Results 31 to 40 of about 18,231 (213)

Molecular determinants involved in the allosteric control of agonist affinity in the GABAB receptor by the GABAB2 subunit [PDF]

open access: yesThe Journal of Biological Chemistry 279, 16 (2004) 15824-30, 2008
The gamma-aminobutyric acid type B (GABAB) receptor is an allosteric complex made of two subunits, GABAB1 (GB1) and GABAB2 (GB2). Both subunits are composed of an extracellular Venus flytrap domain (VFT) and a heptahelical domain (HD). GB1 binds GABA, and GB2 plays a major role in G-protein activation as well as in the high agonist affinity state of ...
arxiv   +1 more source

Communication over the network of binary switches regulates the activation of A$_{2A}$ adenosine receptor [PDF]

open access: yesPLoS Comp. Biol. (2015) 11(2): e1004044, 2014
Dynamics and functions of G-protein coupled receptors (GPCRs) are accurately regulated by the type of ligands that bind to the orthosteric or allosteric binding sites. To glean the structural and dynamical origin of ligand-dependent modulation of GPCR activity, we performed total $\sim$ 5 $\mu$sec molecular dynamics simulations of A$_{2A}$ adenosine ...
arxiv   +1 more source

Novel Roles for Kv7 Channels in Shaping Histamine-Induced Contractions and Bradykinin-Dependent Relaxations in Pig Coronary Arteries. [PDF]

open access: yesPLoS ONE, 2016
Voltage-gated Kv7 channels are inhibited by agonists of Gq-protein-coupled receptors, such as histamine. Recent works have provided evidence that inhibition of vascular Kv7 channels may trigger vessel contractions.
Xingjuan Chen   +3 more
doaj   +1 more source

PKC-dependent Phosphorylation of the H1 Histamine Receptor Modulates TRPC6 Activity

open access: yesCells, 2014
Transient receptor potential canonical 6 (TRPC6) is a cation selective, DAG-regulated, Ca2+-permeable channel activated by the agonists of Gq-protein-coupled heptahelical receptors.
Xingjuan Chen   +7 more
doaj   +1 more source

Neuroreceptor Activation by Vibration-Assisted Tunneling [PDF]

open access: yesScientific Reports 5, Article number: 9990 Published 2015, 2015
G protein-coupled receptors (GPCRs) constitute a large family of receptor proteins that sense molecular signals on the exterior of a cell and activate signal transduction pathways within the cell. Modeling how an agonist activates such a receptor is fundamental for an understanding of a wide variety of physiological processes and it is of tremendous ...
arxiv   +1 more source

Histamine-3 Receptor Inverse Agonists for the Treatment of Obesity: Validation of the Target and Identification of Novel Series

open access: yesCHIMIA, 2009
Obesity is a major risk factor for the development of conditions such as hypertension, hyperglycemia, dyslipidemia, coronary artery disease and cancer.
Pascale David Pierson   +18 more
doaj   +1 more source

Effect of parenchymal stiffness on canine airway size with lung inflation. [PDF]

open access: yesPLoS ONE, 2010
Although airway patency is partially maintained by parenchymal tethering, this structural support is often ignored in many discussions of asthma. However, agonists that induce smooth muscle contraction also stiffen the parenchyma, so such parenchymal ...
Robert H Brown   +2 more
doaj   +1 more source

A normative theory of social conflict [PDF]

open access: yesarXiv, 2023
Social hierarchy in animal groups carries a crucial adaptive function by reducing conflict and injury while protecting valuable group resources. Social hierarchy is dynamic and can be altered by social conflict, agonistic interactions, and aggression.
arxiv  

FFAR1 activation attenuates histamine-induced myosin light chain phosphorylation and cortical tension development in human airway smooth muscle cells

open access: yesRespiratory Research, 2020
Background Activation of free fatty acid receptors (FFAR1 and FFAR4) which are G protein-coupled receptors (GPCRs) with established (patho)physiological roles in a variety of obesity-related disorders, induce human airway smooth muscle (HASM) cell ...
Shengjie Xu   +8 more
doaj   +1 more source

Analytical and Pharmacological Characterization of 1‐(Furan‐2‐Carbonyl)‐LSD (1F‐LSD) and Comparison With 1‐(Thiophene‐2‐Carbonyl)‐LSD (1T‐LSD)

open access: yesDrug Testing and Analysis, EarlyView.
The novel lysergamide 1‐(furan‐2‐carbonyl)‐LSD (1F‐LSD) was analytically characterized. 1F‐LSD showed LSD‐like activity in vivo similar to 1‐(thiophene‐2‐carbonyl)‐LSD (1T‐LSD) used for comparison. Administration studies in mice and LC–MS analysis revealed that 1F‐LSD served as a prodrug.
Simon D. Brandt   +5 more
wiley   +1 more source

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