Results 41 to 50 of about 176,232 (313)

Combined docking and machine learning identify key molecular determinants of ligand pharmacological activity on β2 adrenoceptor

Pharmacology Research & Perspectives, 2022
G protein‐coupled receptors (GPCRs) are valuable therapeutic targets for many diseases. A central question of GPCR drug discovery is to understand what determines the agonism or antagonism of ligands that bind them.
Mireia Jiménez‐Rosés, Bradley Angus Morgan, Maria Jimenez Sigstad, Thuy Duong Zoe Tran, Rohini Srivastava, Asuman Bunsuz, Leire Borrega‐Román, Pattarin Hompluem, Sean A. Cullum, Clare R. Harwood, Eline J. Koers, David A. Sykes, Iain B. Styles, Dmitry B. Veprintsev   +13 more
doaj   +1 more source

Curiouser and Curiouser: The Macrocyclic Lactone, Abamectin, Is also a Potent Inhibitor of Pyrantel/Tribendimidine Nicotinic Acetylcholine Receptors of Gastro-Intestinal Worms. [PDF]

PLoS ONE, 2016
Nematode parasites may be controlled with drugs, but their regular application has given rise to concerns about the development of resistance. Drug combinations may be more effective than single drugs and delay the onset of resistance.
Melanie Abongwa, Samuel K Buxton, Alan P Robertson, Richard J Martin   +3 more
doaj   +1 more source

Caffeine. cognitive and physical performance enhancer or psychoactive drug? [PDF]

, 2015
Caffeine use is increasing worldwide. The underlying motivations are mainly concentration and memory enhancement and physical performance improvement. Coffee and caffeine-containing products affect the cardiovascular system, with their positive inotropic
Aromatario, Mariarosaria, Cappelletti, Simone, Piacentino, Daria, Sani, Gabriele   +3 more
core   +1 more source

An ATP-Binding Cassette Pleiotropic Drug Transporter Protein Is Required for Xenobiotic Tolerance and Antagonism in the Fungal Biocontrol Agent Clonostachys rosea

Molecular Plant-Microbe Interactions, 2014
ATP-binding cassette (ABC) transporters mediate active efflux of natural and synthetic toxicants and are considered to be important for drug tolerance in microorganisms.
Mukesh K. Dubey, Dan Funck Jensen, Magnus Karlsson   +2 more
doaj   +1 more source

The phytocannabinoid, Δ(9) -tetrahydrocannabivarin, can act through 5-HT1 A receptors to produce antipsychotic effects [PDF]

, 2015
Funded by: •GW Pharmaceuticals Acknowledgements: The authors wish to thank Mrs Lesley Stevenson for technical support and Dr John Raymond, Dr Keith Parker and Dr Ethan Russo for providing human 5-HT1A CHO cells.
Cascio, Maria Grazia, Marini, Pietro, Parolaro, Daniela, Pertwee, Roger G., Zamberletti, Erica   +4 more
core   +1 more source

Transferrin receptor 1‐mediated iron uptake supports thermogenic activation in human cervical‐derived adipocytes

FEBS Letters, EarlyView.
In this study, we found that human cervical‐derived adipocytes maintain intracellular iron level by regulating the expression of iron transport‐related proteins during adrenergic stimulation. Melanotransferrin is predicted to interact with transferrin receptor 1 based on in silico analysis.
Rahaf Alrifai, Mizuki Seo, Gyath Karadsheh, Fachrur Rizal Mahendra, Máté Á Demény, Ferenc Győry, János András Mótyán, László Fésüs, Endre Kristóf, Rini Arianti   +9 more
wiley   +1 more source

A New Era of Muscarinic Acetylcholine Receptor Modulators in Neurological Diseases, Cancer and Drug Abuse

Pharmaceuticals
The cholinergic pathways in the central nervous system (CNS) play a pivotal role in different cognitive functions of the brain, such as memory and learning.
Helena Tsimpili, Grigoris Zoidis
doaj   +1 more source

When the most potent combination of antibiotics selects for the greatest bacterial load: the smile-frown transition.

PLoS Biology, 2013
Conventional wisdom holds that the best way to treat infection with antibiotics is to 'hit early and hit hard'. A favoured strategy is to deploy two antibiotics that produce a stronger effect in combination than if either drug were used alone.
Rafael Pena-Miller, David Laehnemann, Gunther Jansen, Ayari Fuentes-Hernandez, Philip Rosenstiel, Hinrich Schulenburg, Robert Beardmore   +6 more
doaj   +1 more source

Hypothermia but not NMDA receptor antagonism protects against stroke induced by distal middle cerebral arterial occlusion in mice.

PLoS ONE, 2020
Excitotoxicity mediated by the N-methyl-D-aspartate receptor (NMDAR) is believed to be a primary mechanism of neuronal injury following stroke. Thus, many drugs and therapeutic peptides were developed to inhibit either the NMDAR at the cell surface or ...
Che-Wei Liu, Kate Hsiurong Liao, Hsin Tseng, Ching Mei Wu, Hsiao-Yun Chen, Ted Weita Lai   +5 more
doaj   +1 more source

Acute antagonism in three-drug combinations for vaginal HIV prevention in humanized mice

Scientific Reports, 2023
Adolescent girls and young women in low- to middle-income countries are disproportionately at risk of becoming HIV-1 infected. New non-vaccine biomedical products aimed at overcoming this global health challenge need to provide a range of safe, effective,
Philippe A. Gallay, Christina M. Ramirez, Marc M. Baum   +2 more
doaj   +1 more source