Results 61 to 70 of about 18,237 (210)

Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]

open access: yes, 2019
In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie   +3 more
core   +2 more sources

Structural Basis of M3 Muscarinic Receptor Dimer/Oligomer Formation [PDF]

open access: yesJournal of Biological Chemistry, 2011
Class A G protein-coupled receptors (GPCRs) are known to form dimers and/or oligomeric arrays in vitro and in vivo. These complexes are thought to play important roles in modulating class A GPCR function. Many studies suggest that residues located on the "outer" (lipid-facing) surface of the transmembrane (TM) receptor core are critically involved in ...
Tong Liu   +4 more
openaire   +3 more sources

The heartbreak of depression: 'Psycho-cardiac' coupling in myocardial infarction [PDF]

open access: yes, 2017
Ample evidence identifies strong links between major depressive disorder (MDD) and both risk of ischemic or coronary heart disease (CHD) and resultant morbidity and mortality. The molecular mechanistic bases of these linkages are poorly defined. Systemic
Budiono, Boris P   +5 more
core   +1 more source

Muscarinic modulation of M and h currents in gerbil spherical bushy cells.

open access: yesPLoS ONE, 2020
Descending cholinergic fibers innervate the cochlear nucleus. Spherical bushy cells, principal neurons of the anterior part of the ventral cochlear nucleus, are depolarized by cholinergic agonists on two different time scales.
Charlène Gillet   +2 more
doaj   +1 more source

G protein subunit dissociation and translocation regulate cellular response to receptor stimulation. [PDF]

open access: yesPLoS ONE, 2009
We examined the role of G proteins in modulating the response of living cells to receptor activation. The response of an effector, phospholipase C-beta to M3 muscarinic receptor activation was measured using sensors that detect the generation of inositol
Mariangela Chisari   +4 more
doaj   +1 more source

Physiological concentrations of bile acids down-regulate agonist induced secretion in colonic epithelial cells [PDF]

open access: yes, 2009
In patients with bile acid malabsorption, high concentrations of bile acids enter the colon and stimulate Cl− and fluid secretion, thereby causing diarrhoea. However, deoxycholic acid (DCA), the predominant colonic bile acid, is normally present at lower
Alan F. Hofmann   +45 more
core   +1 more source

Neuronal Endothelin a Receptor Mediates Experimental and Clinical Vascular Pain through an Endothelial‐Neural Axis

open access: yesAdvanced Science, EarlyView.
The authors develop mouse models by mimicking peripheral vascular diseases, combining multiple strategies and transgenic mouse lines, to demonstrate that ECs, but not macrophages or SMCs, play an active role mediated by endothelial ET‐1/neural ETAR signaling and beyond endothelial homeostatic angiocrine by driving protective pain through the ...
Zuo‐Jie Jiang   +28 more
wiley   +1 more source

A molecular basis for selective antagonist destabilization of dopamine D3 receptor quaternary organization [PDF]

open access: yes, 2017
The dopamine D3 receptor (D3R) is a molecular target for both first-generation and several recently-developed antipsychotic agents. Following stable expression of this mEGFP-tagged receptor, Spatial Intensity Distribution Analysis indicated that a ...
Caltabiano, Gianluigi   +6 more
core   +2 more sources

Intratumoral Nerve Phased Development: A Promising Therapeutic Target

open access: yesMedicine Bulletin, EarlyView.
ABSTRACT The nervous system has emerged as a critical regulator of tumor biology, engaging in dynamic crosstalk with cancer cells. Although the protumorigenic role of innervation is well established, increasing attention is now directed toward reciprocal influences—how tumors actively shape and remodel local nerve networks within the tumor ...
Xiangxian Che   +3 more
wiley   +1 more source

Adreno-Muscarinic Synergy of Contractile Responses From Human Hyperplastic Prostate [PDF]

open access: yesInternational Neurourology Journal
Purpose Adreno-muscarinic synergy, a supra-additional contractile response to simultaneous application of α-adrenoreceptor and muscarinic receptor agonists, is a feature of several lower urinary tract regions that have dual sympathetic and ...
Ben T. Blake-James   +2 more
doaj   +1 more source

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