Results 21 to 30 of about 1,200,697 (382)

Structural Probing and Molecular Modeling of the A3 Adenosine Receptor: A Focus on Agonist Binding

Molecules, 2017
Adenosine is an endogenous modulator exerting its functions through the activation of four adenosine receptor (AR) subtypes, termed A1, A2A, A2B and A3, which belong to the G protein-coupled receptor (GPCR) superfamily.
Antonella Ciancetta, Kenneth A. Jacobson
doaj   +1 more source

Cyclic nucleotide-gated channels: structural basis of ligand efficacy and allosteric modulation [PDF]

, 1997
Most working proteins, including metabolic enzymes, transcription regulators, and membrane receptors, transporters, and ion channels, share the property of allosteric coupling. The term 'allosteric' means that these proteins mediate indirect interactions
Lester, Henry A., Li, Jun, Zagotta, William N.   +2 more
core   +1 more source

Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]

, 2018
The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J., Broad, Lisa M., Brooke, Simon M., Bundgaard, Christoffer, Christopoulos, Arthur, Crabtree, Michael D., Dwomoh, Louis, Felder, Christian C., Langmead, Christopher J., Mogg, Adrian J., Molloy, Colin, Sanger, Helen E., Sexton, Patrick M., Thompson, Karen J., Tobin, Andrew B.   +14 more
core   +1 more source

Licraside as novel potent FXR agonist for relieving cholestasis: structure-based drug discovery and biological evaluation studies

Frontiers in Pharmacology, 2023
Cholestasis is a common clinical disease caused by a disorder in bile acids (BAs) homeostasis, which promotes its development. The Farnesoid X receptor (FXR) plays a critical role in regulating BAs homeostasis, making it an essential target for ...
Lili Xi, Axi Shi, Tiantian Shen, Guoxu Wang, Yuhui Wei, Jingjing Guo   +5 more
doaj   +1 more source

β2 Agonists [PDF]

, 2016
History suggests β agonists, the cognate ligand of the β2 adrenoceptor, have been used as bronchodilators for around 5,000 years, and β agonists remain today the frontline treatment for asthma and chronic obstructive pulmonary disease (COPD). The β agonists used clinically today are the products of significant expenditure and over 100 year's intensive ...
Charlotte K, Billington, Raymond B, Penn, Ian P, Hall   +2 more
openaire   +2 more sources

Immune Checkpoints as Therapeutic Targets in Autoimmunity

Frontiers in Immunology, 2018
Antibodies that block the immune checkpoint receptors PD1 and CTLA4 have revolutionized the treatment of melanoma and several other cancers, but in the process, a new class of drug side effect has emerged—immune related adverse events.
Christopher Paluch, Christopher Paluch, Ana Mafalda Santos, Ana Mafalda Santos, Consuelo Anzilotti, Consuelo Anzilotti, Richard J. Cornall, Richard J. Cornall, Simon J. Davis, Simon J. Davis   +9 more
doaj   +1 more source

Reconciling intrinsic properties of activating TNF receptors by native ligands versus synthetic agonists

Frontiers in Immunology, 2023
The extracellular domain of tumor necrosis factor receptors (TNFR) generally require assembly into a homotrimeric quaternary structure as a prerequisite for initiation of signaling via the cytoplasmic domains.
George Fromm, Suresh de Silva, Taylor H. Schreiber   +2 more
doaj   +1 more source

MODULATION OF CALCIUM CHANNELS IN ARTERIAL SMOOTH-MUSCLE CELLS BY DIHYDROPYRIDINE ENANTIOMERS [PDF]

, 1993
The actions of the optical enantiomers of BAY K 8644 and Sandoz 202,791 were studied on barium inward currents recorded using the whole-cell configuration of the patch clamp technique from enzymatically isolated smooth muscle cells from the rabbit ear ...
Bolton, TB, Hering, S, Hughes, AD, Timin, EN   +3 more
core   +1 more source

In Vitro and In Silico Characterization of G-Protein Coupled Receptor (GPCR) Targets of Phlorofucofuroeckol-A and Dieckol

Marine Drugs, 2021
Phlorotannins are polyphenolic compounds in marine alga, especially the brown algae. Among numerous phlorotannins, dieckol and phlorofucofuroeckol-A (PFF-A) are the major ones and despite a wider biological activity profile, knowledge of the G protein ...
Pradeep Paudel, Su Hui Seong, Se Eun Park, Jong Hoon Ryu, Hyun Ah Jung, Jae Sue Choi   +5 more
doaj   +1 more source

Combination formoterol and inhaled steroid versus beta(2)-agonist as relief medication for chronic asthma in adults and children (Review) [PDF]

, 2009
Background Formoterol has a fast onset of action and can therefore be used to relieve symptoms of asthma. A combination inhaler can deliver formoterol with different doses of inhaled corticosteroid; when used as a reliever both drugs will be delivered ...
Adams, Balanzat, Berggren, Bisgaard, Bisgaard, Bleecker, Bousquet, British Thoracic Society, Bruce, Buhl, Buhl, Cates, Christopher, Greenstone, Haahtela, Haahtela, Higgins, Higgins, Ind, Johansson, Jonkers, Kuna, Kuna, Lundborg, Ni Chroinin, O'Byrne, O'Byrne, O'Byrne, O'Byrne, O'Byrne, Palmqvist, Price, Price, Rabe, Rabe, Rabe, Richter, Salpeter, Scicchitano, Sears, Sovani, Stallberg, Tattersfield, Tattersfield, Vogelmeier, Vogelmeier, Walters   +46 more
core   +1 more source