G-protein-coupled receptors (GPCRs) are currently the most important pharmaceutical targets for drug discovery because they regulate a wide variety of physiological processes. Consequently, simple and convenient detection systems for ligands that regulate the function of GPCR have attracted attention as powerful tools for new drug development. We previously developed a yeast-based fluorescence ...

The adenosine A1 receptor (A1AR) is a G-protein-coupled (GPCR) that provides important therapeutic opportunities for number of conditions including congestive heart failure, tachycardia, and neuropathic pain. development A1AR-selective fluorescent ligands will enhance our understanding the subcellular mechanisms underlying A1AR pharmacology facilitating more efficacious selective therapies. Her...

Timolol is a non-selective beta-adrenergic receptor antagonist administered for treating glaucoma, heart attacks and hypertension. In the present study, we set out to determine whether or not timolol can provoke cataract formation, thus the influence of timolol on the amyloid-type aggregation of crystallin was investigated. We then provided experimental evidence of crystallin aggregation and it...

Blood contamination, such as bloody ascites or hemorrhages during surgery, is a potential hazard for clinical application of fluorescence imaging. In order to overcome this problem, we investigate if fluorescence-lifetime imaging helps to overcome this problem. Samples were prepared at concentrations ranging 0.3-2.4 μm and mixed with 0-10% of blood. Fluorescence intensities and lifetimes of sam...

A conjugate of the high affinity benzodiazepine receptor ligand Ro 15-1788 and the fluorescent 7-nitrobenz-2-oxa-1,3-diazol-4-yl (NBD) moiety was synthesized. This novel compound (BD 623) exhibited excitation and emission maxima at 486 and 542 nm, respectively, and possessed fluorescent properties that are dependent upon the polarity of its environment. BD 623 bound reversibly to benzodiazepine...

Localization and tracking of individual receptors by single-molecule imaging opens unique possibilities to unravel the assembly dynamics signaling complexes in plasma membrane. For this purpose, we here developed a comprehensive workflow for analyzing receptor diffusion interaction live cells at single molecule level with up four colors. We engineered two monomeric GFP variants, which are ortho...

Timolol is a non-selective beta-adrenergic receptor antagonist administered for treating glaucoma, heart attacks and hypertension. In the present study, we set out to determine whether or not timolol can provoke cataract formation, thus the influence of timolol on the amyloid-type aggregation of crystallin was investigated. We then provided experimental evidence of crystallin aggregation and it...

The distal photoreceptors in the tiered retina of Papilio exhibit different spectral sensitivities. There are at least two types of short-wavelength sensitive receptors: an ultraviolet receptor with a normal spectral shape and a violet receptor with a very narrow spectral bandwidth. Furthermore, a blue receptor, a double-peaked green receptor and a single-peaked green receptor exist. The violet...

Limbic encephalitis is an adaptive autoimmune disease, induced by different autoantibodies, which target extracellular neuronal epitopes, such as NMDA or GABAB receptors1,2. Recently our group found another human antibody, which binds to the α1 subunit of the GABAA receptor. Since the GABAA receptor is responsible for the majority of fast inhibitory neurotransmission, we investigated chan...