• Biomolecules & Therapeutics
• /
• 제19권1호
• /
• pp.1-8
• /
• 2011

G-protein coupled receptors (GPCRs) constitute an important class of drug targets and are involved in every aspect of human physiology including sleep regulation, blood pressure, mood, food intake, perception of pain, control of cancer growth, and immune response. Radiometric assays have been the classic method used during the search for potential therapeutics acting at various GPCRs for most GPCR-based drug discovery research programs. An increasing number of diverse small molecules, together with novel GPCR targets identified from genomics efforts, necessitates the use of high-throughput assays with a good sensitivity and specificity. Currently, a wide array of high-throughput tools for research on GPCRs is available and can be used to study receptor-ligand interaction, receptor driven functional response, receptor-receptor interaction,and receptor internalization. Many of the assay technologies are based on luminescence or fluorescence and can be easily applied in cell based models to reduce gaps between in vitro and in vivo studies for drug discovery processes. Especially, cell based models for GPCR can be efficiently employed to deconvolute the integrated information concerning the ligand-receptor-function axis obtained from label-free detection technology. This review covers various platform technologies used for the research of GPCRs, concentrating on the principal, non-radiometric homogeneous assay technologies. As current technology is rapidly advancing, the combination of probe chemistry, optical instruments, and GPCR biology will provide us with many new technologies to apply in the future.

• Journal of Photoscience
• /
• 제4권3호
• /
• pp.97-103
• /
• 1997

The effect of temperature on the fluorescence quenching of 2-(4-Methoxyphenyl)-5-(1-naphthyl)-1,3,4-oxadiazole (MPNO1), 2-(4-Methoxyphenyl)-5-(2-naphthyl)-1,3,4-oxadiazote(MPNO2), by aniline, and 2-Phenylindole (2-PI) by CCk, in toluene by steady state method and in benzene by time-resolved method have been carried out in the temperature range 30 - 70$\circ$C. The Stem-Volmer (S-V) plots, I$_0$/I against quencher concentration [Q] at different temperanares show positive deviations. The fluorescence lifetimes determined at different temperatures show no systematic variations and the variations being within the experimental error, the average values of lifetimes $ $\tau$ (t) are taken for further calculations. Rate constants such as Stem-Volmer quenching constants K$_sv}$, quenching rate parameters k$_q$ and k'$_q$, static quenching constant V and kinetic distance r are determined using the modified Stem-Volmer equation and sphere of action static quenching model. In order to see whether the reactions are diffusion limited, equations k$_q$ = e$^{-Eq/RT}$ and k'$_q$ = e$^{-Eq/RT}$ are used to determine the values of E$_q$ and E'$_q$, the activation energies for collisional quenching and the values of E$_q$ are 14.53. 17.28 and 16.20 kJ mole$^{-1}$ for MPNO1, MPNO2 and 2-PI respectively and the values of E'$_q$ are 14.62 and 17.73 for MPNO1 and MPNO2 respectively. From the magnitudes of various quantities it has been concluded that the reactions are diffusion limited and the observed positive deviations in the S-V plot are due to static and dynamic quenching.

• Bulletin of the Korean Chemical Society
• /
• 제28권8호
• /
• pp.1249-1255
• /
• 2007

We have investigated the photophysical properties of dansyl-N-methylaminobenzoic acid (DABAH) as a ligand and its lanthanide (Ln3+)-cored complexes (Ln3+-(DABA)3(terpy)) in order to determine the main energy transfer pathway for sensitized near infrared emission of Ln3+ ions (Ln3+ = Nd3+ and Er3+) in Ln3+- (DABA)3(terpy). The fluorescence spectrum of DABAH shows a large Stokes shift with increasing solvent polarity. This large Stokes shift might be due to the formation of a twisted intramolecular charge transfer (TICT) state, as demonstrated by the large dipole moment in the excited state. It is in good agreement with the result that the phosphorescence even in the Gd3+-cored complex based on the DABAH ligand was not observed, maybe due to the highly forbidden character of the S1 → T1 transition in the DABAH ligand. A short decay component (ca. 1 ns) was observed in Er3+-(DABA)3(terpy) whereas the fluorescence lifetimes of DABAH and its Gd3+-(DABA)3(terpy) are observed about ~10 ns. The short component could be originated from the energy transfer process between the ligand and the Ln3+ ion. Based on the fluorescence of DABAH its Ln3+- (DABA)3(terpy), the sensitization of Ln3+ luminescence in the Ln3+-(DABA)3(terpy) takes place by the energy transfer via the TICT state of DABAH in the excited singlet state rather than via the excited triplet state.

