Results 91 to 100 of about 131,252 (300)

Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5

, 2022
Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed the location of allosteric binding sites and opened new opportunities for the discovery of novel modulators.
Guillaume Lebon (13850158), Jørgensen, Morten, Kampen, Stefanie, Maurel, Damien, Carlsson, Jens, Rodríguez, David,, Huang, Xinyan,, Monika Kruszyk-Kujawa, Michael Collins, Kampen, Stefanie,, Lebon, Guillaume, David Rodríguez (1632292), Morten Jørgensen (2200657), Stefanie Kampen, Jorgensen, Morten,, Damien Maurel (2020942), Monika Kruszyk-Kujawa (13850152), Axel Rudling, Jens Carlsson, Michael Collins (1905367), Boyle, Noel, Carlsson, Jens,, Jens Carlsson (584038), Maurel, Damien,, Axel Rudling (3691171), Kruszyk-Kujawa, Monika, Huang, Xinyan, David Rodríguez, Xinyan Huang (1335465), Stefanie Kampen (13850149), Guillaume Lebon, Rudling, Axel,, Boyle, Noel,, Lebon, Guillaume,, Collins, Michael, Jr., Damien Maurel, Rudling, Axel, Noel Boyle (13850155), Rodríguez, David, Collins, Michael, Kruszyk-Kujawa, Monika,, Noel Boyle, Collins, Michael, Jr.,, Jorgensen, Morten, Morten Jørgensen, Xinyan Huang   +45 more
core   +1 more source

Conformational Switching of Proteins on Material Surfaces Enabled by Peptide‐Oriented Adsorption

Advanced Functional Materials, EarlyView.
Responsive biointerfaces could be achieved using conformationally responsive proteins; however, their interconversion can be lost upon surface adsorption. Herein, we demonstrate that the incorporation a Au binding peptide into calmodulin allows for binding control on Au wherein the protein retains conformational switching. This capability was confirmed
Sakthirupini Ramamurthy, Kyle B. Meerbott, Lorenzo Travaglini, Garima S. Dobhal, Artur Sawicki, Marc R. Knecht, Tiffany R. Walsh, Dominic J. Glover   +7 more
wiley   +1 more source

Allosteric Regulation at the Crossroads of New Technologies: Multiscale Modeling, Networks, and Machine Learning

Frontiers in Molecular Biosciences, 2020
Allosteric regulation is a common mechanism employed by complex biomolecular systems for regulation of activity and adaptability in the cellular environment, serving as an effective molecular tool for cellular communication.
Gennady M. Verkhivker, Gennady M. Verkhivker, Steve Agajanian, Guang Hu, Peng Tao   +4 more
doaj   +1 more source

Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor [PDF]

, 2017
In this work, we explored the molecular framework of the known CB1R allosteric modulator PSNCBAM-1 with the aim to generate new bioactive analogs and to deepen the structure-activity relationships of this type of compounds.
Marco Macchia, Manera, Clementina, Chiara Arena, Saccomanni, Giuseppe, Bertini, Simone, Clementina Manera, Maria Digiacomo, Mary E. Abood, Gertsch, Jürg, Abood, Mary E., Jürg Gertsch, Simone Bertini, Daniela Nieri, Abood, Mary E, Macchia, Marco, Zhao, Pingwei, Gertsch, JÃ1⁄4rg, Chicca, Andrea, Pingwei Zhao, Digiacomo, Maria, Arena, Chiara, Nieri, Daniela, Andrea Chicca, Gado, Francesca, Francesca Gado, Giuseppe Saccomanni   +25 more
core   +2 more sources

Microfluidic Nano‐Assembly of Red‐Blood‐Cell (RBC) Lipids and Components for Engineering Extracellular Vesicles

