Results 41 to 50 of about 13,221 (154)

A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist

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, Giuseppe La Regina, Nadia Badolati, Sara Passacantilli, Giovanni Battista Rossi, Antonella Accardo, Monica Dentice, Romano Silvestri, Ettore Novellino, Mariano Stornaiuolo   +10 more
openaire   +4 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

Discovery of a Negative Allosteric Modulator of GABA_B Receptors [PDF]

ACS Medicinal Chemistry Letters, 2014
Initialized from the scaffold of CGP7930, an allosteric agonist of GABAB receptors, a series of noncompetitive antagonists were discovered. Among these compounds, compounds 3, 6, and 14 decreased agonist GABA-induced maximal effect of IP3 production in HEK293 cells overexpressing GABAB receptors and Gqi9 proteins without changing the EC50. Compounds 3,
Lin-Hai, Chen, Bing, Sun, Yang, Zhang, Tong-Jie, Xu, Zhi-Xiong, Xia, Jian-Feng, Liu, Fa-Jun, Nan   +6 more
openaire   +2 more sources

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 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

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

Oral expressions and functional analyses of the extracellular calcium-sensing receptor (CaSR) in chicken

Scientific Reports, 2022
In vertebrates, the extracellular calcium-sensing receptor (CaSR) plays a key role in calcium homeostasis by sensing slight changes in extracellular Ca2+. CaSR is also expressed in mammals including rodent taste cells and is involved in sensing kokumi, a
Hikaru Omori, Yuko Kawabata, Yuta Yoshida, Yutaro Nagamoto, Fuminori Kawabata, Shotaro Nishimura, Shoji Tabata   +6 more
doaj   +1 more source

Integrative residue-intuitive machine learning and MD Approach to Unveil Allosteric Site and Mechanism for β2AR

Nature Communications
Allosteric drugs offer a new avenue for modern drug design. However, the identification of cryptic allosteric sites presents a formidable challenge. Following the allostery nature of residue-driven conformation transition, we propose a state-of-the-art ...
Xin Chen, Kexin Wang, Jianfang Chen, Chao Wu, Jun Mao, Yuanpeng Song, Yijing Liu, Zhenhua Shao, Xuemei Pu   +8 more
doaj   +1 more source

Targeting of Metabotropic Glutamate Receptors for the Development of Novel Antidepressants

Chronic Stress, 2019
Since discovering that ketamine has robust antidepressant effects, the glutamatergic system has been proposed as an attractive target for the development of novel antidepressants.
Shigeyuki Chaki, Hiroyuki Koike, Kenichi Fukumoto   +2 more
doaj   +1 more source

Pitfalls of NMDA Receptor Modulation by Neuroactive Steroids. The Effect of Positive and Negative Modulation of NMDA Receptors in an Animal Model of Schizophrenia

Biomolecules, 2021
Evidence from clinical and preclinical studies implicates dysfunction of N-methyl-D-aspartate receptors (NMDARs) in schizophrenia progression and symptoms.
Kristina Holubova, Marketa Chvojkova, Barbora Hrcka Krausova, Vojtech Vyklicky, Eva Kudova, Hana Chodounska, Ladislav Vyklicky, Karel Vales   +7 more
doaj   +1 more source