• 한국임상수의학회지
• /
• 제30권1호
• /
• pp.22-26
• /
• 2013

To monitor the reproductive patterns of endangered orangutan, Time-resolved fluorescence immuno assay (TR-FIA) were used to analyze metabolites of sex hormones in feces. Orangutan had long-term interbirth intervals (amenorrhea) during lactation period in which the secretion of sex hormones was repressed. The concentration of progesterone in the serum of pregnant orangutan was 30fold higher than that in non-pregnant orangutan. However, the concentration of hCG during pregnant period was different from the result of other primates. The present study suggested that age is not the important factor in determining the reproduction capability, because it is rather greatly influenced by the combination of various factors. Tracing metabolites of sex hormones in orangutan feces seems to be provide the effective solution for the infertility in orangutan. This study result shows the basic data in operating conservation project for endangered orangutan.

• Journal of Photoscience
• /
• 제1권1호
• /
• pp.15-23
• /
• 1994

The absorption and fluorescence spectral properties of piroxicam (PRX) in the hydrogenbonding solvents show the most sensitive dependence on the concentration ranging from 8 x 10$^{_5}$ to 2 x10$^{_5}$ M. These are attributed to both the solvent-mediated ground-state intermolecular proton transfer (GSIerPT) leading to formation of the ground state anion and the excited-state intmmolecular proton transfer (ESIraPT). The concentration dependences of the time-resolved emission kinetics at both room temperature and 77 K have also been investigated. It is shown that in the excited state, the ESIraPT of PRX is the dominant process to form a keto tautomer at the high concentration, whereas at the low concentration the excited-state conformational change of the anion is an additional process leading to formation of a zwitterion. The ESI~PT of PRX in the hydrogenbonding solvent is coupled with the ultrafast excited-state solvent reorganization.

• 한국재료학회지
• /
• 제6권12호
• /
• pp.1242-1247
• /
• 1996

Spatially fixed bichromophoric systems with nonidentical chromophores have been extensively employed for studies of electron transfer and excitation transfer. Excitation hopping behavior between two naphthy1 moieties on 7,14-dihydro-7,14-ethanodibenz[a,h] anthracene(DEA)has been explored by the time-resolved fluorescence anisotropy measurements. The experimentally obtained value of the hopping rate in DEA agrees at least qualitatively with that calculated on the basis of the Dexter's theory, but disagrees with that calculated on the basis of the Forster's theory, indicates that for a pair of donor and acceptor with inter-chromophore separation as short as 4.5 $\AA$, excitation transfer via electron exchange is a predominant process.

• Bulletin of the Korean Chemical Society
• /
• 제17권7호
• /
• pp.616-621
• /
• 1996

The transfer of excitation energy from solvent to solute in polystyrene films doped with 2-(2'-hydroxyphenyl)benzothiazole (HBT) which undergoes intramolecular proton transfer in excited electronic state has been studied by employing steady state and time-resolved fluorescence measurements. The degree of Forster overlap between donor and acceptor molecule in this system is estimated to be moderate. Energy transfer efficiency increases with solute concentration at low concentration range and levels off at high concentration. It is observed that the excimer form of polystyrene is largely involved in energy transfer process. Photostability of HBT in polystyrene to UV light is also investigated to get insight into the long wavelength absorption band of HBT which was observed upon electron radiation.

