Results 41 to 50 of about 172,419 (282)

Mapping the druggable allosteric space of G-protein coupled receptors: a fragment-based molecular dynamics approach. [PDF]

, 2010
To address the problem of specificity in G-protein coupled receptor (GPCR) drug discovery, there has been tremendous recent interest in allosteric drugs that bind at sites topographically distinct from the orthosteric site. Unfortunately, structure-based
Ivetac, Anthony, McCammon, J Andrew
core   +2 more sources

Augmented β2-adrenergic signaling dampens the neuroinflammatory response following ischemic stroke and increases stroke size

Journal of Neuroinflammation, 2019
Background Ischemic stroke provokes a neuroinflammatory response and simultaneously promotes release of epinephrine and norepinephrine by the sympathetic nervous system.
Kendra J. Lechtenberg, Scott T. Meyer, Janelle B. Doyle, Todd C. Peterson, Marion S. Buckwalter   +4 more
doaj   +1 more source

Mirtazapine decreases stimulatory effects of reboxetine on cortisol, adrenocorticotropin and prolactin secretion in healthy male subjects [PDF]

, 2004
Reboxetine is a selective noradrenaline reuptake inhibitor, whereas mirtazapine acts as an antagonist at noradrenergic alpha(2), serotonin (5-HT2), 5-HT3 and histamine H-1 receptors.
Baghai, Thomas C., Laakmann, G., Schule, C.   +2 more
core   +1 more source

Lactoferrin treatment activates acetylcholinesterase, decreasing acetylcholine levels in non‐small cell lung cancer (NSCLC) cell culture supernatants, inhibiting cell survival

FEBS Open Bio, EarlyView.
Representation of the suggested mode of action of lactoferrin (Lf) in nonsmall cell lung cancer (NSCLC) A549 cells. Lf induces activation of caspase‐3 by activating p53 and AChE leading to decreased ACh concentrations. In turn, ACh signaling leads to activation of VEGF and AKT and blocking of caspase‐3.
Stuti Goel, Caroline Wozniak, Aya Sabri, Ben Haddad, Brooke Lopo, Alvaro Cobos, Sarah Sarofim, Jeffrey Guthrie, Deborah Heyl, Hedeel Guy Evans   +9 more
wiley   +1 more source

Anti-adrenergic effects of endothelin on human atrial action potentials are potentially anti-arrhythmic [PDF]

, 2006
Endothelin-1 (ET-1) is elevated in patients with atrial fibrillation (AF) and heart failure. We investigated effects of ET-1 on human atrial cellular electrophysiological measurements expected to influence the genesis and maintenance of AF.
Kane, K.A., Rankin, A.C., Redpath, C., Workman, A.J.   +3 more
core   +1 more source

Molecular determinants of signal transduction in tropomyosin receptor kinases

FEBS Open Bio, EarlyView.
Tropomyosin receptor kinases control critical neuronal functions, but how do the same receptors produce diverse cellular responses? This review explores the structural mechanisms behind Trk signaling diversity, focusing on allosteric modulation and ligand bias.
Giray Enkavi
wiley   +1 more source

Distribution and density of α- and β-adrenergic receptor binding sites in the bovine mammary gland [PDF]

, 2017
Radioreceptor binding studies were designed to localize and determine the number of α and β-adrenergic receptors in the mammary gland of lactating cows.
Blum, Jürg W., Bruckmaier, Rupert M., Hammon, Harald M., Honegger, Ulrich E.   +3 more
core  

Patatin‐domain‐containing (phospho)lipases under control: Mammalian co‐regulators and pathogenic activation mechanisms

FEBS Open Bio, EarlyView.
Patatin domain‐containing (phospho)lipases are lipid‐hydrolyzing enzymes central to metabolism, membrane remodeling, and signaling. Their activity relies on precise co‐activation mechanisms involving protein–protein interactions and conformational rearrangements.
Noopur Dubey, Lina Riegler‐Berket, Monika Oberer   +2 more
wiley   +1 more source

Synthesis, Docking Study and β-Adrenoceptor Activity of Some New Oxime Ether Derivatives

Molecules, 2014
A new series of oxime ethers 4a–z was designed and synthesized to test the blocking activity against β1 and β2-adrenergic receptors. Docking of these ether derivatives into the active site of the identified 3D structures of β1 and β2-adrenergic receptors
Hazem A. Ghabbour, Eman R. El-Bendary, Mahmoud B. El-Ashmawy, Mohamed M. El-Kerdawy   +3 more
doaj   +1 more source

Serum Activity Against G Protein–Coupled Receptors and Severity of Orthostatic Symptoms in Postural Orthostatic Tachycardia Syndrome

Journal of the American Heart Association: Cardiovascular and Cerebrovascular Disease, 2020
Background Postural orthostatic tachycardia syndrome (POTS) is characterized by excessive heart rate increase on standing and orthostatic intolerance. Previous data indicate autoimmune involvement.
Isabella Kharraziha, Jonas Axelsson, Fabrizio Ricci, Giuseppe Di Martino, Margaretha Persson, Richard Sutton, Artur Fedorowski, Viktor Hamrefors   +7 more
doaj   +1 more source