Results 191 to 200 of about 121,181 (303)

Novel GluN2B-Selective NMDA Receptor Negative Allosteric Modulator Possesses Intrinsic Analgesic Properties and Enhances Analgesia of Morphine in a Rodent Tail Flick Pain Model. [PDF]

ACS Chem Neurosci, 2023
Harris LD, Regan MC, Myers SJ, Nocilla KA, Akins NS, Tahirovic YA, Wilson LJ, Dingledine R, Furukawa H, Traynelis SF, Liotta DC.   +10 more
europepmc   +1 more source

Allosteric Competition and Inhibition in AMPA Receptors

Excitatory neurotransmission is principally mediated by α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-subtype ionotropic glutamate receptors (AMPARs).
Gonzalez, Cuauhtemoc U, Hale, W Dylan, Lau, Albert Y, Jayaraman, Vasanthi, Huganir, Richard L, Montaño Romero, Alejandra, Twomey, Edward C   +6 more
core   +1 more source

The Endothelial CXCR Family in Vascular Health and Disease

iNew Medicine, EarlyView.
ABSTRACT Endothelial cells (ECs) form the dynamic interface between blood and tissue, serving as key regulators of vascular homeostasis, inflammation, and repair. Among the molecular systems governing endothelial behavior, the C‐X‐C motif chemokine receptor (CXCR) family—originally characterized in immunology for its roles in leukocyte trafficking and ...
Zhiming Wu, Yandi Wu, Suowen Xu, Yu Huang, Li Wang   +4 more
wiley   +1 more source

Negative Allosteric Modulators of A_2AR: A New Weapon for Cancer Immunotherapy?

Journal of Medicinal Chemistry
Adenosine-mediated activation of A2AR drives immunosuppressive signaling in high-adenosine tumor microenvironments (TMEs), impeding anticancer immunity. Targeting A2AR with negative allosteric modulators (NAMs) is a promising approach for cancer immunotherapy: unlike the orthosteric antagonists currently in use, which face competitive and off-target ...
openaire   +3 more sources

Supporting Information: On-Cell Saturation Transfer Difference NMR Spectroscopy on Ion Channels: Characterizing Negative Allosteric Modulator Binding Interactions of P2X7

Double difference STD NMR spectra for AZ10606120 and JNJ-47965567 with WT hP2X7 (Figures S1 and S2); comparison of AZ10606120 and JNJ-47965567 positions in the binding pocket from XRD of pdP2X7 (Figure S3); comparison of docking poses for AZ10606120 and ...
Browne, Jacob, Angulo, Jesús, Wallace, Matthew, Stokes, Leanne, Monaco, Serena   +4 more
core   +1 more source

Advances in GPCRs Associated With Wnt Signaling Within the Auditory System

Medicine Bulletin, EarlyView.
ABSTRACT G protein‐coupled receptors (GPCRs) that interact with the Wnt signaling pathway are pivotal for auditory system homeostasis, as they orchestrate inner ear development, hair cell (HC) regeneration, and hearing preservation. Frizzled (FZD) receptors, the core Wnt‐related GPCRs, bind Wnt ligands and co‐receptors (e.g., LRP5/6) to activate both ...
Liang Wang, Changling Xu, Jiangang Fan, Renjie Chai   +3 more
wiley   +1 more source

Plasmepsins as Antimalarial Drug Targets—Then, Now, and the Future

Medicinal Research Reviews, EarlyView.
ABSTRACT Malaria is a devastating disease caused by Plasmodium parasites. Plasmodium parasites express ten cathepsin D‐like aspartyl proteases, called plasmepsins (PMs). These PMs have diverse roles fulfill diverse functions throughout the parasite's lifecycle, though several exhibit functional redundancies. Among them, PMV, PMIV, and PMX are essential
Brad E. Sleebs
wiley   +1 more source

Sustained treatment with an α5 GABA A receptor negative allosteric modulator delays excitatory circuit development while maintaining GABAergic neurotransmission. [PDF]

Neuropharmacology, 2021
Nuwer JL, Brady ML, Povysheva NV, Coyne A, Jacob TC.   +4 more
europepmc   +1 more source

Small‐Molecule Kinase Inhibitors Modulating Circadian Rhythms

Medicinal Research Reviews, EarlyView.
ABSTRACT The circadian clock mechanism generates 24‐h rhythms crucial for regulating various physiological processes, and its dysregulation has been implicated in numerous diseases. In cells, the circadian clock operates through a transcriptional‐translational feedback loop, where phosphorylation plays a pivotal role in maintaining accurate circadian ...
Irene Castellino, Manuela Bartolini, Rudolf Andrys, Kamil Musilek   +3 more
wiley   +1 more source

Targeting PAR-2 with a negative allosteric modulator increases tumor antigen presentation and potentiates anti-PD-1 immunotherapy. [PDF]

J Immunother Cancer
Aouad S, Kadiri M, Allard D, Skora E, Giraud L, Fuselier C, Desroys du Roure P, Mousson A, Janvier A, Baron L, Franchet C, Lecru L, Routy B, Malo J, Brugat T, Blayo AL, Schann S, Stagg J.   +17 more
europepmc   +1 more source