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