Results 51 to 60 of about 13,221 (154)

Negative and positive allosteric modulators of the P2X₇receptor [PDF]

British Journal of Pharmacology, 2008
Background and purpose:Antagonist effects at the P2X7receptor are complex with many behaving in a non‐competitive manner. In this study, the effects ofN‐[2‐({2‐[(2‐hydroxyethyl)amino]ethyl}amino)‐5‐quinolinyl]‐2‐tricyclo[3.3.1.13,7]dec‐1‐ylacetamide (compound‐17) andN2‐(3,4‐difluorophenyl)‐N1‐[2‐methyl‐5‐(1‐piperazinylmethyl)phenyl]glycinamide ...
A D, Michel, L J, Chambers, D S, Walter
openaire   +2 more sources

Negative allosteric modulators of cannabinoid receptor 1: Ternary complexes including CB1, orthosteric CP55940 and allosteric ORG27569

Journal of Biomolecular Structure and Dynamics, 2021
In October 2019, the first X-ray crystal structure of a ternary cannabinoid receptor 1 (CB1) complex (PDB ID: 6KQI) was published, including the well-known orthosteric agonist, CP55940, and the well-studied negative allosteric modulator, ORG27569.
AyoOluwa O. Aderibigbe, Pankaj Pandey, Robert J. Doerksen   +2 more
openaire   +3 more sources

Distinct potency of compounds targeting the T1R3 subunit in modulating the response of human sweet and umami taste receptors

Scientific Reports
The heterodimeric G-protein-coupled receptors T1R2/T1R3 and T1R1/T1R3 have been identified as sweet and umami taste receptors, respectively, and both of these receptors share the T1R3 subunit.
Maiko Kawasaki, Yuta Kidera, Ryusei Goda, Chiaki Taketani, Misato Ide, Wataru Fujii, Tomoya Nakagita, Takumi Misaka   +7 more
doaj   +1 more source

Structural Basis for Negative Allosteric Modulation of GluN2A-Containing NMDA Receptors [PDF]

Neuron, 2016
NMDA receptors mediate excitatory synaptic transmission and regulate synaptic plasticity in the central nervous system, but their dysregulation is also implicated in numerous brain disorders. Here, we describe GluN2A-selective negative allosteric modulators (NAMs) that inhibit NMDA receptors by stabilizing the apo state of the GluN1 ligand-binding ...
Feng, Yi, Tung-Chung, Mou, Katherine N, Dorsett, Robert A, Volkmann, Frank S, Menniti, Stephen R, Sprang, Kasper B, Hansen   +6 more
openaire   +2 more sources

Negative Modulation of the Metabotropic Glutamate Receptor Type 5 as a Potential Therapeutic Strategy in Obesity and Binge-Like Eating Behavior

Frontiers in Neuroscience, 2021
Obesity is a multifactorial disease, which in turn contributes to the onset of comorbidities, such as diabetes and atherosclerosis. Moreover, there are only few options available for treating obesity, and most current pharmacotherapy causes severe ...
Tadeu P. D. Oliveira, Bruno D. C. Gonçalves, Bruna S. Oliveira, Antonio Carlos P. de Oliveira, Helton J. Reis, Claudia N. Ferreira, Daniele C. Aguiar, Aline S. de Miranda, Fabiola M. Ribeiro, Erica M. L. Vieira, András Palotás, András Palotás, Luciene B. Vieira   +12 more
doaj   +1 more source

Analysis of positive and negative allosteric modulation in metabotropic glutamate receptors 4 and 5 with a dual ligand

Scientific Reports, 2017
As class C GPCRs and regulators of synaptic activity, human metabotropic glutamate receptors (mGluRs) 4 and 5 are prime targets for allosteric modulation, with mGlu5 inhibition or mGlu4 stimulation potentially treating conditions like chronic pain and ...
James A. R. Dalton, Jean-Philippe Pin, Jesús Giraldo   +2 more
doaj   +1 more source

Modulating Human Follicle Stimulating Hormone Signaling Activity Using Negative Allosteric Modulators

The FASEB Journal, 2019
Human follicle stimulating hormone (hFSH) is a gonadotropin hormone involved in maturation of ovarian follicles and estrogen production in females and spermatogenesis in males. Its release is regulated via the hypothalamic‐pituitary‐gonadal axis.
Jillian R Love, Brian D Cohen
openaire   +1 more source

The E2.65A mutation disrupts dynamic binding poses of SB269652 at the dopamine D2 and D3 receptors. [PDF]

PLoS Computational Biology, 2018
The dopamine D2 and D3 receptors (D2R and D3R) are important targets for antipsychotics and for the treatment of drug abuse. SB269652, a bitopic ligand that simultaneously binds both the orthosteric binding site (OBS) and a secondary binding pocket (SBP)
Ravi Kumar Verma, Ara M Abramyan, Mayako Michino, R Benjamin Free, David R Sibley, Jonathan A Javitch, J Robert Lane, Lei Shi   +7 more
doaj   +1 more source

Cannabidiol binding and negative allosteric modulation at the cannabinoid type 1 receptor in the presence of delta-9-tetrahydrocannabinol: An In Silico study.

PLoS ONE, 2019
Recent evidence has raised in discussion the possibility that cannabidiol can act as a negative allosteric modulator of the cannabinoid type 1 receptor. Here we have used computational methods to study the modulation exerted by cannabidiol on the effects
Hery Chung, Angélica Fierro, C David Pessoa-Mahana   +2 more
doaj   +1 more source

Steroid hormone receptors and prostate cancer: role of structural dynamics in therapeutic targeting

Asian Journal of Andrology, 2016
Steroid hormone receptors (SHRs) act in cell type- and gene-specific manner through interactions with coregulatory proteins to regulate numerous physiological and pathological processes at the level of gene regulation.
Raj Kumar
doaj   +1 more source