Results 11 to 20 of about 766,676 (298)
Characterization of TR‐107, a novel chemical activator of the human mitochondrial protease ClpP
Pharmacology Research & Perspectives, 2022 We recently described the identification of a new class of small‐molecule activators of the mitochondrial protease ClpP. These compounds synthesized by Madera Therapeutics showed increased potency of cancer growth inhibition over the related compound ...
Emily M. J. Fennell +16 more
doaj +1 more source
A TNFR2-Specific TNF Fusion Protein With Improved In Vivo Activity
Frontiers in Immunology, 2022 Tumor necrosis factor (TNF) receptor-2 (TNFR2) has attracted considerable interest as a target for immunotherapy. Indeed, using oligomeric fusion proteins of single chain-encoded TNFR2-specific TNF mutants (scTNF80), expansion of regulatory T cells and ...
Juan Gamboa Vargas +20 more
doaj +1 more source
α1D-Adrenoceptors are responsible for the high sensitivity and the slow time-course of noradrenaline-mediated contraction in conductance arteries [PDF]
, 2013 The objective of this study was to determine whether the different time-course characteristics of α1-adrenoceptor-mediated contraction in arteries can be related to the subtypes involved.
Alexander +53 more
core +1 more source
Marine Drugs, 2023 Hypaphorines, tryptophan derivatives, have anti-inflammatory activity, but their mechanism of action was largely unknown. Marine alkaloid L-6-bromohypaphorine with EC50 of 80 μM acts as an agonist of α7 nicotinic acetylcholine receptor (nAChR) involved ...
Igor A. Ivanov +17 more
doaj +1 more source
, 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 +2 more
openaire +2 more sources
Molecules, 2023 With overexpression in various cancers, the gastrin-releasing peptide receptor (GRPR) is a promising target for cancer imaging and therapy. However, the high pancreas uptake of reported GRPR-targeting radioligands limits their clinical application.
Lei Wang +9 more
doaj +1 more source
High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist
Molecules, 2021 Relaxin/insulin-like family peptide receptor 3 (RXFP3) belongs to class A G protein-coupled receptor family. RXFP3 and its endogenous ligand relaxin-3 are mainly expressed in the brain with important roles in the regulation of appetite, energy metabolism,
Guangyao Lin +11 more
doaj +1 more source
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
Probing the role of the cation–π interaction in the binding sites of GPCRs using unnatural amino acids [PDF]
, 2009 We describe a general application of the nonsense suppression methodology for unnatural amino acid incorporation to probe drug–receptor interactions in functional G protein-coupled receptors (GPCRs), evaluating the binding sites of both the M2 muscarinic
Ballesteros +31 more
core +3 more sources
Effects of methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and in Balb/c mice exposed to a radial-arm maze [PDF]
, 2012 The role of the histamine H3 receptor (H3R) in anxiety is controversial, due to limitations in drug selectivity and limited validity of behavioral tests used in previous studies. In the present report, we describe two experiments.
Abuhamdah, Rushdie M. +4 more
core +1 more source