• 방사성폐기물학회지
• /
• 제20권4호
• /
• pp.371-382
• /
• 2022

Carbonates are inorganic ligands that are abundant in natural groundwater. They strongly influence radionuclide mobility by forming strong complexes, thereby increasing solubility and reducing soil absorption rates. We characterized the spectroscopic properties of Am(III)-carbonate species using UV-Vis absorption and time-resolved laser-induced fluorescence spectroscopy. The deconvoluted absorption spectra of aqueous Am(CO₃)₂^- and Am(CO₃)₃^3- species were identified at red-shifted positions with lower molar absorption coefficients compared to the absorption spectrum of aqua Am³⁺. The luminescence spectrum of Am(CO₃)₃^3- was red-shifted from 688 nm for Am³⁺ to 695 nm with enhanced intensity and an extended lifetime. Colloidal Am(III)-carbonate compounds exhibited absorption at approximately 506 nm but had non-luminescent properties. Slow formation of colloidal particles was monitored based on the absorption spectral changes over the sample aging time. The experimental results showed that the solubility of Am(III) in carbonate solutions was higher than the predicted values from the thermodynamic constants in OECD-NEA reviews. These results emphasize the importance of kinetic parameters as well as thermodynamic constants to predict radionuclide migration. The identified spectroscopic properties of Am(III)-carbonate species enable monitoring time-dependent species evolution in addition to determining the thermodynamics of Am(III) in carbonate systems.

• 한국대기환경학회지
• /
• 제22권5호
• /
• pp.590-603
• /
• 2006

Size-and time-resolved aerosol samples were collected using an eight-stage Davis rotating unit for monitoring (DRUM) sampler from 23 March to 29 April 2001 at Gosan, Jeju Island, Korea, which is one of the super sites of Asia-Pacific Regional Aerosol Characterization Experiment(ACE-Asia). These samples were analyzed using synchrotron X-ray fluorescence for 3-hr average concentrations of 19 elements including Al, Si, S, Cl, K, Ca, Ti, V, Cr, Mn, Fe, Ni, Cu, Zn, As, Se, Br, Rb, and Pb. The size-resolved data sets were then analyzed using the positive matrix factorization(PMF) technique to identify possible sources and estimate their contributions to particulate matter mass. PMF analysis uses the uncertainty of the measured data to provide an optimal weighting. Twelve sources were resolved in eight size ranges($0.09{\sim}12{\mu}m$) and included continental soil, local soil, sea salt, biomass/biofuel burning, coal combustion, oil combustion, municipal incineration, nonferrous metal source, ferrous metal source, gasoline vehicle, diesel vehicle, and volcanic emission. The PMF result of size-resolved source contributions showed that natural sources represented by local soil, sea salt, continental soil, and volcanic emission contributed about 79% to the predicted primary particulate matter(PM) mass in the coarse size range ($1.15{\sim}12{\mu}m$) while anthropogenic sources such as coal combustion and biomass/biofuel burning contributed about 58% in the fine size range($0.56{\sim}2.5{\mu}m$). The diesel vehicle source contributed mostly in ultra-fine size range($0.09{\sim}0.56{\mu}m$) and was responsible for about 56% of the primary PM mass.

• Bulletin of the Korean Chemical Society
• /
• 제23권2호
• /
• pp.281-285
• /
• 2002

The photophysical properties and the singlet oxygen generation efficiencies of meso-tetraphenyl-trithiasapphyrin $(S_3TPS)$ and meso-tetmkis(p-methoxy phenyl)-trithiasapphy rin ((p-MeO)-$S_3TPS$) have been investigated, utilizing steady-state and time-resolved spectroscopic methods to elucidate the possibility of their use as photosensitizers for photodynamic therapy (PDT). The observed photophysical properties were compared with those of other porphyrin-like photosensitizers in geometrical and electronic structural aspects, such as extended ${\pi}$ conjugation, structural distortion, and internal heavy atoms. The steady-state electronic absorption and fluorescence spectra were both red-shifted due to the extended ${\pi}$-conjugation. The fluorescence quantum yields were measured as very small. Even though intersystem crossing rates were expected to increase due to the increment of spin orbital coupling, the triplet quantum yields were measured as less than 0.15. Such characteristics can be ascribed to the more enhanced internal conversion rates compared with the intersystem crossing rates. Furthermore, the triplet state lifetimes were shortened to -1.0 ${\mu}s$ as expected. Therefore, the singlet oxygen quantum yields were estimated to be near zero due to the fast triplet state decay rates and the inefficient energy transfer to the oxygen molecule as well as the low triplet quantum yields. The low efficiencies of energy transfer to the oxygen molecule can be attributed to the lower oxidation potential and/or the energetically low lying triplet state. Such photophysical factors should be carefully evaluated as potential photosensitizers that have extended ${\pi}$-conjugation and heavy core atoms synthesized for red-shifted absorption and high triplet state quantum yields.