The kinetics of G-protein-coupled receptor activation and deactivation has, so far, been measured only indirectly, most frequently by assessing the production of various second messengers. We have developed methods based on fluorescence resonance energy transfer to quantify the kinetics of receptor activation by agonist (measured as conformational change in the receptor), the kinetics of G-prot...

objective(s): we previously reported a series of quinazoline derivatives as vascular-targeting anticancer agents. in this study, we investigated the mechanism underlying the anti-angiogenic activity of the quinazoline derivative compound 11d. materials and methods: we examined the effects of quinazoline derivative 11d on vascular endothelial growth factor receptor-2 (vegfr2) activation via vegf...

cladribine, an analogue of deoxyadenosine, is highly toxic for both non-dividing and proliferating cells and has shown activity in the treatment of several malignancies. therefore, the aim of the present study is to investigate the cytotoxicity effect of cladribine (2-cda) on the breast cancer cell line, mcf-7 (estrogen receptor positive, er+). mtt assay, annexin v-fluorescein/pi and hoechst 33...

introduction: stimulation of peptidergic fibers activates microglia in the dorsal horn. microglia activation causes fractalkine (fkn) release, a neuron-glia signal, which enhances pain. the transient vanilloid receptor 1 (trpv1) mediates the release of neuropeptides, which can subsequently activate glia. trpv1 and trpv2 are generally expressed on c and aδ fibers, respectively. expression of bot...

cellular and molecular pathways link thrombosis and innate immune system during sepsis. extrinsic pathway activation of protease thrombin through fviia and tissue factor (tf) in sepsis help activate its endothelial cell (ec) membrane protease activated receptor 1 (par-1). thrombin adjusts the ec cycle through activation of g proteins (g12/13), and later through rho gefs (guanine nucleotide exch...