Results 1 to 10 of about 31,985 (308)

EAR-20 peptide, a novel NMDA receptor positive allosteric modulator [PDF]

Frontiers in Pharmacology
Allosteric modulation of ligand-gated ion channels provides a powerful mechanism to fine-tune their activity without competing with endogenous ligands.
Roberto García-Díaz, Roberto García-Díaz, Roberto García-Díaz, Aida Castellanos, Federico Miguez-Cabello, Javier Picañol, Anna Priscil·la Pérez-González, Esther Gratacòs-Batlle, Nohora Vega-Castro, Xavier Altafaj, Xavier Altafaj, Edwin A. Reyes-Guzmán, Edgar A. Reyes-Montaño, Xavier Gasull, Xavier Gasull, David Soto, David Soto   +16 more
doaj   +2 more sources

Characterization of a novel positive allosteric modulator of the α1A-Adrenergic receptor [PDF]

Current Research in Pharmacology and Drug Discovery, 2023
α1-Adrenergic Receptors (ARs) are G-protein Coupled Receptors (GPCRs) that regulate the sympathetic nervous system via the binding and activation of norepinephrine (NE) and epinephrine (Epi). α1-ARs control various aspects of neurotransmission, cognition,
Robert S. Papay, Jonathan D. Macdonald, Shaun R. Stauffer, Dianne M. Perez   +3 more
doaj   +2 more sources

PTK7 is a positive allosteric modulator of GPR133 signaling in glioblastoma [PDF]

Cell Reports, 2023
Summary: The adhesion G-protein-coupled receptor GPR133 (ADGRD1) supports growth of the brain malignancy glioblastoma. How the extracellular interactome of GPR133 in glioblastoma modulates signaling remains unknown.
Joshua D. Frenster, Hediye Erdjument-Bromage, Gabriele Stephan, Niklas Ravn-Boess, Shuai Wang, Wenke Liu, Devin Bready, Jordan Wilcox, Björn Kieslich, Manuel Jankovic, Caroline Wilde, Susanne Horn, Norbert Sträter, Ines Liebscher, Torsten Schöneberg, David Fenyo, Thomas A. Neubert, Dimitris G. Placantonakis   +17 more
doaj   +2 more sources

The binding and mechanism of a positive allosteric modulator of Kv3 channels [PDF]

Nature Communications
Small-molecule modulators of diverse voltage-gated K+ (Kv) channels may help treat a wide range of neurological disorders. However, developing effective modulators requires understanding of their mechanism of action.
Qiansheng Liang, Gamma Chi, Leonardo Cirqueira, Lianteng Zhi, Agostino Marasco, Nadia Pilati, Martin J. Gunthorpe, Giuseppe Alvaro, Charles H. Large, David B. Sauer, Werner Treptow, Manuel Covarrubias   +11 more
doaj   +2 more sources

Gestodene, a novel positive allosteric modulator of PAR1, enhances PAR1-mediated human platelet aggregation [PDF]

Frontiers in Pharmacology
Background: Protease-activated receptor 1 (PAR1) is expressed in human platelets and can be activated by low concentrations of thrombin. Vorapaxar, a selective antagonist of PAR1, inhibits thrombin-induced calcium mobilization in human platelet, which is
So-Hyeon Park, Yunkyung Heo, Il Kwon, Sungwoo Jo, Hyejin Jeon, Yechan Lee, Jieun Kim, Ji Hoe Heo, Wan Namkung, Wan Namkung   +9 more
doaj   +2 more sources

REPROGRAMMING CBX8-PRC1 FUNCTION WITH A POSITIVE ALLOSTERIC MODULATOR [PDF]

Cell Chemical Biology, 2021
ABSTRACTCanonical targeting of Polycomb Repressive Complex 1 (PRC1) to repress developmental genes is mediated by cell type-specific, paralogous chromobox (CBX) proteins (CBX2, 4, 6, 7 and 8). Based on their central role in silencing and their misregulation associated with human disease including cancer, CBX proteins are attractive targets for small ...
Junghyun L. Suh, Daniel Bsteh, Bryce Hart, Yibo Si, Tyler M. Weaver, Carina Pribitzer, Roy Lau, Shivani Soni, Heather Ogana, Justin M. Rectenwald, Jacqueline L. Norris, Stephanie H. Cholensky, Cari Sagum, Jessica D. Umana, Dongxu Li, Brian Hardy, Mark T. Bedford, Shannon M. Mumenthaler, Heinz-Josef Lenz, Yong-Mi Kim, Gang Greg Wang, Ken H. Pearce, Lindsey I. James, Dmitri B. Kireev, Catherine A. Musselman, Stephen V. Frye, Oliver Bell   +26 more
openaire   +3 more sources

Recent Advances in the Discovery of Nicotinic Acetylcholine Receptor Allosteric Modulators

Molecules, 2023
Positive allosteric modulators (PAMs), negative allosteric modulators (NAMs), silent agonists, allosteric activating PAMs and neutral or silent allosteric modulators are compounds capable of modulating the nicotinic receptor by interacting at allosteric ...
Dina Manetti, Silvia Dei, Hugo R. Arias, Laura Braconi, Alessio Gabellini, Elisabetta Teodori, Maria Novella Romanelli   +6 more
doaj   +1 more source

The allosterically modulated FFAR2 is transactivated by signals generated by other neutrophil GPCRs.

PLoS ONE, 2023
Positive allosteric modulators for free fatty acid receptor 2 (FFAR2/GPR43), that affect receptor function through binding to two distinct allosteric binding sites, were used to determine the correlation between the responses induced in neutrophils by ...
Simon Lind, Kenneth L Granberg, Huamei Forsman, Claes Dahlgren   +3 more
doaj   +2 more sources

Prospects for the use of allosteric drugs in real-world clinical practice

Реальная клиническая практика: данные и доказательства, 2023
While the clinical validity of the use of allosteric regulation is known, scientists are working on the discovery of new methods for the development of allosteric drugs that can modulate the functions of enzymes, depending on the desired therapeutic ...
I. R. Svechkareva, A. S. Kolbin
doaj   +1 more source

Conformational fingerprinting of allosteric modulators in metabotropic glutamate receptor 2

eLife, 2022
Activation of G protein-coupled receptors (GPCRs) is an allosteric process. It involves conformational coupling between the orthosteric ligand binding site and the G protein binding site. Factors that bind at non-cognate ligand binding sites to alter the
Brandon Wey-Hung Liauw, Arash Foroutan, Michael R Schamber, Weifeng Lu, Hamid Samareh Afsari, Reza Vafabakhsh   +5 more
doaj   +1 more source