Results 101 to 110 of about 121,181 (303)

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

Pharmacodynamic Model of Parathyroid Hormone Modulation by a Negative Allosteric Modulator of the Calcium-Sensing Receptor [PDF]

The AAPS Journal, 2011
In this study, a pharmacodynamic model is developed, based on calcium-parathyroid hormone (PTH) homeostasis, which describes the concentration-effect relationship of a negative allosteric modulator of the calcium-sensing receptor (CaR) in rats. Plasma concentrations of drug and PTH were determined from plasma samples obtained via serial jugular vein ...
Anson K, Abraham, Tristan S, Maurer, Amit S, Kalgutkar, Xiang, Gao, Mei, Li, David R, Healy, Donna N, Petersen, David A, Griffith, Donald E, Mager   +8 more
openaire   +2 more sources

Computational analysis of negative and positive allosteric modulator binding and function in metabotropic glutamate receptor 5 (in)activation

, 2014
Metabotropic glutamate receptors (mGluRs) are high-profile G-protein coupled receptors drug targets because of their involvement in several neurological disease states, and mGluR5 in particular is a subtype whose controlled allosteric modulation, both ...
Dalton, James A. R., Gómez-Santacana, Xavier, Llebaria, Amadeu, Giraldo, Jesús   +3 more
core   +1 more source

The First Negative Allosteric Modulator for Dopamine D2 and D3 Receptors SB269652 May Lead to a New Generation of Antipsychotic Drugs [PDF]

, 2017
D2 and D3 dopamine receptors belong to the largest family of cell surface proteins in eukaryotes, the G protein-coupled receptors (GPCRs). Considering their crucial physiological functions and their relatively accessible cellular locations, GPCRs ...
Irene Fasciani, Fasciani, Irene, Mario Rossi, Francesco Marampon, Marco Scarselli, SCARSELLI, MARCO, MAGGIO, ROBERTO, ROSSI, MARIO, Marampon, Francesco, Roberto Maggio   +9 more
core   +1 more source

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

Computational Analysis of Negative and Positive Allosteric Modulator Binding and Function in Metabotropic Glutamate Receptor 5 (In)Activation

, 2016
Metabotropic glutamate receptors (mGluRs) are high-profile G-protein coupled receptors drug targets because of their involvement in several neurological disease states, and mGluR5 in particular is a subtype whose controlled allosteric modulation, both ...
Xavier Gómez-Santacana (2106892), Amadeu Llebaria (1626844), Jesús Giraldo (1558987), James A. R. Dalton (2106895)   +3 more
core   +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

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

Cannabidiol binding and negative allosteric modulation at the cannabinoid type 1 receptor in the presence of delta-9-tetrahydrocannabinol: An In Silico study.

PLoS ONE, 2019
Recent evidence has raised in discussion the possibility that cannabidiol can act as a negative allosteric modulator of the cannabinoid type 1 receptor. Here we have used computational methods to study the modulation exerted by cannabidiol on the effects
Hery Chung, Angélica Fierro, C David Pessoa-Mahana   +2 more
doaj   +1 more source

The E2.65A mutation disrupts dynamic binding poses of SB269652 at the dopamine D2 and D3 receptors. [PDF]

PLoS Computational Biology, 2018
The dopamine D2 and D3 receptors (D2R and D3R) are important targets for antipsychotics and for the treatment of drug abuse. SB269652, a bitopic ligand that simultaneously binds both the orthosteric binding site (OBS) and a secondary binding pocket (SBP)
Ravi Kumar Verma, Ara M Abramyan, Mayako Michino, R Benjamin Free, David R Sibley, Jonathan A Javitch, J Robert Lane, Lei Shi   +7 more
doaj   +1 more source