronal excitability, and brain function.
Paul Whiteaker, Yao Huang, Yongchang Chang   +2 more
doaj   +1 more source