Results 11 to 20 of about 121,181 (303)

A negative allosteric modulator of PDE4D enhances learning after traumatic brain injury. [PDF]

Neurobiol Learn Mem, 2018
&NA; Traumatic brain injury (TBI) significantly decreases cyclic AMP (cAMP) signaling which produces long‐term synaptic plasticity deficits and chronic learning and memory impairments.
Titus DJ, Wilson NM, Alcazar O, Calixte DA, Dietrich WD, Gurney ME, Atkins CM.   +6 more
europepmc   +3 more sources

A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist. [PDF]

Biochemistry, 2018
The WNT pathway interconnects a network of signaling events involved in a huge plethora of cellular processes, from organogenesis to tissue homeostasis. Despite its importance, the exiguity of organic drugs directly targeting the members of the Frizzled family of WNT receptors has hampered progress across the whole spectrum of biological fields in ...
Gennaro Riccio, Sara Bottone, G. La Regina, Nadia Badolati, S. Passacantilli, G. Rossi, A. Accardo, M. Dentice, R. Silvestri, E. Novellino, Mariano Stornaiuolo   +10 more
semanticscholar   +6 more sources

Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator [PDF]

eLife, 2017
Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex diseases (i.e. chronic pain). JF-NP-26 is an inactive photocaged derivative of the metabotropic glutamate type
Joan Font, Marc López-Cano, Serena Notartomaso, Pamela Scarselli, Paola Di Pietro, Roger Bresolí-Obach, Giuseppe Battaglia, Fanny Malhaire, Xavier Rovira, Juanlo Catena, Jesús Giraldo, Jean-Philippe Pin, Víctor Fernández-Dueñas, Cyril Goudet, Santi Nonell, Ferdinando Nicoletti, Amadeu Llebaria, Francisco Ciruela   +17 more
doaj   +3 more sources

The Antiseizure Drug Perampanel Is a Subunit-Selective Negative Allosteric Modulator of Kainate Receptors. [PDF]

J Neurosci, 2022
Perampanel (PMP) is a third-generation antiseizure drug reported to be a potent and selective noncompetitive negative allosteric modulator of one subfamily of ionotropic glutamate receptor (iGluR), the α-amino-3-hydroxy-S-methylisoxazole-4-propionic acid
Taniguchi S, Stolz JR, Swanson GT.
europepmc   +2 more sources

An aptamer agonist of the insulin receptor acts as a positive or negative allosteric modulator, depending on its concentration. [PDF]

Exp Mol Med, 2022
Aptamers are widely used as binders that interact with targets with high affinity or as inhibitors of the function of target molecules. However, they have also been used to modulate target protein function, which they achieve by activating the target or ...
Yunn NO, Lee J, Lee HS, Oh EJ, Park M, Park S, Jin SY, Shin E, Lee JWY, Kim Y, Bae SS, Ryu SH.   +11 more
europepmc   +2 more sources

Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of Cannabinoid CB1 Receptor Bound to a Negative Allosteric Modulator, ORG27569, and Analogs. [PDF]

J Med Chem, 2022
A growing number of G-protein-coupled receptor (GPCR) structures reveal novel transmembrane lipid-exposed allosteric sites. Ligands must first partition into the surrounding membrane and take lipid paths to these sites.
Obi P, Natesan S.
europepmc   +2 more sources

Basmisanil, a highly selective GABA_A-α5 negative allosteric modulator: preclinical pharmacology and demonstration of functional target engagement in man. [PDF]

Sci Rep, 2021
GABAA-α5 subunit-containing receptors have been shown to play a key modulatory role in cognition and represent a promising drug target for cognitive dysfunction, as well as other disorders.
Hipp JF, Knoflach F, Comley R, Ballard TM, Honer M, Trube G, Gasser R, Prinssen E, Wallace TL, Rothfuss A, Knust H, Lennon-Chrimes S, Derks M, Bentley D, Squassante L, Nave S, Nöldeke J, Wandel C, Thomas AW, Hernandez MC.   +19 more
europepmc   +2 more sources

Sodium is a negative allosteric regulator of the ghrelin receptor

Cell Reports, 2023
Summary: The functional properties of G protein-coupled receptors (GPCRs) are intimately associated with the different components in their cellular environment.
Guillaume Ferré, Antoniel A.S. Gomes, Maxime Louet, Marjorie Damian, Paulo M. Bisch, Olivier Saurel, Nicolas Floquet, Alain Milon, Jean-Louis Banères   +8 more
doaj   +2 more sources

The Negative Allosteric Modulator EU1794-4 Reduces Single-Channel Conductance and Ca²⁺ Permeability of GluN1/GluN2A N-Methyl-d-Aspartate Receptors. [PDF]

Mol Pharmacol, 2021
NMDA receptors are ligand-gated ion channels that mediate a slow, Ca2+-permeable component of excitatory synaptic currents. These receptors are involved in several important brain functions, including learning and memory, and have also been implicated in
Perszyk RE, Zheng Z, Banke TG, Zhang J, Xie L, McDaniel MJ, Katzman BM, Pelly SC, Yuan H, Liotta DC, Traynelis SF.   +10 more
europepmc   +2 more sources

Blocking glutamate mGlu₅ receptors with the negative allosteric modulator CTEP improves disease course in SOD1^G93A mouse model of amyotrophic lateral sclerosis. [PDF]

Br J Pharmacol, 2021
The pathogenesis of amyotrophic lateral sclerosis (ALS) is not fully clarified, although excessive glutamate (Glu) transmission and the downstream cytotoxic cascades are major mechanisms for motor neuron death. Two metabotropic glutamate receptors (mGlu1
Milanese M, Bonifacino T, Torazza C, Provenzano F, Kumar M, Ravera S, Zerbo AR, Frumento G, Balbi M, Nguyen TPN, Bertola N, Ferrando S, Viale M, Profumo A, Bonanno G.   +14 more
europepmc   +2 more sources