Advanced Healthcare Materials, EarlyView.
Engineered red blood cell‐derived extracellular vesicles (eRBCEVs) are synthesized via controlled microfluidic assembly from native RBC lipids, enabling tunable encapsulation of proteins, nucleic acids, nanoparticles, and viral vectors. The platform demonstrates reproducible nanoscale architecture, preserved membrane composition, and functional cargo ...
Chiranth K. Nagaraj, Xilal Y. Rima, Kim T. Nguyen, Courtney Culkins, Nana Boateng, Jacob Doon‐Ralls, Alejandro Bresolin, Xin Huang, Hong Li, Vahedi Amid, Ajeet Pal Singh, Dharti Shantaram, Anastasiia Amari, Mangesh D. Hade, Nicholas R. Merriam, Zachary D. Schultz, Scott Q. Harper, Nizar Y. Saad, Setty M. Magaña, Willa A. Hsueh, Rachel E. Kopec, Blaise R. Kimmel, Andre F. Palmer, Eduardo Reátegui   +23 more
wiley   +1 more source

Allosteric enhancers, allosteric agonists and ago-allosteric modulators: where do they bind and how do they act?

, 2007
Udgivelsesdato: 2007-AugMany small-molecule agonists also display allosteric properties. Such ago-allosteric modulators act as co-agonists, providing additive efficacy--instead of partial antagonism--and they can affect--and often improve--the potency of
Schwartz, Thue W, Holst, Birgitte, Thue W. Schwartz, Birgitte Holst   +3 more
core   +1 more source

TOLLIP Inhibits Psoriasis Progression via Suppressing PKM2‐Mediated Glycolysis in Keratinocytes

Advanced Science, EarlyView.
In this study, we identify TOLLIP as a critical regulator of psoriasis pathogenesis through its modulation of glycolytic metabolism. Our findings establish the TOLLIP‐PKM2‐glycolysis axis as a key mechanism linking metabolic reprogramming to psoriasis pathogenesis, and propose TOLLIP as a promising therapeutic target.
Xiuhuan Jiang, Guoying Miao, Na Shen, Qingxia Han, Xiaoru Han, Zichang Qiao, Kexin Feng, Zhuo Tan, Yaguang Wang, Xiuhua Liu, Chen Wu, Zhenzhen Yan   +11 more
wiley   +1 more source

Analysis of equilibrium binding of an orthosteric tracer and two allosteric modulators.

PLoS ONE, 2019
Allosteric ligands bind to receptors at sites that are distinct from those endogenous agonists and orthosteric pharmacological agents interact with. Both an allosteric and orthosteric ligand bind simultaneously to the receptor to form a ternary complex ...
Jan Jakubík, Alena Randáková, Esam E El-Fakahany, Vladimír Doležal   +3 more
doaj   +1 more source

Allosteric modulation of adenosine A1 and cannabinoid 1 receptor signaling by G‐peptides

Pharmacology Research & Perspectives, 2020
While allosteric modulation of GPCR signaling has gained prominence to address the need for receptor specificity, efforts have mainly focused on allosteric sites adjacent to the orthosteric ligand‐binding pocket and lipophilic molecules that target ...
Anja M. Touma, Rabia U. Malik, Tejas Gupte, Sivaraj Sivaramakrishnan   +3 more
doaj   +1 more source

Design and Engineering of an Artificial Bifunctional N‐Deacetylase/N‐Sulfotransferase for the Biosynthesis of N‐Sulfated Heparosan

Advanced Science, EarlyView.
An artificial bifunctional N‐deacetylase/N‐sulfotransferase was engineered in Escherichia coli by combining screened N‐deacetylases with an NST domain. The integrated engineering strategy improved enzyme performance. The optimized enzyme efficiently converted heparosan into N‐sulfated heparosan, addressing a key bottleneck in microbial heparin ...
Xintong Xi, Ruirui Xu, Daoan Wang, Guobin Yin, Xinjing Wang, Haiqin Chen, Guocheng Du, Jian Chen, Zhen Kang   +8 more
wiley   +1 more source