Results 51 to 60 of about 3,750,504 (279)

Allo-network drugs: Extension of the allosteric drug concept to protein-protein interaction and signaling networks [PDF]

, 2013
Allosteric drugs are usually more specific and have fewer side effects than orthosteric drugs targeting the same protein. Here, we overview the current knowledge on allosteric signal transmission from the network point of view, and show that most ...
Csermely, Péter, Nussinov, Ruth, Szilágyi, András, Nussinov R   +3 more
core   +2 more sources

Discovery of Novel Gq-Biased LPA1 Negative Allosteric Modulators [PDF]

SLAS Discovery, 2017
Lysophosphatidic acid (LPA) activates the G-protein-coupled receptor LPA1, which regulates various cellular processes, including cell proliferation and migration. Although LPA1 transduces cellular responses via Gq, Gi, and G12/13, associations between these signaling molecules and cellular phenotypes remain poorly characterized due to the lack of ...
Yuji, Shimizu, Masaharu, Nakayama
openaire   +2 more sources

Amyloid Beta Peptide Is an Endogenous Negative Allosteric Modulator of Leptin Receptor [PDF]

Neuroendocrinology, 2020
<b><i>Introduction:</i></b> Metabolic dysfunction is now recognized as a pivotal component of Alzheimer’s disease (AD), the most common dementia worldwide. However, the precise molecular mechanisms linking metabolic dysfunction to AD remain elusive.
Cecon, Erika, Lhomme, Tori, Maurice, Tangui, Luka, Marine, Chen, Min, Silva, Anisia, Wauman, Joris, Zabeau, Lennart, Tavernier, Jan, Prévot, Vincent, Dam, Julie, Jockers, Ralf   +11 more
openaire   +3 more sources

In Vivo Non-radioactive Assessment of mGlu5 Receptor-Activated Polyphosphoinositide Hydrolysis in Response to Systemic Administration of a Positive Allosteric Modulator

Frontiers in Pharmacology, 2018
mGlu5 receptor-mediated polyphosphoinositide (PI) hydrolysis is classically measured by determining the amount of radioactivity incorporated in inositolmonophosphate (InsP) after labeling of membrane phospholipids with radioactive inositol. Although this
Anna R. Zuena, Luisa Iacovelli, Rosamaria Orlando, Luisa Di Menna, Paola Casolini, Giovanni Sebastiano Alemà, Gabriele Di Cicco, Giuseppe Battaglia, Ferdinando Nicoletti, Ferdinando Nicoletti   +9 more
doaj   +1 more source

Effect of δ value on binding of allosteric modulator to two allosteric sites.

, 2019
Simulation of tracer binding (ordinate) in the presence an allosteric modulator binding to two allosteric sites for various combinations of positive and negative cooperativity with the tracer indicated at headings of individual plots.
Esam E. El-Fakahany (339452), Alena Randáková (339451), Jan Jakubík (339449), Vladimír Doležal (339453)   +3 more
core   +1 more source

Neuronal activity patterns in the mediodorsal thalamus and related cognitive circuits are modulated by metabotropic glutamate receptors. [PDF]

, 2015
The mediodorsal thalamus (MD) likely plays an important role in cognition as it receives abundant afferent connections from the amygdala and prefrontal cortex (PFC).
Salt, T.E., Copeland, C.S., Neale, S.A., Neale, SA, Salt, TE, Copeland, CS   +5 more
core   +1 more source

A Light-Controlled Allosteric Modulator Unveils a Role for mGlu4 Receptors During Early Stages of Ischemia in the Rodent Cerebellar Cortex

Frontiers in Cellular Neuroscience, 2018
Metabotropic glutamate receptors (mGlus) are G Protein coupled-receptors that modulate synaptic transmission and plasticity in the central nervous system.
Simon Bossi, Romain Helleringer, Micaela Galante, Ester Monlleó, Ana Trapero, Xavier Rovira, Hervé Daniel, Amadeu Llebaria, Heather McLean   +8 more
doaj   +1 more source

Negative and positive allosteric modulators of the P2X ₇ receptor [PDF]

British Journal of Pharmacology, 2008
Background and purpose: Antagonist effects at the P2X 7 receptor are complex with many behaving in a non‐competitive manner. In this study, the effects of N ‐[2‐({2‐[(2‐hydroxyethyl)amino]ethyl}amino)‐5‐
A D, Michel, L J, Chambers, D S, Walter
openaire   +2 more sources

Effect of γ value on binding of allosteric modulator to two allosteric sites.

, 2019
Simulation of tracer binding (ordinate) in the presence an allosteric modulator binding to two allosteric sites for various combinations of positive and negative cooperativity with the tracer indicated at headings of individual plots.
Esam E. El-Fakahany (339452), Alena Randáková (339451), Jan Jakubík (339449), Vladimír Doležal (339453)   +3 more
core   +1 more source

Negative and positive allosteric modulators of the α7 nicotinic acetylcholine receptor regulates the ability of adolescent binge alcohol exposure to enhance adult alcohol consumption

Frontiers in Behavioral Neuroscience, 2023
Rationale and Objectives: Ethanol acts directly on the α7 Nicotinic acetylcholine receptor (α7). Adolescent-binge alcohol exposure (ABAE) produces deleterious consequences during adulthood, and data indicate that the α7 receptor regulates these damaging ...
Zachary A. Rodd, Zachary A. Rodd, H. Scott Swartzwelder, R. Aaron Waeiss, R. Aaron Waeiss, Serhii O. Soloviov, Serhii O. Soloviov, Debomoy K. Lahiri, Debomoy K. Lahiri, Debomoy K. Lahiri, Debomoy K. Lahiri, Debomoy K. Lahiri, Eric A. Engleman, Eric A. Engleman, William A. Truitt, William A. Truitt, Richard L. Bell, Richard L. Bell, Sheketha R. Hauser, Sheketha R. Hauser   +19 more
doaj   +1 more source