Results 61 to 70 of about 37,458 (256)

Allosteric Modulators Hit the TSH Receptor [PDF]

Endocrinology, 2014
The receptor for TSH (TSHR) has captured our interest and imagination since it was first demonstrated to be a major human antigen in autoimmune thyroid disease. The original realization that the immunoglobulin fraction of sera from patients with Graves' disease incorporated unique human autoantibodies to the TSHR led to the unraveling of the great ...
Terry F, Davies, M Rejwan, Ali, Rauf, Latif   +2 more
openaire   +2 more sources

Oppositely Charged Single Enzyme Nanogels Form Versatile Coacervates for Efficient Enzyme Cascade Catalysis

Advanced Materials, EarlyView.
Oppositely charged single enzyme nanogels (SENs) phase‐separate into bi‐enzymatic coacervate microdroplets, acting as both scaffold and functional units. By tuning SEN ratios, these coacervates create specific microenvironments that enable selective small‐molecule enrichment and efficient intermediate diffusion.
Andoni Rodriguez‐Abetxuko, Nadia A. Erkamp, Neshat Moslehi, Yannick H. A. Leurs, Lars Paffen, Işil Yeşil Gür, Jana Stojanović, Hugo Brasselet, Laura van der Weel, Ulf Hanefeld, Ilja K. Voets, Jan C. M. van Hest   +11 more
wiley   +1 more source

Allosteric modulators of M1 muscarinic receptors enhance acetylcholine efficacy and decrease locomotor activity and turning behaviors in zebrafish

Scientific Reports
Allosteric modulation of muscarinic acetylcholine receptors (mAChR) has been identified as a potential strategy for regulating cholinergic signaling in the treatment of various neurological disorders.
Corey J. Widman, Sestina Ventresca, Jillian Dietrich, Gwendolynne Elmslie, Hazel Smith, Gina Kaup, Aaron Wesley, Madeline Doenecke, Frederick E. Williams, Isaac T. Schiefer, John Ellis, William S. Messer Jr.   +11 more
doaj   +1 more source

Targeting UXS1‐Dependent Glucuronate Detoxification Potentiates Metformin's Anti‐Tumor Efficacy in Lung Adenocarcinoma

Advanced Science, EarlyView.
This study reveals that metformin promotes glucuronic acid metabolism in lung adenocarcinoma by activating UGDH S476 phosphorylation and enhancing the conversion of UDPG to UDPGA based on metabolomics analysis. Through compound virtual screening, it is found that plantainoside targeting UGDH downstream UXS1 leads to UDPGA toxicity accumulation ...
Qihai Sui, Zhencong Chen, Guangyao Shan, Zhengyang Hu, Xing Jin, Jiaqi Liang, Yanjun Yi, Jiacheng Yin, Haochun Shi, Xifei Jiang, Junjie Xi, Zongwu Lin, Cheng Zhan, Fenghao Sun, Wei Jiang   +14 more
wiley   +1 more source

Modulation of hemoglobin dynamics by an allosteric effector [PDF]

Protein Science, 2017
AbstractHemoglobin (Hb) is an extensively studied paradigm of proteins that alter their function in response to allosteric effectors. Models of its action have been used as prototypes for structure‐function relationships in many proteins, and models for the molecular basis of its function have been deeply studied and extensively argued.
Lal, Jyotsana, Maccarini, Marco, Fouquet, Peter, Ho, Nancy, T, Ho, Chien, Makowski, Lee   +5 more
openaire   +4 more sources

Allosteric Modulation of αβδ GABAA Receptors

Pharmaceuticals, 2010
GABAA receptors mediate the majority of the fast inhibition in the mature brain and play an important role in the pathogenesis of many neurological and psychiatric disorders.
Hua-Jun Feng
doaj   +1 more source

Natural Products Inspired Scaffold Diversification Leads to Unnatural Molecular Warhead and Covalent Strategy to Modulating Protein Function through Electrophilic Bromine Transfer

Advanced Science, EarlyView.
We report a new thiolate‐reactive α,α‐gem‐dibromo lactam warhead that activates transcription factor Nrf2 and demonstrates anti‐inflammatory activities, which have implications in cancer, neurodegeneration, and cardiovascular diseases. RNA‐seq illuminated detailed transcriptional profiles, and chemical reactions with cysteine‐containing compounds ...
Beau R. Brummel, Sofia Kokkaliari, Qiwen Gao, Jinjing Chen, Larissa Costa de Almeida, Srinivasarao Tenneti, Derek A. Leas, Eli Levit, Lewis S. Alexander, Khalil A. Abboud, Pingrong Wei, Michael D. Cameron, James R. Rocca, Ranjala Ratnayake, Donna D. Zhang, Hendrik Luesch, Robert W. Huigens III   +16 more
wiley   +1 more source

Voltage-dependent dynamics of the BK channel cytosolic gating ring are coupled to the membrane-embedded voltage sensor

eLife, 2018
In humans, large conductance voltage- and calcium-dependent potassium (BK) channels are regulated allosterically by transmembrane voltage and intracellular Ca2+.
Pablo Miranda, Miguel Holmgren, Teresa Giraldez   +2 more
doaj   +1 more source

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

Functional Analysis of Ligand‐Gated Chloride Channels in a Cnidarian Sheds Light on the Evolution of Inhibitory Signaling

Advanced Science, EarlyView.
We uncover a large variety of putative inhibitory ligand‐gated ion channels (LGICs) in the phylum Cnidaria, the sister group to all bilaterian animals. Phylogenetic analysis suggests a complex evolutionary history of inhibitory LGICs with diverse neurotransmitter ligands.
Abhilasha Ojha, Linda Kloss, Juan D. Montenegro, Simone Albani, Audrey Ortega‐Ramírez, Mihaela Raycheva, Sylvia Joussen, Sabrina Kaul, Michèle Bachmann, Lisa Huf, Günther Schmalzing, Alison G. Cole, Ulrich Technau, Stefan Gründer   +13 more
wiley   +1 more source