Results 1 to 10 of about 107,657 (326)

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   +7 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   +5 more sources

4-Chlorophenylguanidine is an ASIC3 agonist and positive allosteric modulator

Journal of Pharmacological Sciences, 2017
Acid-sensing ion channels (ASICs) are proton-sensitive sodium channels that open in response to lowered extracellular pH and are expressed in the central and peripheral nervous systems.
Amruta S. Agharkar, Eric B. Gonzales
doaj   +4 more sources

Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABAA receptor positive allosteric modulator [PDF]

Neuropharmacology, 2020
Zuranolone (SAGE-217) is a novel, synthetic, clinical stage neuroactive steroid GABAA receptor positive allosteric modulator designed with the pharmacokinetic properties to support oral daily dosing.
Amit Modgil, Paul A Davies, Francesco G Salituro   +2 more
exaly   +3 more sources

Reprogramming CBX8-PRC1 function with a positive allosteric modulator [PDF]

Cell Chemical Biology, 2021
Canonical 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).
J. L. Suh, Daniel Bsteh, Yibo Si, Bryce Hart, T. Weaver, C. Pribitzer, R. Lau, S. Soni, H. Ogana, Justin M. Rectenwald, J. Norris, Stephanie H. Cholensky, Cari A. Sagum, Jessica D. Umana, Dongxu Li, Brian P. Hardy, M. Bedford, S. Mumenthaler, H. Lenz, Yong-Mi Kim, G. Wang, K. Pearce, L. James, D. Kireev, C. Musselman, S. Frye, O. Bell   +26 more
semanticscholar   +4 more sources

Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia

Nature Communications, 2023
TRPV1 as a drug target suffers from side effects of hypothermia. Here, authors engineer a peptide, sRhTx, as a positive allosteric modulator of TRPV1 channel. It potentiates the activity of TRPV1 to reversibly ablate pain-sensing nerve terminals for long-
Heng Zhang, Jia-Jia Lin, Ya-Kai Xie, Xiu-Zu Song, Jia-Yi Sun, Bei-Lei Zhang, Yun-Kun Qi, Zhen-Zhong Xu, Fan Yang   +8 more
doaj   +2 more sources

Suppression of neuroinflammation by an allosteric agonist and positive allosteric modulator of the α7 nicotinic acetylcholine receptor GAT107

Journal of Neuroinflammation, 2021
Background The α7 nicotinic acetylcholine receptor (α7 nAChR) negatively regulates the synthesis and release of pro-inflammatory cytokines by immune cells.
Tehila Mizrachi, Oshrit Marsha, Karen Brusin, Yael Ben-David, Ganesh A. Thakur, Adi Vaknin-Dembinsky, Millet Treinin, Talma Brenner   +7 more
doaj   +2 more sources

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

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   +3 more sources

Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7

Cell Chemical Biology, 2019
Polycomb-directed repression of gene expression is frequently misregulated in human diseases. A quantitative and target-specific cellular assay was utilized to discover the first potent positive allosteric modulator (PAM) peptidomimetic, UNC4976, of ...
Kelsey N Lamb, Daniel Bsteh, Sarah N Dishman   +2 more
exaly   +2 more sources